Jacob Schor ND FABNO

December 2011




“Here we come a-wassailing

Among the leaves so green,

Here we come a wand'ring,

So fair to be seen.”



I tend to ignore things I don’t recognize.  Take wassail for example. I’ve heard the verses of this song all my life, but it wasn’t until someone handed me a steaming cup of hot wassail to drink that I had a clue what wassail was.



“Love and joy come to you,

And to you a wassail too,

And God bless you

And send you a happy new year,

And God send you a happy new year.”


The word wassail is old English (OE) and so dates from before 1066. It derives from the Old Norse 'Ves heill', that was turned into the Anglo-Saxon toast “wæs þu hæl,” meaning "be thou hale" or "be in good health." [I assume that the Old English letters in that phrase will be lost in this email.]


While wassail is a spiced beverage, wassailing is also a verb. Wassailing as an active practice falls into two distinct categories. There is a wassail that can be translated as a kind of active “house-visiting”, somewhat akin to Christmas caroling, but with a hint of Halloween Trick or Treating to it. Then there is what can best be described as orchard wassailing, a practice that probably goes far back into history and refers to a practice of singing to apple trees to promote a good harvest for the coming year.  This wassailing tradition predates the celebration of Christmas.


The house visiting wassailing has its roots in the middle ages.  Peasants would arrive at the homes of their lords, while not actually begging, but in a choreographed bit of demanding that ended with the lords giving  them gifts.  Apparently tradition allowed the peasants to be surprisingly demanding with their expectations of feast and drink.


We are not daily beggars

Who beg from door to door,

But we are neighbour's children

Whom you have seen before.


These familiar words to this song, probably the best known of all the wassail songs, were well-known throughout England in the middle 19th century. Its roots may go back even further. The editors of The Oxford Book of Carols (OBC) suggest that Shakespeare may have heard this song sung outside of his house at Christmas. [1]


There are many recipes for the wassail beverage.  Almost all use apple cider as a base to which various exotic and imported spices were added.  There are some recipes that forget about the original tree ritual entirely and add a few spices to beer. 


There are endless variations of wassail recipes on the web.  All seem to contain exotic ingredients that if available in early England were clearly only found at the tables of the very well off.


Here’s a basic recipe:


2 quarts Apple Cider

              1 cup     Orange Juice

              1 cup     Lemon Juice

              1 cup     Pineapple Juice

              3 sticks Cinnamon

              2 teaspoons Whole Cloves

              1/3 cup honey


Combine all ingredients.  Heat for 1 hour to combine the flavors.  Some recipes add baked apples, tea, cranberry juice or beaten eggs.  Our colleague Dr. Jenny DeMeaux tells me she adds Red Hots.


There is little chance that this is the wassail that Shakespeare knew in his time, especially the redhots. 


Reading the various recipes and the ingredients for wassail, one still finds that they are quite healthy and that they would instill better health, especially in lean times, to people deprived of fresh produce.  The large quantities of lemon juice and orange juice may have provided the vitamin C needed to ward off scurvy.


In recent years medical researchers have begun to realize that apples are good for health and protect against disease.  They protect against cancer, heart disease and pulmonary problems.  


In the October 2008 issue of Planta Medica, Gerhauser reviewed the current knowledge on the anti-cancer actions of apples. “In brief, apple extracts and components, especially oligomeric procyanidins, have been shown to influence multiple mechanisms relevant for cancer prevention in in vitro studies. These include antimutagenic activity, modulation of carcinogen metabolism, antioxidant activity, anti-inflammatory mechanisms, modulation of signal transduction pathways, antiproliferative and apoptosis-inducing activity, as well as novel mechanisms on epigenetic events and innate immunity.”     The chemicals in apples appear to trigger apoptosis (suicide) in genetically damaged cells.  The procyanidins contained in apples offer protection against colon cancer. 


On of my research heroes, Liu from Cornell University successfully demonstrated in a rat model of human breast cancer that moderate apple consumption lowered risk. “…. whole apple extracts prevent mammary cancer in a rat model in a dose-dependent manner at doses comparable to human consumption of one, three, and six apples a day. This study demonstrated that whole apple extracts effectively inhibited mammary cancer growth in the rat model; thus, consumption of apples may be an effective strategy for cancer protection”


Apples are an excellent source of quercetin, a chemical usually appreciated for its anti cancer effect. A November 2007 paper added a new use for quercetin into our materia medica, it lowers blood pressure. “These data are the first to our knowledge to show that quercetin supplementation reduces blood pressure in hypertensive subjects.”

A July 2008 paper tells us the chemical mechanism that allows apples to protect against atherosclerosis.  A 2010 trial suggests that applejuice improves Alzheimer’s disease.


Apples also offer protection against asthma and COPD.  Interestingly researchers haven’t been able to pinpoint which particular flavonoid is responsible.  Mixed all together in apples they work but tested separately they don’t seem to work.


All the recipes for wassail include orange juice and lemon juice.  Neither grow in England but were in earlier times probably imported from Spain and possibly other Mediterranean countries.  We’ve all grown up knowing that both juices contain vitamin C and thus were healthy.  A summary paper on the health benefits of orange juice published in August 2008 tells us there is a lot going on in citrus fruits and reviewed new findings in anticancer, cardiovascular, and anti-inflammatory activity.  The results of a clinical trial reported in August 2010 tell us that drinking orange juice helped women engaged in an exercise program improve their lipid profile.


It should be noted that intake of either apple juice or orange juice is reported to reduce peak plasma levels of aliskiren by 80%   Don’t recognize the name aliskiren?  It’s a blood pressure medication, sold under the trade name Tekturna, in the U.S.


Back in 2006 a paper suggested that orange juice might be useful in preventing or treating osteoporosis.  In a study of orchectomized rats those given daily orange juice increased their bone density, bone strength, blood antioxidant levels and other measures of health.


All the wassail recipes seem to include cinnamon and other exotic spices.  Spices have long been valued for their health and medicinal properties.  Of late, cinnamon especially has been the subject of some interesting research.  In December 2008, a paper suggested that cinnamon oil added to hot springs could keep them free from bacterial overgrowth particularly the nasty bugs that cause Legionaire’s Disease.   The preceding summer, another paper suggested cinnamon could protect against colon cancer.  The chemical constituents of cinnamon  have anti inflammatory effects,    reduce insulin resistance and have an antiglycation effect.

A paper set for publication in January 2012 suggests that at least in rats, cinnamon lowers cholesterol levels.   A clinical trial from 2011 informs us that cinnamon chewing gums kill off bacteria in the mouth associated with bad breath.  An October 2010 report tells us that taking 2 grams per day of cinnamon successfully lowered blood sugar levels in people diagnosed type 2 diabetes.


Cloves apparently have the highest radical scavenging activity of any of the common spices. They also have a strong chelating action on heavy metals. Components of cloves have been suggested as a possible treatment for Parkinson’s Disease.


It takes little imagination to think that for a hungry and somewhat undernourished people, that a generous helping of wassail might have provided a significant impact at improving the health of those who consumed it.


Tradition has it that the proper time to go wassailing is the Twelfth Night of Christmas but it doesn't hurt to start early and continue later.






God bless the Master of this house,

Likewise the Mistress too;

And all the little children

That round the table go.






Planta Med. 2008 Oct;74(13):1608-24. Epub 2008 Oct 14.Links

    Cancer chemopreventive potential of apples, apple juice, and apple components.

    Gerhauser C.


    Division of Toxicology and Cancer Risk Factors, German Cancer Research Center (DKFZ), Heidelberg, Germany. c.gerhauser@dkfz.de


    Apples ( MALUS sp., Rosaceae) are a rich source of nutrient as well as non-nutrient components and contain high levels of polyphenols and other phytochemicals. Main structural classes of apple constituents include hydroxycinnamic acids, dihydrochalcones, flavonols (quercetin glycosides), catechins and oligomeric procyanidins, as well as triterpenoids in apple peel and anthocyanins in red apples. Several lines of evidence suggest that apples and apple products possess a wide range of biological activities which may contribute to health beneficial effects against cardiovascular disease, asthma and pulmonary dysfunction, diabetes, obesity, and cancer (reviewed by Boyer and Liu, Nutr J 2004). The present review will summarize the current knowledge on potential cancer preventive effects of apples, apple juice and apple extracts (jointly designated as apple products). In brief, apple extracts and components, especially oligomeric procyanidins, have been shown to influence multiple mechanisms relevant for cancer prevention in IN VITRO studies. These include antimutagenic activity, modulation of carcinogen metabolism, antioxidant activity, anti-inflammatory mechanisms, modulation of signal transduction pathways, antiproliferative and apoptosis-inducing activity, as well as novel mechanisms on epigenetic events and innate immunity. Apple products have been shown to prevent skin, mammary and colon carcinogenesis in animal models. Epidemiological observations indicate that regular consumption of one or more apples a day may reduce the risk for lung and colon cancer.



J Nutr Biochem. 2007 Jul;18(7):427-42. Epub 2007 Feb 23.Click here to read Links

    Effects of dietary flavonoids on apoptotic pathways related to cancer chemoprevention.

    Ramos S.


    Department of Metabolism and Nutrition, Instituto del Frío, Consejo Superior de Investigaciones Científicas, 28040 Madrid, Spain. s.ramos@if.csic.es <s.ramos@if.csic.es>


    Epidemiological studies have described the beneficial effects of dietary polyphenols (flavonoids) on the reduction of the risk of chronic diseases, including cancer. Moreover, it has been shown that flavonoids, such as quercetin in apples, epigallocatechin-3-gallate in green tea and genistein in soya, induce apoptosis. This programmed cell death plays a critical role in physiological functions, but there is underlying dysregulation of apoptosis in numerous pathological situations such as Parkinson's disease, Alzheimer's disease and cancer. At the molecular level, flavonoids have been reported to modulate a number of key elements in cellular signal transduction pathways linked to the apoptotic process (caspases and bcl-2 genes), but that regulation and induction of apoptosis are unclear. The aim of this review is to provide insights into the molecular basis of the potential chemopreventive activities of representative flavonoids, with emphasis on their ability to control intracellular signaling cascades responsible for regulating apoptosis, a relevant target in cancer-preventive approach.


Carcinogenesis. 2005 Jul;26(7):1291-5. Epub 2005 Mar 24.Click here to read Links

    Chemopreventive properties of apple procyanidins on human colon cancer-derived metastatic SW620 cells and in a rat model of colon carcinogenesis.

    Gossé F, Guyot S, Roussi S, Lobstein A, Fischer B, Seiler N, Raul F.


    Laboratoire d'Oncologie Nutritionnelle, Université Louis Pasteur EA 3430, Institut de Recherche contre les Cancers de l'Appareil Digestif (IRCAD), Strasbourg, France.


    Apples contain several classes of polyphenols: monomers (catechins, epicatechins) and oligomers/polymers, such as the procyanidins. Our aim was (i) to study anti-proliferative mechanisms on human metastatic colon carcinoma (SW620 cells) of apple polyphenol fractions (monomers or procyanidins) and (ii) to evaluate their anti-carcinogenic properties in vivo. Two polyphenol-enriched fractions were isolated from apples. Fraction non-procyanidins contained 73% phenolic monomers and no procyanidins, while fraction procyanidins contained 78% procyanidins and no monomers. Inhibition of SW620 cell growth was only observed with fraction P (IC50 = 45 microg/ml). After a 24-h exposure of cells to fraction P, protein kinase C activity was inhibited by 70% and a significant increase in extracellular signal-regulated kinases 1 and 2 and c-jun N-terminal kinases expression was observed together with the down-regulation of polyamine biosynthesis and the activation of caspase-3. Colon carcinogenesis was induced in rats by intraperitoneal injections of azoxymethane, once a week for 2 weeks. Seven days after the last injection, Wistar rats received fraction P (0.01%) dissolved in drinking water. After 6 weeks of treatment, the colon of rats receiving procyanidins showed a significant (P < 0.01) reduction of the number of preneoplastic lesions when compared with controls receiving water. The total number of hyperproliferative crypts and of aberrant crypt foci was reduced by 50% in rats receiving 0.01% apple procyanidins in their drinking water. Our results show that apple procyanidins alter intracellular signaling pathways, polyamine biosynthesis and trigger apoptosis in tumor cells. These compounds antagonize cancer promotion in vivo. In contrast with absorbable drugs, these natural, non toxic, dietary constituents reach the colon where they are able to exert their antitumor effects.



J Agric Food Chem. 2005 Mar 23;53(6):2341-3.Click here to read Links

    Apples prevent mammary tumors in rats.

    Liu RH, Liu J, Chen B.


    Department of Food Science, Cornell University, Ithaca, New York 14853-7201, USA. RL23@cornell.edu


    Regular consumption of fruits and vegetables has been consistently shown to be associated with reduced risk of developing chronic diseases such as cancer and cardiovascular disease. Apples are commonly consumed and are the major contributors of phytochemicals in human diets. It was previously reported that apple extracts exhibit strong antioxidant and antiproliferative activities and that the major part of total antioxidant activity is from the combination of phytochemicals. Phytochemicals, including phenolics and flavonoids, are suggested to be the bioactive compounds contributing to the health benefits of apples. Here it is shown that whole apple extracts prevent mammary cancer in a rat model in a dose-dependent manner at doses comparable to human consumption of one, three, and six apples a day. This study demonstrated that whole apple extracts effectively inhibited mammary cancer growth in the rat model; thus, consumption of apples may be an effective strategy for cancer protection.


J Nutr. 2007 Nov;137(11):2405-11.Click here to read Links

    Quercetin reduces blood pressure in hypertensive subjects.

    Edwards RL, Lyon T, Litwin SE, Rabovsky A, Symons JD, Jalili T.


    Division of Nutrition, University of Utah, Salt Lake City, UT 84112, USA.


    Epidemiological studies report that quercetin, an antioxidant flavonol found in apples, berries, and onions, is associated with reduced risk of coronary heart disease and stroke. Quercetin supplementation also reduces blood pressure in hypertensive rodents. The efficacy of quercetin supplementation to lower blood pressure in hypertensive humans has never been evaluated. We tested the hypothesis that quercetin supplementation reduces blood pressure in hypertensive patients. We then determined whether the antihypertensive effect of quercetin is associated with reductions in systemic oxidant stress. Men and women with prehypertension (n = 19) and stage 1 hypertension (n = 22) were enrolled in a randomized, double-blind, placebo-controlled, crossover study to test the efficacy of 730 mg quercetin/d for 28 d vs. placebo. Blood pressure (mm Hg, systolic/diastolic) at enrollment was 137 +/- 2/86 +/- 1 in prehypertensives and 148 +/- 2/96 +/- 1 in stage 1 hypertensive subjects. Blood pressure was not altered in prehypertensive patients after quercetin supplementation. In contrast, reductions in (P < 0.01) systolic (-7 +/- 2 mm Hg), diastolic (-5 +/- 2 mm Hg), and mean arterial pressures (-5 +/- 2 mm Hg) were observed in stage 1 hypertensive patients after quercetin treatment. However, indices of oxidant stress measured in the plasma and urine were not affected by quercetin. These data are the first to our knowledge to show that quercetin supplementation reduces blood pressure in hypertensive subjects. Contrary to animal-based studies, there was no quercetin-evoked reduction in systemic markers of oxidative stress.



J Agric Food Chem. 2008 Jul 23;56(14):5558-63. Epub 2008 Jun 18.Click here to read Links

    Apple polyphenols and fibers attenuate atherosclerosis in apolipoprotein E-deficient mice.

    Auclair S, Silberberg M, Gueux E, Morand C, Mazur A, Milenkovic D, Scalbert A.


    Unité de Nutrition Humaine, UMR1019, INRA, Centre de Recherche de Clermont Ferrand/Theix, 63122 Saint-Genès-Champanelle, France.


    Atherosclerosis, which is closely linked to nutritional habits, is a major cause of mortality in Western countries. Most of the previous investigations carried out on health effects of apples have been focused on their capacity to lower lipid concentration as well as on their antioxidant effects. The aim of the present study was to investigate the antiatherosclerotic effects of apple polyphenols and fibers. A crude apple polyphenol extract and low-viscosity apple fibers isolated from cider apples were administered separately or in association with the diet of apo E-deficient mice. After 4 months of supplementation, lipemia and oxidative stress biomarkers were measured and atheroslerotic lesions assessed by histomorphometry. Total plasmatic cholesterol and triacylgycerol levels were not affected by supplementation, and hepatic cholesterol level was lower in the group supplemented with both fibers and polyphenols. Uric acid concentrations and antioxidant capacity (FRAP) in plasma were reduced in all groups supplemented with polyphenols or fibers. The mean lesion area was reduced by 17, 38, and 38%, respectively, for the polyphenol, fiber, and polyphenol + fiber groups. Apple constituents supplied at nutritional doses therefore limit the development of atherosclerotic lesions in the aorta of apo E-deficient mice. On the basis of the results, we hypothesize that apple fibers and polyphenols may play a role in preventing atherosclerosis disease by decreasing uric acid plasma level.



Am J Alzheimers Dis Other Demen. 2010 Jun;25(4):367-71. Epub 2010 Mar 25.

Apple juice improved behavioral but not cognitive symptoms in moderate-to-late stage Alzheimer's disease in an open-label pilot study.

Remington R, Chan A, Lepore A, Kotlya E, Shea TB.


Center for Cell Neurobiology and Neurodegeneration Research, University of Massachusetts-Lowell, USA.


Preclinical studies demonstrate that apple juice exerts multiple beneficial effects including reduction of central nervous system oxidative damage, suppression of Alzheimer's disease (AD) hallmarks, improved cognitive performance, and organized synaptic signaling. Herein, we initiated an open-label clinical trial in which 21 institutionalized individuals with moderate-to-severe AD consumed 2 4-oz glasses of apple juice daily for 1 month. Participants demonstrated no change in the Dementia Rating Scale, and institutional caregivers reported no change in Alzheimer's Disease Cooperative Study (ADCS)-Activities of Daily Living (ADL) in this brief study. However, caregivers reported an approximate 27% (P < .01) improvement in behavioral and psychotic symptoms associated with dementia as quantified by the Neuropsychiatric Inventory, with the largest changes in anxiety, agitation, and delusion. This pilot study suggests that apple juice may be a useful supplement, perhaps to augment pharmacological approaches, for attenuating the decline in mood that accompanies progression of AD, which may also reduce caregiver burden.





Eur Respir J. 2005 Sep;26(3):449-52.Click here to read Links

    Dietary intake of flavonoids and asthma in adults.

    Garcia V, Arts IC, Sterne JA, Thompson RL, Shaheen SO.


    Dept of Public Health Sciences, King's College London, 5th Floor, Capital House, 42 Weston St, London, SE1 3QD, UK.


    Epidemiological studies have suggested that a high consumption of apples may protect against asthma and chronic obstructive pulmonary disease. This effect has been attributed to their high flavonoid content, but few studies have investigated the relationship between flavonoid intake and obstructive lung disease directly. In a population-based, case-control study of 1,471 adults aged 16-50 yrs in London (UK), the present study examined whether dietary intake of catechins, flavonols and flavones was negatively associated with asthma, asthma severity and chronic sputum production. Asthma was defined by positive responses to a standard screening questionnaire in 1996 and information about usual diet was obtained by a food frequency questionnaire in 1997. After controlling for potential confounders, dietary intake of these three flavonoid subclasses was not significantly associated with asthma, (odds ratio per quintile (95% confidence interval) = 0.94 (0.86-1.02); 1.00 (0.92-1.09); 0.98 (0.88 -1.08) for flavones, flavonols and total catechins, respectively) nor was it associated with asthma severity, or chronic sputum production. In conclusion, no evidence was found for a protective effect of three major subclasses of dietary flavonoids on asthma. It is possible that other flavonoids or polyphenols present in apples may explain the protective effect of apples on obstructive lung disease.



J Agric Food Chem. 2008 Aug 13;56(15):6185-205. Epub 2008 Jul 2.Click here to read Links

    Update on uses and properties of citrus flavonoids: new findings in anticancer, cardiovascular, and anti-inflammatory activity.

    Benavente-García O, Castillo J.


    Research and Development Department of Nutrafur-Furfural Español S.A., Camino Viejo de Pliego s/n, 80320 Alcantarilla, Murcia, Spain. laboratorio@nutrafur.com


    Significantly, much of the activity of Citrus flavonoids appears to impact blood and microvascular endothelial cells, and it is not surprising that the two main areas of research on the biological actions of Citrus flavonoids have been inflammation and cancer. Epidemiological and animal studies point to a possible protective effect of flavonoids against cardiovascular diseases and some types of cancer. Although flavonoids have been studied for about 50 years, the cellular mechanisms involved in their biological action are still not completely known. Many of the pharmacological properties of Citrus flavonoids can be linked to the abilities of these compounds to inhibit enzymes involved in cell activation. Attempts to control cancer involve a variety of means, including the use of suppressing, blocking, and transforming agents. Suppressing agents prevent the formation of new cancers from procarcinogens, and blocking agents prevent carcinogenic compounds from reaching critical initiation sites, while transformation agents act to facilitate the metabolism of carcinogenic components into less toxic materials or prevent their biological actions. Flavonoids can act as all three types of agent. Many epidemiological studies have shown that regular flavonoid intake is associated with a reduced risk of cardiovascular diseases. In coronary heart disease, the protective effects of flavonoids include mainly antithrombotic, anti-ischemic, anti-oxidant, and vasorelaxant. It is suggested that flavonoids decrease the risk of coronary heart disease by three major actions: improving coronary vasodilatation, decreasing the ability of platelets in the blood to clot, and preventing low-density lipoproteins (LDLs) from oxidizing. The anti-inflammatory properties of the Citrus flavonoids have also been studied. Several key studies have shown that the anti-inflammatory properties of Citrus flavonoids are due to its inhibition of the synthesis and biological activities of different pro-inflammatory mediators, mainly the arachidonic acid derivatives, prostaglandins E 2, F 2, and thromboxane A 2. The anti-oxidant and anti-inflammatory properties of Citrus flavonoids can play a key role in their activity against several degenerative diseases and particularly brain diseases. The most abundant Citrus flavonoids are flavanones, such as hesperidin, naringin, or neohesperidin. However, generally, the flavones, such as diosmin, apigenin, or luteolin, exhibit higher biological activity, even though they occur in much lower concentrations. Diosmin and rutin have a demonstrated activity as a venotonic agent and are present in several pharmaceutical products. Apigenin and their glucosides have been shown a good anti-inflammatory activity without the side effects of other anti-inflammatory products. In this paper, we discuss the relation between each structural factor of Citrus flavonoids and the anticancer, anti-inflammatory, and cardiovascular protection activity of Citrus flavonoids and their role in degenerative diseases.


    PMID: 18593176 [PubMed - indexed for MEDLINE]



Maturitas. 2010 Dec;67(4):343-7. Epub 2010 Aug 21.

Orange juice improved lipid profile and blood lactate of overweight middle-aged women subjected to aerobic training.

Aptekmann NP, Cesar TB.


Food and Nutrition Department, Faculty of Pharmaceutical Sciences, Sao Paulo State University (UNESP), Araraquara, Brazil. naptekmann@yahoo.com.br



This study investigated how consumption of orange juice associated with aerobic training affected serum lipids and physical characteristics of overweight, middle-aged women.


The experimental group consisted of 13 women who consumed 500 mL/d of orange juice and did 1h aerobic training 3 times a week for 3 months. The control group consisted of another 13 women who did the same aerobic training program but did not consume orange juice.


At the end of the experiment, the control group lost an average of 15% of fat mass (P<0.05) and 2.5% of weight (P<0.05), whereas the experimental group lost 11% of fat mass and 1.2% of weight (P<0.05). Consumption of orange juice by the experimental group was associated with increased dietary intake of vitamin C and folate by 126% and 61% respectively. Serum LDL-C decreased 15% (P<0.05) and HDL-C increased 18% (P<0.05) in the experimental group, but no significant change was observed in the control group. Both groups improved the anaerobic threshold by 20% (P<0.05), but blood lactate concentration decreased 27% in the experimental group compared to the 17% control group, suggesting that experimental group has less muscle fatigue and better response to training.


The consumption of 500 mL/d of orange juice associated with aerobic training in overweight women decreased cardiovascular disease risk by reducing LDL-C levels and increasing HDL-C levels. This association also decreased blood lactate concentration and increased anaerobic threshold, showing some improvement in the physical performance.

Copyright © 2010 Elsevier Ireland Ltd. All rights reserved.



Br J Clin Pharmacol. 2011 May;71(5):718-26. doi: 10.1111/j.1365-2125.2010.03898.x.

Orange and apple juice greatly reduce the plasma concentrations of the OATP2B1 substrate aliskiren.

Tapaninen T, Neuvonen PJ, Niemi M.


Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, Helsinki, Finland.



The aim of this study was to investigate the effects of orange juice and apple juice on the pharmacokinetics and pharmacodynamics of aliskiren.


In a randomized crossover study, 12 healthy volunteers ingested 200 ml of orange juice, apple juice or water three times daily for 5 days. On day 3, they ingested a single 150-mg dose of aliskiren. Plasma aliskiren concentrations were measured up to 72 h, its excretion into urine up to 12 h and plasma renin activity up to 24 h.


Orange and apple juice reduced aliskiren peak plasma concentrations by 80% (95% CI 63%, 89%, P < 0.001) and 84% (95% CI 72%, 91%, P < 0.001), and the area under the plasma aliskiren concentration-time curve (AUC) by 62% (95% CI 47%, 72%, P < 0.001) and 63% (95% CI 46%, 74%, P < 0.001), respectively, but had no significant effect on its elimination half-life or renal clearance. The decreases in aliskiren AUC by orange and apple juice correlated with aliskiren AUC during the water phase (r= 0.98, P < 0.001). Plasma renin activity was 87% and 67% higher at 24 h after aliskiren during the orange juice and apple juice phases, respectively, than during the water phase (P < 0.05).


Orange juice and apple juice greatly reduce the plasma concentrations and renin-inhibiting effect of aliskiren, probably by inhibiting its OATP2B1-mediated influx in the small intestine. Concomitant intake of aliskiren with orange or apple juice is best avoided.

© 2011 The Authors. British Journal of Clinical Pharmacology © 2011 The British Pharmacological Society.


Nutrition. 2006 May;22(5):559-63. Epub 2006 Feb 10.Click here to read Links

    Citrus juice modulates bone strength in male senescent rat model of osteoporosis.

    Deyhim F, Garica K, Lopez E, Gonzalez J, Ino S, Garcia M, Patil BS.


    Department of Human Sciences, Texas A&M University-Kingville, Kingsville, Texas, USA. farzad.deyhim@tamuk.edu


    OBJECTIVE: An experiment evaluated the effect of citrus juice on enhancing serum antioxidant status and on osteoporosis prevention in orchidectomized rats. METHODS: Thirty-six 1-y-old male rats were randomized to two groups: a sham-control group (n = 9) and an orchidectomized group (n = 27). The orchidectomized group was divided into three groups of nine and assigned to one of the following treatments: orchidectomy, orchidectomy plus orange juice, and orchidectomy plus grapefruit juice. Sixty days after initiation of the study, all rats were killed, blood was collected, and serum was harvested for total antioxidant status and indices of bone formation and resorption. Femoral density and biomechanical properties were monitored. RESULTS: Orchidectomy decreased (P < 0.05) total antioxidant capacity, femoral density, and biomechanical properties and increased (P < 0.05) alkaline phosphatase, acid phosphatase, and urinary excretion of hydroxyproline compared with the sham-control group. In contrast to orchidectomy, orchidectomy plus orange juice and orchidectomy plus grapefruit juice reversed (P < 0.05) orchidectomy-induced antioxidant suppression, decreased (P < 0.05) alkaline phosphatase and acid phosphatase activities, moderately restored (P = 0.07) femoral density, increased (P < 0.05) femoral strength, significantly delayed time-induced femoral fracture, and decreased (P < 0.05) urinary excretion of hydroxyproline. CONCLUSION: The present study supports the supposition in that drinking citrus juice positively affects serum antioxidant status and bone strength.


    PMID: 16472977 [Pu



Water Res. 2008 Dec;42(20):5022-5030. Epub 2008 Sep 27.Click here to read Links

    Influence of pH on bioactivity of cinnamon oil against Legionella pneumophila and its disinfection efficacy in hot springs.

    Chang CW, Chang WL, Chang ST.


    Institute of Environmental Health, College of Public Health, National Taiwan University, Room 740, 7F, No. 17, Xuzhou Road, Taipei 100, Taiwan, Republic of China; Research Center for Genes, Environmental and Human Health, National Taiwan University, Taipei, Taiwan, Republic of China; Center for Research on Environmental and Occupational Health, National Taiwan University, Taipei, Taiwan, Republic of China.


    Cinnamon oil extracted from leaves of Cinnamomum osmophloeum has recently been proved as a promising antibacterial agent against Legionella pneumophila, an etiological agent of human pneumonia known as Legionnaires' disease. However, the pH effects on the efficacy of cinnamon oil against L. pneumophila and its applicability to recreational spring water remain unknown. We therefore determined the bactericidal activity of cinnamon oil at pH 3-10 in phosphate-buffered saline (PBS) and in four kinds of springs with various conductivity (259-5595muscm(-1)) and pH (2.1-7.7) levels. Results show L. pneumophila cells were more susceptible to cinnamon oil at pH 8-10 than at pH 4-6 in PBS, which became more evident as increasing contact time from 10 to 60min. An increase in concentration of cinnamon oil and contact time significantly increased the anti-L. pneumophila activity (P</=0.001), indicating a consistent biocidal effect regardless of pH. Interestingly, this dose-response biocidal effect was also observed in spring waters. Moreover, L. pneumophila of 4logCFUml(-1) in spring waters was completely inactivated within 60min by cinnamon oil at 300-750mugml(-1), with the highest inactivation in alkaline hydrogen carbonate spring. The great bioactivity of cinnamon oil demonstrates its potential to be used to control Legionella growth in recreational spring water and possibly other niches generally at basic pH, e.g., cooling towers.



Clin Lab Sci. 2008 Summer;21(3):151-7.Links

    Growth inhibition of human colon cancer cells by plant compounds.

    Duessel S, Heuertz RM, Ezekiel UR.


    Department of Clinical Laboratory Science, Doisy College of Health Sciences, Saint Louis University, St. Louis, MO 63104, USA.


    OBJECTIVE: Evidence is accumulating that compounds of plant origin (phytochemicals) exert anti-cancer effects. The purpose of this study was to determine if resveratrol, cinnamaldehyde, and piperine (from red grapes, cinnamon, black pepper respectively) have anti-proliferative effects on colon cancer. DESIGN: Quantitative effects of each phytochemical on concentration responses and time courses of proliferation of cultured human colon cancer cells (DLD-1) were assessed. SETTING: Research was performed at Saint Louis University. MAIN OUTCOMES MEASURES: Responses were measured by spectrophotometry of surviving cells stained by a dye method. RESULTS: Phytochemicals displayed anti-proliferative effects on DLD-1 cells in concentration- and kinetic-dependent manners. Cinnamaldehyde offered statistically significant effects at 24 hours [200 microM], 48 hours [100 - 200 microM], and 72 hours [200 microM]. Piperine displayed a trend towards anti-proliferation at 24 hours and statistically significant inhibition at 48 and 72 hours [100 - 200 microM]. Resveratrol displayed significant anti-proliferative effects at 24 hours [50-200 microM], 48 hours [10-200 microM], and 72 hours [10-200 microM]. CONCLUSION: Cinnamaldehyde, piperine, and resveratrol offer significant in vitro anti-proliferative effects on cultured human colon cancer cells. While each phytochemical exhibited significant anti-proliferative effects, resveratrol results were most impressive in that lower concentrations administered at regular intervals were significantly effective. These results taken together with everyday dietary availability of concentrations used in this study strongly suggest that regular intake of low doses of these phytochemicals offer preventive effects against colon cancer.



Bioresour Technol. 2008 Jun;99(9):3908-13. Epub 2007 Sep 10.Click here to read Links

    Anti-inflammation activities of essential oil and its constituents from indigenous cinnamon (Cinnamomum osmophloeum) twigs.

    Tung YT, Chua MT, Wang SY, Chang ST.


    School of Forestry and Resource Conservation, National Taiwan University, Taipei 106, Taiwan.


    In this study, chemical compositions of hydrodistilled essential oil and anti-inflammatory activities from the twigs of Cinnamomum osmophloeum Kaneh. were investigated for the first time. The chemical constituents of the twig essential oil were further analyzed by GC-MS and they were found to be L-bornyl acetate (15.89%), caryophyllene oxide (12.98%), gamma-eudesmol (8.03%), beta-caryophyllene (6.60%), T-cadinol (5.49%), delta-cadinene (4.79%), trans-beta-elemenone (4.25%), cadalene (4.19%), and trans-cinnamaldehyde (4.07%). The effects of essential oil on nitric oxide (NO) and prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages were also examined. Results of nitric oxide tests indicated that twig essential oil and its major constituents such as trans-cinnamaldehyde, caryophyllene oxide, L-borneol, L-bornyl acetate, eugenol, beta-caryophyllene, E-nerolidol, and cinnamyl acetate have excellent activities. These findings demonstrated that essential oil of C. osmophloeum twigs have excellent anti-inflammatory activities and thus have great potential to be used as a source for natural health products.



PPAR Res. 2008;2008:581348. Epub 2008 Dec 11.Links

    Improved Insulin Resistance and Lipid Metabolism by Cinnamon Extract through Activation of Peroxisome Proliferator-Activated Receptors.

    Sheng X, Zhang Y, Gong Z, Huang C, Zang YQ.


    Key Laboratory of Nutrition and Metabolism, Institute for Nutritional Sciences, Shanghai Institutes for Biological Sciences, Graduate School of CAS, Chinese Academy of Sciences, 319 Yue Yang Road, Shanghai 200031, China.


    Peroxisome proliferator-activated receptors (PPARs) are transcriptional factors involved in the regulation of insulin resistance and adipogenesis. Cinnamon, a widely used spice in food preparation and traditional antidiabetic remedy, is found to activate PPARgamma and alpha, resulting in improved insulin resistance, reduced fasted glucose, FFA, LDL-c, and AST levels in high-caloric diet-induced obesity (DIO) and db/db mice in its water extract form. In vitro studies demonstrate that cinnamon increases the expression of peroxisome proliferator-activated receptors gamma and alpha (PPARgamma/alpha) and their target genes such as LPL, CD36, GLUT4, and ACO in 3T3-L1 adipocyte. The transactivities of both full length and ligand-binding domain (LBD) of PPARgamma and PPARalpha are activated by cinnamon as evidenced by reporter gene assays. These data suggest that cinnamon in its water extract form can act as a dual activator of PPARgamma and alpha, and may be an alternative to PPARgamma activator in managing obesity-related diabetes and hyperlipidemia.



J Agric Food Chem. 2008 Mar 26;56(6):1907-11. Epub 2008 Feb 20.Click here to read Links

    Cinnamon bark proanthocyanidins as reactive carbonyl scavengers to prevent the formation of advanced glycation endproducts.

    Peng X, Cheng KW, Ma J, Chen B, Ho CT, Lo C, Chen F, Wang M.


    School of Biological Sciences, The University of Hong Kong, Hong Kong, People's Republic of China.


    Cinnamon bark has been reported to be effective in the alleviation of diabetes through its antioxidant and insulin-potentiating activities. In this study, the inhibitory effect of cinnamon bark on the formation of advanced glycation endproducts (AGEs) was investigated in a bovine serum albumin (BSA)-glucose model. Several phenolic compounds, such as catechin, epicatechin, and procyanidin B2, and phenol polymers were identified from the subfractions of aqueous cinnamon extract. These compounds showed significant inhibitory effects on the formation of AGEs. Their antiglycation activities were not only brought about by their antioxidant activities but also related to their trapping abilities of reactive carbonyl species such as methylglyoxal (MGO), an intermediate reactive carbonyl of AGE formation. Preliminary study on the reaction between MGO and procyanidin B2 revealed that MGO-procyanidin B2 adducts are primary products which are supposed to be stereoisomers. This is the first report that proanthocyanidins can effectively scavenge reactive carbonyl species and thus inhibit the formation of AGEs. As proanthocyanidins behave in a similar fashion as aminoguanidine (AG), the first AGE inhibitor explored in clinical trials, they show great potential to be developed as agents to alleviate diabetic complications.



Pak J Pharm Sci. 2012 Jan;25(1):141-7.

Lipid lowering effect of Cinnamomum zeylanicum in hyperlipidaemic albino rabbits.

Javed I, Faisal I, Rahman Z, Khan MZ, Muhammad F, Aslam B, Ahmad M, Shahzadi A.


Department of Physiology and Pharmacology, University of Agriculture Faisalabad, Pakistan.


The purpose of the present study was to investigate the lipid lowering effect of Cinnamomum zeylanicum (Cinnamon) in hyperlipidaemic albino rabbits. For this purpose, forty eight albino rabbits were randomly divided into eight equal groups; untreated control on normal routine feed, untreated control on butter and cholesterol, treated control on synthetic cholesterol lowering drug simvastatin (Tablet survive (R) 20 mg), three treated groups on three respective doses of C. zeylanicum bark powder and two treated groups on water and methanol extracts of C. zeylanicum bark powder. Butter ad lib and cholesterol powder 500 mg/kg body weight were used to induce experimental hyperlipidaemia in all groups except untreated control group. The results suggested that C. zeylanicum bark powder at the rate of 0.50 g/kg, 0.75 g/kg and methanol extract equivalent to 0.75 g/kg powder produced respective percent reductions in total lipids by 45, 49 and 64; triglycerides by 38, 53 and 60; total cholesterol by 53, 64 and 69 and LDL-cholesterol by 50, 59 and 62. However, at these dosage levels HDL-cholesterol showed respective percent increase of 42, 48 and 53. Nonetheless, C. zeylanicum bark powder at the level of 0.25g/kg and C. zeylanicum extract in water could not significantly reduce lipid profile indicators. Based on these studies, it can safely be said that C. zeylanicum bark powder methanol extract equivalent to 0.75g/kg bark powder and simvastatin (0.6 mg/kg b. wt.) were equieffective in treating hyperlipidaemia.





J Clin Dent. 2011;22(1):23-6.

Short-term germ-killing effect of sugar-sweetened cinnamon chewing gum on salivary anaerobes associated with halitosis.

Zhu M, Carvalho R, Scher A, Wu CD.


Department of Pediatric Dentistry, College of Dentistry, University of Illinois at Chicago, Chicago, IL, USA.



The present study investigated the short-term germ-killing effect of sugar-sweetened cinnamon chewing gum on total and H2S-producing salivary anaerobes.


Fifteen healthy adult subjects were recruited in the double-blind, crossover clinical study. The three test chewing gums included: 1) sugared chewing gum containing cinnamic aldehyde and natural flavors (CinA+); 2) sugared chewing gum without cinnamic aldehyde but with natural flavors (CinA-); and 3) non-sugared chewing gum base (GB) without any flavors and without cinnamic aldehyde. A three-day "washout" period followed each treatment. Each subject chewed gum under supervision for 20 minutes at 60 chews/minute. Unstimulated whole saliva samples were collected before the subjects chewed the gum and at 20 minutes after expectoration of the gum. All saliva samples were serially diluted, plated on blood agar or agar plates that select for bacteria producing H2S, incubated anaerobically for three days, and enumerated for viable colony counts of total and H2S-producing salivary anaerobes.


Significant reductions in total salivary anaerobes (p < 0.01) and H2S-producing salivary anaerobes (p < 0.01) were observed 20 minutes after subjects chewed the CinA+ gum. The chewing of CinA- gum also significantly reduced total salivary anaerobes (p < 0.05) and H2S-producing salivary anaerobes (p < 0.05). However, no statistically significant difference in germ-killing effect was detected between the CinA+ and CinA- gums, although there was a numeric difference. The chewing of a gum base (GB) alone did not result in a significant reduction in the total or H2S-producing salivary anaerobes (p > 0.05).


The commercially available sugar-sweetened cinnamon chewing gum may benefit halitosis by reducing volatile sulfur compounds producing anaerobes in the oral cavity.



Diabet Med. 2010 Oct;27(10):1159-67. doi: 10.1111/j.1464-5491.2010.03079.x.

Glycated haemoglobin and blood pressure-lowering effect of cinnamon in multi-ethnic Type 2 diabetic patients in the UK: a randomized, placebo-controlled, double-blind clinical trial.

Akilen R, Tsiami A, Devendra D, Robinson N.


Faculty of Health and Human Science, Thames Valley University, London, UK. rakilen22@hotmail.com



To determine the blood glucose lowering effect of cinnamon on HbA1c, blood pressure and lipid profiles in people with type 2 diabetes.


58 type 2 diabetic patients (25 males and 33 females), aged 54.9 ± 9.8, treated only with hypoglycemic agents and with an HbA1c more than 7% were randomly assigned to receive either 2g of cinnamon or placebo daily for 12 weeks.


After intervention, the mean HbA1c was significantly decreased (P<0.005) in the cinnamon group (8.22% to 7.86%) compared with placebo group (8.55% to 8.68%). Mean systolic and diastolic blood pressures (SBP and DBP) were also significantly reduced (P<0.001) after 12 weeks in the cinnamon group (SBP: 132.6 to 129.2 mmHg and DBP: 85.2 to 80.2 mmHg) compared with the placebo group (SBP: 134.5 to 134.9 mmHg and DBP: 86.8 to 86.1 mmHg). A significant reduction in fasting plasma glucose (FPG), waist circumference and body mass index (BMI) was observed at week 12 compared to baseline in the cinnamon group, however, the changes were not significant when compared to placebo group. There were no significant differences in serum lipid profiles of total cholesterol, triglycerides, HDL and LDL cholesterols neither between nor within the groups.


Intake of 2g of cinnamon for 12 weeks significantly reduces the HbA1c, SBP and DBP among poorly controlled type 2 diabetes patients. Cinnamon supplementation could be considered as an additional dietary supplement option to regulate blood glucose and blood pressure levels along with conventional medications to treat type 2 diabetes mellitus.

© 2010 The Authors. Diabetic Medicine © 2010 Diabetes UK.



Biofactors. 2007;31(3-4):219-27.Click here to read Links

    Free radical scavenging activity, metal chelation and antioxidant power of some of the Indian spices.

    Yadav AS, Bhatnagar D.


    School of Biochemistry, Devi Ahilya University, Indore, Madhya Pradesh, India.


    Food constituents are the major source of various phytochemicals and micronutrients. The importance of these dietary constituents has been stressed in recent years due to their antioxidant and anticarcinogenic potential. Spices used in Indian foods such as cloves (Syzygium aromaticum), licorice (Glycyrrhiza glabra), mace (aril of Myristica fragans), and greater cardamom (Amomum subulatum) were tested for their antioxidant properties in vitro. The metal chelating activity, bleomycin dependent DNA oxidation, diphenyl-p-picryl hydrazyl (DPPH) radical scavenging activity and the ferric reducing /antioxidant power (FRAP) were measured in rat liver homogenate in presence of spices. Metal chelating activity was significantly high with all the spice extracts except mace. The spices due to higher reducing potential (in presence of bleomycin-FeCl_{3}) showed increased DNA oxidation. Cloves showed the highest DPPH radical scavenging activity, followed by licorice, mace and cardamom. FRAP values for cloves were also the highest, while other spices showed comparatively lesser FRAP values. The results show that the spices tested are strong antioxidants and may have beneficial effects on human health.



Biol Pharm Bull. 2007 Mar;30(3):423-7.Click here to read Links

    Eugenol [2-methoxy-4-(2-propenyl)phenol] prevents 6-hydroxydopamine-induced dopamine depression and lipid peroxidation inductivity in mouse striatum.

    Kabuto H, Tada M, Kohno M.


    Kagawa Prefectural College of Health Sciences, 281-1 Mure-cho, Takamatsu 761-0123, Japan. kabuto@chs.pref.kagawa.jp


    As superoxide (.O2-) and hydroxyl radical (.OH) have been implicated in the pathogenesis of Parkinson disease, free radical scavenging and antioxidants have attracted attention as way to prevent progression of this disease. We examined the effects of eugenol, an essential oil extracted from cloves, on 6-hydroxydopamine (6-OHDA)-induced dopamine (DA) reduction in the mouse striatum. Eugenol administration 3 d before and 7 more days following one intracerebroventricular 6-OHDA injection prevented the reduction of striatal DA and its metabolites. Eugenol administration for 3 d reduced the increase of thiobarbituric acid-reactive substances (an indicator of lipid peroxidation) induced by ferric ion and increased glutathione (GSH) and L-ascorbate (Asc) in the striatum. Eugenol did not change the levels of catalase, glutathione peroxidase, or superoxide dismutase-like activities. Eugenol is known to have .O2- and .OH scavenging activities in vitro. These results suggest that eugenol prevents 6-OHDA-induced DA depression by preventing lipid peroxidation directly and indirectly (via stimulation of GSH and Asc generating systems). Furthermore, increased GSH may protect cell death by conjugating with p-quinone produced in 6-OHDA auto-oxidation. The effects of eugenol treatment in this model suggest its possible usefulness for the treatment of Parkinson disease.