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The Anti-inflammatory and Other Physiological Modulating Effects of Naturally Occurring Xanthones
by Alfred Garbutt, D.C., D.A.C.R.B., D.A.B.C.N., D.A.A.P.M., D.A.B.D.A., F.A.C.C.R.S.

Context:
Since aging, diabetes mellitus, cancers, cardiovascular diseases, autoimmune disorders, asthma, COPD, post-operative states and so many other disorders have inflammation as a significant complication or as their cause then as health care providers, the safe control of inflammation should be one of our primary endeavors. NSAIDs are not a safe means for long-term control of inflammation, therefore, the mangosteen whole fruit and its xanthones with virtually no side effects should be seriously considered as a therapeutic modality.

Evidence Acquisition:
Reference data was gathered from the U.S. National Library of Medicine and National Institutes of Health databases at pubmed.com and from the book “The Xanthone Effect” by David A. Morton, Ph.D., Phytoceutical Research, LLC.

Results:
Xanthones are a group of biologically active chemicals that predominately naturally occur in the fruit of the Garcinia mangostana plant, commonly referred to as mangosteen. A German scientist by the name of Schmidt in 1855 isolated the first of this group of chemicals and created the word xanthone, which comes from xanthos, the Greek word for yellow.

Western medicine and alternative health care has not until recent times even heard of xanthones or mangosteen
due to the plant being so restricted in its growth to the tropics, especially the Southeast Asian region.
If you go to http://pubmed.com you will find over 1,500 xanthone related abstract references, at least 73 found under mangosteen and 65 under Garcinia mangostana.

There has been at least 46 xanthones isolated in the mangosteen fruit, primarily in the pericarp (rind). These xanthones have the same structural skeleton made up of two benzene rings joined by a carbonyl and an oxygen molecule. This configuration along with the type and position of attached chemical groups will give each type of xanthone its unique properties. This is why xanthones can be involved in such a variety of different physiological activities. Research from around the world has and is showing that xanthones have anti-inflammatory, antihistamine, anti-oxidant, immune modulating, anti-microbial and tumor shrinking properties.

Research by a group of scientists in India showed that mangostin, a major xanthone, was “active in suppressing acute as well as chronic inflammation.” Gopalakrishnan C, et al. Effect of mangostin, a xanthone from Garcinia mangostana Linn in immunopathological & inflammatory reactions. Indian J Exp Biol. 1980; 18(8):843-846.

Japanese researchers found that “gamma-mangostin… reduces prostaglandin generation through its direct inhibition of COX (cylooxygenase).” This research was indirectly demonstrating that gamma-mangostin prevents COX-2 gene transcription and it “is one of the candidates of the drugs for treatment of brain diseases accompanied with inflammation.” These researchers further stated that “ gamma-mangostin serves not only as a new attractive pharmacological tool for studying the molecular mechanism underlying inflammation but also as a new lead compound for drug development for the prevention and/or treatment of inflammation and brain diseases.”
Nakatani K, et al. Inhibition of cyclooxygenase and prostaglandin E2 synthesis by gamma-mangostin, a xanthone derivation in mangosteen, in C6 rat glioma cells. Biochem Pharmacol. 2002; 2002;63(1):1137-1141.


“has an anti-allergy/anti-inflammatory activity due to inhibitions of histamine release and prostaglandin E2 synthesis.”
Nakatani K, et al. Inhibitions of histamine release and prostaglandin E2 synthesis by mangosteen, a Thai medicinal Plant. Biol Pharm Bull. 2002; 25(9):1137-1141.

“mangosteen extract may be a useful crude drug for treatment of allergy and/or inflammation.”
Chairungsrilerd N, et al. Histaminergic and serotonergic receptor blocking substance from the medicinal plant Garcinia mangostana. Planta Med. 1996; 62(5): 471-472.


“In conclusion, alpha- and gamma-mangostins from G. mangostana are bioactive substances with anti-inflammatory effects.” Chen LG, et al. Anti-inflammatory activity of mangostins from Garcinia mangostana. Food Chem Toxicol.2008 Feb; 46(2): 688-93. Epub 2007 Sep 26.

“The above results indicate the cardioprotective effect of mangiferin against ISPH (isoproterenol)-induced myocardial infarction in rats.” Prabhu, et al. Department of Biochemistry, University of Madras, Guindy Campus Chennai 600 025, India.

“The present study was designed to evaluate the effect of alpha-mangostin on the antioxidant defense system and lipid peroxidation against isoproterenol-induced myocardial infarction in rats.”
and
“These findings indicate the protective effect of alpha-mangostin on lipid peroxidation and antioxidant tissue defense system during ISO (isoproterenol)-induced myocardial infarction in rats.”

Devi Sampath, et al. Cardioprotective effect of alpha-mangostin, a xanthone derivative from mangosteen on tissue defense system against isoproterenol-induced myocardial infarction in rats. Centre for Advanced Studies in Botany, University of Madras, Guindy Campus, Chennai, India.

“gamma-mangostin (6) exhibited hydroxyl radical-scavenging activity”
Chin et al. Xanthones with quinone reductase-inducing activity from the fruits of Garcinia mangostana (Mangosteen).
Phytochemistry. 2008 Feb;69(3):754-8. Epub 2007 Nov 7.
“These results suggest that alpha-mangostin is a novel competitive histamine H1 receptor antagonist in smooth muscle cells.” Chairunqsrilerd, et al. Pharmacological properties of alpha-mangostin, a novel histamine H1 receptor antagonist. Eur J Pharmacol.1996 Oct 31; 314(3): 351-6.
“MF (Mangiferin) lowered the blood glucose level of KK-Ay mice 3 weeks after oral administration (p < 0.01). However, no effect on the blood glucose level in normal mice was seen, indicating that MF could be useful in treating type-2 diabetes. In addition, MF improved hyperinsulinemia and, on insulin tolerance test, reduced blood glucose levels of KK-Ay mice. From these findings, it seems likely that MF exerts its antidiabetic activity by decreasing insulin resistance.”
Miura, et al. Phytomedicine.2001 Mar;8(2): 85-7. Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan

“MF (30 mg/kg) reduced the blood cholesterol (p<0.05) and triglyceride level (p<0.01) of KK-Ay mice with exercise 2 weeks after oral administration when compared with the control group.” Muira, et al. The suppressive effect of mangiferin with exercise on blood lipids in type 2 diabetes. Biol Pharm Bull. 2001 Sep; 24(9): 1091-2.

“our data indicated that Garcinia mangostana (mangostin) had a strong inhibitory effect on Propionibacterium acnes and Staphylococcus epidermidis.” Chomnawang J. Antimicrobial effects of Thai medicinal plants against acne-inducing bacteria. Ethnopharmacol. 2005 Oct 3; 101(1-3): 330-3.

A mouthwash with the rind of the mangosteen reduced levels of oral volatile sulfur compounds. Rassameemasmaung S. Effects of herbal mouthwash containing the pericarp extract of Garcinia mangostana L on halitosis, plaque and papillary bleeding index. J Int Acad Peridontol. 2007 Jan; 9(1): 19-25.

“The isolated proanthocyanidins are potent peroxyl radical scavengers as evidenced by the high oxygen radical scavenging capacity at 1.7 x 10 (4) micromol TE/g, much higher than that of pine bark and grape seed extracts.”
Fu C, et al. Oligomeric proanthocyanidins from mangosteen pericarps. J Agric Food Chem. 2007 Sep 19; 55(19): 7689-94. Epub 2007 Aug 23.


Conclusion:
Inflammation in its initial stage is important for initiating various healing processes, however, reoccurring or persistent inflammation can have very deleterious effects and should be minimized.

Based upon the quantity of fundamental peer reviewed published data and reports of clinical application of the mangosteen with its variety of xanthones and other anti-oxidants, the whole fruit mangosteen should be considered as a relatively safe and prime alternative to help reduce and/or prevent excess inflammation in our patient population.

 

Copyright © 2002 Alfred W. Garbutt, III, D.C., Inc.