Xanthone Research

Xanthone Research Studies

Directly below, you’ll see a long list of diseases and conditions. The numerals next to each one relate to a published report on  xanthone research:

1. by the scientific team noted
2. at what research center / university &
3. when the tests were performed,  dating from 1993 to the present day

• Allergies 9, 13 & 23
• Artery Blockage 28
• Atherosclerosis (hardening of the arteries) 3
• Blood Pressure 12 & 22
• Breast Cancer  25 & 29
• Cancer 1, 5, 16, 30
• Cardiovascular Disease 8, 12, 18 & 28
• Cholesterol 19
• Depression 2
• Diabetes 20
• Epilepsy 15
• Epstein Barr 17
• HIV 6, 14
• Inflammation 4, 9, 13
• Intra-cellular bacteria
• Leukemia 27
• Liver Cancer 24
• Lung Cancer 24
• Malaria 10
• Melanoma 25
• Renal cancer 25
• Staph bacteria 7
• Stroke Prevention 8, 18
• Tuberculosis 26
• Tumors 16

30    Cancer

Alpha-mangostin induces Ca(2+)-ATPase-dependent apoptosis via mitochondrial pathway in PC12 cells.

J Pharmacol Sci. 2004 May;95(1):33-40. Sato A, Fujiwara H, Oku H, Ishiguro K, Ohizumi Y. Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.

The researchers investigated the cell death effects of eight xanthones on pheochromocytoma (cancer) cells. Among these compounds, alpha-mangostin, from the fruit hull of Garcinia mangostana L. (mangosteen fruit), had the most potent effect with apoptosis (death) of these cells.

29    Breast Cancer

Antiproliferation, antioxidation and induction of apoptosis by Garcinia mangostana (mangosteen) on SKBR3 human breast cancer cell line. J Ethnopharmacol.

2004 Jan;90(1):161-6. Moongkarndi P, Kosem N, Kaslungka S, Luanratana O, Pongpan N, Neungton N.Department of Microbiology, Faculty of Pharmacy, Mahidol University, Sri Ayudthaya Road, Rajdhevee, Bangkok 10400, Thailand.

These investigators found that an extract from the pericarp of the mangosteen fruit inhibited the growth of breast cancer cells. They also showed that the extract had potent antioxidant and cancer cell death properties. They concluded that the extract from the pericarp of the mangosteen fruit has potential for chemoprevention.

28    Artery Blockage & Cardiovascular Disease

Relationship between protective effect of xanthone on endothelial cells and endogenous nitric oxide synthase inhibitors.

Bioorg Med Chem. 2003 Nov 17;11(23):5171-7. Jiang DJ, Hu GY, Jiang JL, Xiang HL, Deng HW, Li YJ.
Department of Pharmacology, School of Pharmaceutical Sciences, Central South University, Changsha 410078, China.

The researchers found that xanthone preserved endothelial cells inhibited the increased adhesion of monocytes to endothelial cells induced by oxidized LDL. This is especially important in preventing plaque formation and the subsequent blockage of arteries and cardiovascular disease.

27    Leukemia

Induction of apoptosis by xanthones from mangosteen in human leukemia cell lines.

August 2003 Matsumoto K, Akao Y, Kobayashi E, Ohguchi K, Ito T, Tanaka T, Iinuma M, Nozawa Y. Gifu International Institute of Biotechnology, 1-1 Naka-Fudogaoka, Kakamigahara, Gifu 504-0838, Japan.

These authors examined the effects of six xanthones extracted from the pericarps of the mangosteen fruit, Garcinia mangostana, on the cell growth inhibition of human leukemia cell line HL60. All xanthones displayed growth inhibitory effects. Among them, alpha-mangostin (a xanthone) showed the most potent ability to cause the cancer cells death.

26    Tuberculosis

Antimycobacterial activity of prenylated xanthones from the fruits of Garcinia mangostana.

Chem Pharm Bull (Tokyo). 2003 Jul;51(7):857-9. Suksamrarn S, Suwannapoch N, Phakhodee W, Thanuhiranlert J, Ratananukul P, Chimnoi N, Suksamrarn A. Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok, Thailand.

Xanthones, isolated from the fruit hulls and the edible arils and seeds of Garcinia mangostana, mangosteen fruit, were tested for their anti- tuberculosis potential. The investigators found alpha & beta mangostins and garcinone B exhibited strong inhibitory effect against Mycobacterium Tuberculosis (TB).

25    Breast, Renal & Melanoma Cancer

Xanthones as inhibitors of growth of human cancer cell lines and their effects on the proliferation of human lymphocytes in vitro.

Bioorg Med Chem. 2002 Dec;10(12):3725-30. Pedro M, Cerqueira F, Sousa ME, Nascimento MS, Pinto M. Centro de Estudos de Quimica Organica, Fitoquimica e Farmacologia da Universidade do Porto, Faculdade de Farmacia, Porto, Portugal.

Twenty-seven xanthones were assessed for their capacity to inhibit in vitro the growth of three human cancer cell lines:

• breast cancer
• renal cancer
• melanoma

Inhibition of growth of these cancer cell lines depended on the type of xanthone used in the study.

24    Liver & Lung Cancer

Garcinone E, a xanthone derivative, has potent cytotoxic effect against the patocellular carcinoma cell lines.

Planta Med. 2002 Nov;68(11):975-9. Ho CK, Huang YL, Chen CC. Department of Medical Research & Education, Veterans General Hospital,Taipei, ROC.

Treatment of hepatocellular carcinomas liver cancer with chemotherapy has generally been disappointing and it is most desirable to have more effective new drugs. The investigators extracted and purified 6 xanthone compounds from the rinds (peel) of the fruit of Garcinia mangostana, mangosteen fruit. The investigators tested this extract on 14 different human liver cancer cell lines. Several chemotherapeutic agents (drugs) were included in the study for comparison.

The results showed that one of the xanthone derivatives which could be identified as garcinone E has potent cytotoxic effect (kill cells) on all liver cancer cell lines as well as on the other gastric and lung cancer cell lines included in the screen. The investigators suggested that garcinone E may be potentially useful for the treatment of certain types of cancer.

23    Allergies

Inhibitions of histamine release and prostaglandin E2 synthesis by mangosteen, a Thai medicinal plant.

Biol Pharm Bull. 2002 Sept;25(9):1137-41. Nakatani K, Atsumi M, Arakawa T, Oosawa K, Shimura S, Nakahata N, Ohizumi Y. Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.

The fruit hull of mangosteen, Garcinia mangostana L., mangosteen fruit, has been used as a Thai indigenous medicine for many years. However, its mechanism of action as a medicine has not been elucidated. The present study was undertaken to examine the effects of mangosteen fruit extracts on histamine release and prostaglandin E2 synthesis.

The investigators found the mangosteen fruit extract strongly inhibited histamine release and prostaglandin E2 synthesis. This has great importance in preventing allergies.

22    Reduce Blood Pressure

Antihypertensive and vasorelaxing activities of synthetic xanthone derivatives.

Bioorg Med Chem. 2002 Mar;10(3):567-72. Wang LW, Kang JJ, Chen IJ, Teng CM, Lin CN. School of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan 807, ROC.

The researchers studied a series of xanthones and related compounds. The antihypertensive (against high blood pressure) and vasorelaxing (relaxing of the blood vessels to prevent high blood pressure) activity of compounds on cardiovascular system was evaluated. All the compounds tested exhibited effective hypotensive (lower blood pressure) activity in anesthetized rats.

21

Hmm…this one’s a bit beyond us…but googling:

• cyclooxygenase &
• prostaglandin

seems to indicate that the Xanthone can provide relief from Inflammation & Pain.

Inhibition of cyclooxygenase and prostaglandin E2 synthesis by gamma-mangostin, a xanthone derivative in mangosteen, in C6 rat glioma cells. Biochem Pharmacol.2002 Jan 1;63(1):73-9. Nakatani K, Nakahata N, Arakawa T,Yasuda H, Ohizumi Y. Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Aramaki, Aoba-ku, 980-8578, Sendai, Japan.

The fruit hull of mangosteen fruit, Garcinia mangostana L., has been used for many years as a medicine for treatment of skin infection, wounds, and diarrhea in Southeast Asia. In the present study, the investigators studied the effect of gamma-mangostin, a xanthone contained in the mangosteen fruit, and showed it had a potent inhibitory activity of prostaglandin E2 (PGE2) release.

20     Diabetes

Antidiabetic activity of a xanthone compound, mangiferin.

Phytomedicine. 2001 Mar;8(2):85-7. Miura T, Ichiki H, Hashimoto I, Iwamoto N, Kato M, Kubo M, Ishihara E, Komatsu Y, Okada M, Ishida T, Tanigawa K. Suzuka University of Medical Science, Mie, Japan.

Mangiferin, a xanthone, lowered the blood glucose (sugar) level  in diabetic type II mice. From these findings, it seems likely that mangiferin exerts its antidiabetic activity by decreasing insulin resistance.

19     LDL Cholesterol

Inhibition of lipoprotein oxidation by prenylated xanthones derived from mangostin. Free Radic Res. 2000 Nov;33(5):643-59. Mahabusarakam W, Proudfoot J, Taylor W, Croft K. Chemistry Department, Prince of Songkla
University, Hat Yai, Thailand.

Oxidative damage is thought to play a critical role in cardiovascular and other chronic diseases. This has led to considerable interest in the antioxidant activity of dietary compounds. The researchers have previously shown that the xanthone, mangostin (found in mangosteen fruit), can inhibit the oxidation of LDL, low density lipoprotein (bad cholesterol).

Researchers studied more xanthone derived compounds and found enhanced antioxidant activities.

Note: If the oxidation of LDL cholesterol can be prevented or inhibited, then the LDL-cholesterol cannot exert its “bad” effect and cause heart disease.

18    Cardiovascular Disease & Stroke Prevention

Antiplatelets activity of some xanthone derivatives.

Acta Pol Pharm. 1999 Jul-Aug;56(4):319-24. Rajtar G, Zolkowska D, Kleinrok Z, Marona H. Department of Pharmacology and Toxicology, Medical University School, Lublin, Poland.

Researchers studied the effects of 12 xanthone derived compounds on platelet aggregation. They found five of them inhibited thrombin-induced platelet aggregation (clot formation).

17    Epstein Barr

Chiral 2-amino-1-butanol xanthone derivatives as potential antiarrhythmic and hypotensive agents.

Acta Pol Pharm. 1999 Jan-Feb;56(1):87-90. Librowski T, Czarnecki R, Jastrzebska M. Department of Pharmacodynamics, Collegium Medicum Jagiellonian University, Krakow, Poland.

Xanthones as inhibitors of Epstein-Barr virus activation.

16    Cancer

Cancer Lett. 1998 Oct 23;132(1-2):113-7 Ito C, Itoigawa M, Furukawa H, Rao KS, Enjo F, Bu P, Takayasu J, Tokuda H, Nishino H. Faculty of Pharmacy, Meijo University, Nagoya, Japan.

Researchers screened 20 xanthones and found that 3 of them to have valuable anti-tumor (against cancer) activities.

15    Epilepsy

Synthesis and anticonvulsant effects of some aminoalkanolic derivatives of xanthones.

Pharmazie. 1998 Oct 53(10):672-6. Marona H. Department of Chemical Technology of Drugs, Collegium Medicum, Jagiellonian University, Krakow, Poland.

Researchers studied compounds derived from xanthone for anticonvulsant activities. They found several xanthone derived compounds to be active in anticonvulsant tests.

14    HIV

Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection.

Planta Med. 1998 Mar;64(2):97-109. Vlietinck AJ, De Bruyne T, Apers S, Pieters LA. Department of Pharmaceutical Sciences, University of Antwerp (UA), Belgium.

The investigators showed many compounds of plant origin have been identified that inhibit different stages in the replication cycle of human immunodeficiency virus HIV. Among these compounds, the xanthone mangostin, derived from mangosteen fruit, was shown to inhibit the replication cycle of HIV.

13    Allergies & Inflammation

Novel types of receptor antagonists from the medicinal plant Garcinia mangostana.

Nippon Yakurigaku Zasshi. 1997 Oct;110 Suppl 1:153P-158P. Furukawa K, Chairungsrilerd N, Ohta T, Nozoe S, Ohizumi Y. Department of Pharmaceutical MolecularBiology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.

Here the researchers used a crude extract of the fruit hull of Garcinia mangostana L, mangosteen fruit. On the basis of physicochemical data, the active substances were identified as alpha-mangostin and gamma-mangostin in the crude extract. The researchers found that alpha-Mangostin and gamma-mangostin may become novel types of lead compounds for histamine and serotonin receptor antagonists (fight allergies and inflammation).

12    Cardiovascular Disease & The Blood

Mechanism of vasorelaxation of thoracic aorta caused by xanthones.

Eur J Pharmacol. 1997 Oct 1;336(1):23-8. Cheng YW, Kang JJ. Institute of Toxicology, College of Medicine, National Taiwan University, Taipei.

The researchers showed vasorelaxation (relaxing of the tension of blood vessel walls) activity of the xanthones studied.

11

Kills intra-cellular bacteria…such as the STD Chlamydia, we believe.

Immunopharmacological activity of polysaccharide from the pericarp of mangosteen garcinia: phagocytic intracellular killing activities.

J Med Assoc Thai. 1997 Sep;80 Suppl 1:S149-54. Chanarat P, Chanarat N, Fujihara M, Nagumo T. Department of Clinical Microscopy, Faculty of Associated Medical Sciences, Chiang Mai University, Thailand.

Polysaccharides from the pericarps of mangosteen, Garcinia mangostana Linn., mangosteen fruit, were extracted from the dried ground pericarps of the mangosteen fruit. The results showed that the number of S. enteritidis (bacteria) in cultured monocyte with extract of the pericarp of the mangosteen fruit was killed. This paper showed that polysaccharides in the extract can stimulate phagocytic cells to kill intracellular bacteria (S. enteritidis).

10    Malaria

Xanthones as antimalarial agents; studies of a possible mode of action.

FEBS Lett. 1997 Jun 2;409(1):67-73. Ignatushchenko MV, Winter RW, Bachinger HP, Hinrichs DJ, Riscoe MK. Department of Biochemistry and Molecular Biology, Oregon Health Sciences University, Portland 97201, USA.

Researchers showed potent antimalarial activities for the xanthones studied.

9    Allergies & Inflammation

Histaminergic and serotonergic receptor blocking substances from the medicinal plant Garcinia mangostana.

Planta Med. 1996 Oct;62(5):471-2. Chairungsrilerd N, Furukawa K, Ohta T, Nozoe S, Ohizumi Y. Japan.

The investigators studied an extract of the fruit hull of Mangosteen, Garcinia mangostana L., mangosteen fruit. On the basis of pharmacological data, they determined that alpha-mangostin and gamma-mangostin (xanthones in mangostana) are a histaminergic and a serotonergic receptor blocking agent, respectively. That is, they have the ability to prevent allergies and inflammation.

8    Cardiovascular Disease & Stroke Prevention

Synthesis and antithrombotic effect of xanthone derivatives.

J Pharm Pharmacol. 1996 Sep;48(9):887-90. Lin CN, Hsieh HK, Liou SJ, Ko HH, Lin HC, Chung MI, Ko FN, Liu HW, Teng CM. School of Pharmacy, Department of Internal Medicine, Kaohsiung Medical College, Taiwan, R.O.C.

Researchers studied several xanthone-derived compounds and found them to possess potent antithrombotic (anti-clotting) activities.

7    Staph Bacteria:

skin infections, boils etc.

Antibacterial activity of xanthones from guttiferaeous plants against methicillin-resistant Staphylococcus aureus.

J Pharm Pharmacol. 1996 Aug;48(8):861-5. Iinuma M, Tosa H, Tanaka T, Asai F, Kobayashi Y, Shimano R, Miyauchi K. Department of Pharmacognosy, Gifu Pharmaceutical University, Japan.

The investigators showed that extracts of Garcinia mangostana, mangosteen fruit, possessed inhibitory effects against the growth of S. aureus (staph bacteria). The strong in-vitro antibacterial activity of xanthone derivatives against both methicillin-resistant and methicillin sensitive Staphylococcus aureus suggests the compounds might find wide pharmaceutical use.

6    HIV

Active constituents against HIV-1 protease from Garcinia mangostana.

Planta Med. 1996 Aug;62(4):381-2. Chen SX, Wan M, Loh BN.

The investigators found that an extract of Garcinia mangostana L., mangosteen fruit, showed potent inhibitory activity against HIV-1 protease which affects the replication of HIV.

5    Cancer

Xanthone derivatives as potential anti-cancer drugs.

J Pharm Pharmacol. 1996 May;48(5):539-44. Lin CN, Liou SJ, Lee TH, Chuang YC, Won SJ. School of Pharmacy, Kaohsiung Medical College, Taiwan, Republic of China.

Researchers showed xanthone-derived compounds to have potent anti-tumor activities against human cancer cells.

4    Inflammation

Synthesis and anti-inflammatory effects of xanthone derivatives.

J Pharm Pharmacol. 1996 May;48(5):532-8. Lin CN, Chung MI, Liou SJ, Lee TH, Wang JP. School of Pharmacy, Kaohsiung Medical College, Taiwan, R.O.C.

The researchers studied 18 xanthone derived compounds and found that some of these compounds possessed strong anti-inflammatory properties.

3     Atherosclerosis

(hardening of the arteries)

Mangostin inhibits the oxidative modification of human low density lipoprotein.

Free Radic Res. 1995 Aug;23(2):175-84. Williams P, Ongsakul M, Proudfoot J, Croft K, Beilin L. University of Western Australia, Department of Medicine, Royal Perth Hospital, Australia.

The oxidation of low density lipoprotein (LDL) may play an important role in atherosclerosis. The researchers investigated the possible antioxidant effects of mangostin, isolated from Garcinia mangostana (found in mangosteen fruit), on the oxidation of human LDL (bad cholesterol).

From these results, they concluded that mangostin is acting as a free radical scavenger (“mop up” sponge) to protect the LDL from oxidative damage in this in vitro system. In other words, it a potent antioxdiant.

2    Depression

Screening of unsubstituted cyclic compounds as inhibitors of monoamine oxidases.

Biochem Pharmacol. 1994 Jun 15 47(12):2307-10. Thull U, Testa B. Institut de Chimie Therapeutique, Ecole de Pharmacie, Universite de Lausanne,Switzerland.

Of several compounds studied, xanthones emerged as a potent monoamine oxidase inhibitor (a powerful anti-depressant).

1    Cancer

Gamma-pyrone compounds as potential anti-cancer drugs

J Pharm Pharmacol.1993 Sep;45(9):791-4. Liou SS, Shieh WL, Cheng TH, Won SJ, Lin CN. Natural Products Research Center, Kaohsiung Medical College, Taiwan, Republic of China

Researchers studied several compounds and found xanthones with enhanced anti-tumor activity against human cancer cells.