Purwantiningsih ., Abas Hj Hussin


Herbal remedies are often used concomitantly with prescribed medication, which leads to an increase in the potential of herb-drug interactions. Orthosiphon stamineus is one of the popular herbal preparations that is traditionally used, especially as a diuretic or for the elimination of kidney stones. The inhibitory effect of O. stamineus extract on human cytochrome P450 isoforms, namely CYP1A2, CYP3A4, CYP2C9 and CYP2D6, has been determined using luminescent methods. The final concentrations of O. stamineus extract tested were 0.01, 0.1, 1, 10, 100 and 1000µg/mL. IC50 value was used to assess the modulation potencies for each CYP isoform. The extract showed a moderate inhibition towards CYP2C9 with the IC50 of 20.12µg/mL and showed IC50 of 49.90, 89.24 and 97.82µg/mL for CYP1A2, CYP2D6 and CYP3A4, respectively. These data suggest that O. stamineus extract may potentiate the herb-drug interaction via CYP inhibition.

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Akowuah GA., Zhari, I., Norhayati I., Sadikun A., Khamsah SM. 2004. Sinensitin, eupatorin, 3’-hydroxy-5, 6, 7, 4’-tetramethoxyflavone and rosmarinic acid contents and antioxidative effect of Orthosiphon stamineus from Malaysia. Food Chem. 82: 559-566.

Barnes J., Mills SY., Abbot NC., Willoughby M., Ernst E.1998. Different standards for reporting ADRs to herbal remedies and conventional OTC medicines: face-to-face interviews with 515 users of herbal remedies. Br. J. Clin. Pharmacol. 45: 496-500.

Booven DV., Marsh S., McLeod H., Carrillo MW., Sangkuhl K., Klein TE., Altman RB. 2010. Cytochrome P450 2C9-CYP2C9. Pharmacogenet Genomics. 20(4): 277-281.

Bosetti A., Sobol M., Ma D., Good T., Liu D., Cali JJ. 2005. Bioluminescent ytochrome P450 assays. Pharmacology. 3: 9-18.

Chin JH., Hussin AH., Ismail S. 2009. Effect of Orthosiphon Stamineus Leaf Extracts On Hepatic Cytochrome P450, UGT And GST Activity In STZ-Induced Diabetic Rats. J.Adv. Scie.Arts. 1(1): 1-8.

Chin JH., Hussin AH. 2011. Orthosiphon Stamineus Increases metabolism of Aminopyrine in Female Rat Hepatocytes by Inhibiting Protein Kinase-A. Int. J. Pharm. Sci. Res. 2(7): 1777-1780.

Fugh-Berman A. 2000. Herb-drug interactions. Lancet. 355: 134-138.

Fugh-Berman A., Ernst E. 2001. Herb-drug interactions: review and assessment of report reliability. Br. J. Clin. Pharmacol. 52: 587-595.

Hanapi NA., Azizi J., Ismail S., Mansor SM. 2010. Evaluation of selected Malaysian medicinal plants on phase I drug metabolizing enzymes, CYP2C9, CYP2D6 and CYP3A4 activities in vitro. Int. J. Pharm. 6(4): 494-499.

Indubala J., Ng LT. 2000. Herbs: The Green Pharmacy of Malaysia 1st ed. Vinpress Sdn. Bhd., Kuala Lumpur, pp.76.

Ioannides C. 2002. Xenobiotic Metabolis: an Overview. In C. Ioannides (Ed.), Enzymes Systems The Metabolise Drugs and Other Xenobiotics. John Wiley & Sons, Ltd., West Sussex, pp. 1-30.

Ismail S., Hanapi NA., Halim MRA., Uchaipichat V., Mackenzie PI. 2010. Effects of Andrographis paniculata and Orthosiphon stamineus extracts on the glucuronidation of 4-methylumbelliferone in human UGT isoforms. Molecules. 15: 3578-3592.

Izzo AA., Ernst E. 2001. Interactions between herbal medicines and prescribed drugs: a systematic review. Drugs. 61(15): 2163-2175.

Izzo AA., Borrelli F., Capasso R. 2002. Herbal medicine: the dangers of drug interaction. Trends Pharmacol. Sci. 23: 358-359.

Markowitz JS, de Vane CL., Boulton DW., Carson SW., Nahaz Z., Risch SC. 2000. Effect of St. John’s wort (Hypericum perforatum) on cytochrome P-450 2D6 and 3A4 activity in healthy volunteers. Life Sci. 66: 33-39.

Ohnishi A., Matsuo H., Yamada S., Takanaga H., Morimoto S., Shoyama Y., Ohtani H., Sawada Y. 2000. Effect of furanocoumarin derivatives in grapefruit juice on the uptake of vinblastine by Caco-2 cells and on the activity of cytochrome P450 3A4. Br. J. Pharmacol. 130: 1369-1377.

Pietta P., Simonetti P., Mauri P. 1998. Anioxidant activity of selected medicinal plants. J. Agric. Food Chem. 46: 4487–4490.

Qiu F., Zhang R., Sun J., Jiye A., Hao H., Peng Y., Ai H., Wang G. 2008. Inhibitory Effects of Seven Components of Danshen Extract on Catalytic Activity of Cytochrome P450 Enzyme in Human Liver Microsomes. Drug Metab. Dispos. 36(7): 1308-1314.

Sumaryono, W., Proksc, P., Wray, V., Witte, L., and Hartmann, T. 1991. Qualitative and quantitative analysis of the phenolic constituents from Orthosiphon aristatus. Planta Med. 57: 176–180.

Tezuka Y., Stampoulis P., Banskota AJ., Awale S., Kadota S., Saiki I. 2000. Constituents of the Vietnamese medicinal plant Orthosiphon stamineus. Chem. Pharm. Bull. 48: 1711–1719.

Wang Z., Gorski JC., Hamman MA., Huang S-M., Lesko LJ., Hall SD. 2001. The effects of St John's wort (Hypericum perforatum) on human cytochrome 450 activity. Clin. Pharmacol. Ther. 70: 317-326

Wiart C. 2002. Orthosiphon stamineus, Benth. In: F. K. WONG (Ed.). Medicinal plants of Southeast Asia. Prentice Hall, Selangor, pp. 264.

Wilkinson GR. 1997. The effects of diet, aging and disease-states on presystemic elimination and oral drug bioavailability in humans. Adv. Drug Deliv. Rev. 27: 129-159.

Winitthana T., Niwattisaiwong N., Patarapanich C., Tantisira MH., Lawanprasert S. 2011. In vitro inhibitory effects of asiaticoside and madecassoside on human cytochrome P450. Toxicology in vitro. 25 (4): 890-896.

Zhou SF., Gao YH., Wen QJ., Huang M., Xu AL., Paxton JW. 2003. Interactions of herbs with cytochrome P450. Drug Metab. Rev. 35: 35-98.

Zhou S., Koh HL., Gao Y., Gong Z., Lee EJD. 2004. Herbal bioactivation: The good, the bad and the ugly. Life Sci. 74: 935-968.



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