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Research Project: Discovery and Development of Natural Products for Pharmaceutical and Agrochemical Applications II

Location: Natural Products Utilization Research

Title: Evaluation of drug interaction potential of Labisia pumila (Kacip Fatimah) and its constituents

Author
item MANDA, VAMISHI - University Of Mississippi
item DALE, OLIVIA - University Of Mississippi
item AWORTWE, CHARLES - University Of Stellenbosch
item ALI, ZULFIGAR - University Of Mississippi
item KHAN, IKHLAS - University Of Mississippi
item WALKER, LARRY - University Of Mississippi
item KHAN, SHABANA - University Of Mississippi

Submitted to: FRONTIERS IN PHARMACOLOGY
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 7/11/2014
Publication Date: 8/8/2014
Publication URL: http://handle.nal.usda.gov/10113/62474
Citation: Manda, V.K., Dale, O.R., Awortwe, C., Ali, Z., Khan, I.A., Walker, L.A., Khan, S.I. 2014. Evaluation of drug interaction potential of Labisia pumila (Kacip Fatimah) and its constituents. FRONTIERS IN PHARMACOLOGY. 5(178):1-13. https://doi.org/10.3389/fphar.2014.00178.
DOI: https://doi.org/10.3389/fphar.2014.00178

Interpretive Summary: Labisia pumila (Kacip Fatimah) is a popular herb in Malaysia that has been traditionally used to improve women’s health, and to facilitate or hasten delivery in childbirth. Recently it has been identified as one of the top five herbs used in Malaysia for treating variety of ailments. Also, it is sold commercially in the form of herbal tea, powder, capsules and tablets in many countries. Due to the increasing popularity and wide spread use of herbal supplements throughout the world; there is a potential risk of herb-drug interactions when these supplements are taken in combination with conventional drugs. The current study was aimed to study the potential of Kacip Fatimah to cause any drug interactions. Our results showed that Kacip Fatimah has the potential to cause drug interactions and further studies are needed to see if these interactions can occur in humans.

Technical Abstract: Labisia pumila (Kacip Fatimah) is a popular herb in Malaysia that has been traditionally used in a number of women's health applications such as to improve libido, relieve postmenopausal symptoms, and to facilitate or hasten delivery in childbirth. In addition, the constituents of this plant have been reported to possess anticancer, antioxidant, and anti-inflammatory properties. Clinical studies have indicated that cytochrome P450s (CYPs), P-glycoprotein (P-gp), and Pregnane X receptor (PXR) are the three main modulators of drug-drug interactions which alter the absorption, distribution, and metabolism of drugs. Given the widespread use of Kacip Fatimah in dietary supplements, the current study focuses on determining the potential of its constituents to affect the activities of CYPs, P-gp, or PXR using in vitro assays which may provide useful information toward the risk of herb-drug interaction with concomitantly used drugs. Six compounds isolated from the roots of L. pumila (2 saponins and 4 alkyl phenols) were tested, in addition to the methanolic extract. The extract of L. pumila showed a significant time dependent inhibition (TDI) of CYP3A4, reversible inhibition of CYP2C9 and 2C19 and a weak inhibition of 1A2 and 2D6 as well as an inhibition of P-gp and rifampicin-induced PXR activation. The alkyl phenols inhibited CYP3A4 (TDI), CYP2C9, and 2C19 (reversible) while saponins inhibited P-gp and PXR. In conclusion, L. pumila and its constituents showed significant modulation of all three regulatory proteins (CYPs, P-gp, and PXR) suggesting a potential to alter the pharmacokinetic and pharmacodynamic properties of conventional drugs if used concomitantly.