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    Human Cytochrome P450 Enzyme Modulation by Gymnema sylvestre : A Predictive Safety Evaluation by LC-MS/MS

    Bera Rammohan1, Karmakar Samit2, Das Chinmoy3, Saha Arup3, Kundu Amit3, Sarkar Ratul3, Karmakar Sanmoy3★, Adhikari Dipan3, Sen Tuhinadri3★ Corresponding author

    1. 1Division of Pharmacology, Dept.of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
    2. 2Dept. of Physiology, Bankura Sammilani Medical College & Hospital, Kenduadihi, Bankura, West Bengal, India.
    3. 3Department of Botany, Hooghly Mohsin College, Chinsurah, Hooghly, West Bengal, India.

    CORRESPONDENCE

    Karmakar Sanmoy

    Department of Botany, Hooghly Mohsin College, Chinsurah, Hooghly, West Bengal, India.

    sanmoykarmakar@gmail.com

    Received: 17-06-2015; Revised: 14-07-2015; Accepted: 30-09-2016.

    Volume 12, Issue 47s · pp. 389–394 · PUBLISHED 30 September 2016 · DOI: 10.4103/0973-1296.191441

    View on Pharmacogn. Mag. original site ↗

    ABSTRACT

    Background: Traditionally GS is used to treat diabetes mellitus. Drug-herb interaction of GS via cytochrome P450 enzyme system by substrate cocktail method using HLM has not been reported. Objective: To evaluate the in-vitro modulatory effects of GS extracts (aqueous, methanol, ethyl acetate, chloroform and n-hexane) and deacylgymnemic acid (DGA) on human CYP1A2, 2C8, 2C9, 2D6 and 3A4 activities in HLM. Material and Methods: Probe substrate-based LCMS/MS method was established for all CYPs. The metabolite formations were examined after incubation of probe substrates with HLM in the presence or absence of extracts and DGA. The inhibitory effects of GS extracts and DGA were characterized with kinetic parameters IC50 and Ki values. Results: GS extracts showed differential effect on CYP activities in the following order of inhibitory potency: ethyl acetate > Chloroform > methanol > n-hexane > aqueous > DGA. This differential effect was observed against CYP1A2, 2C9 and less on CYP3A4 and 2C8 but all CYPs were unaffected by aqueous extract and DGA. The ethyl acetate and chloroform extract exhibited moderate inhibition towards CYP1A2 and 3A4. The aqueous extract and DGA however showed negligible inhibition towards all five major human CYPs with very high IC50 values (>90µg/ml). Conclusion: The results of our study revealed that phytoconstituents contained in GS, particularly in ethyl acetate and chloroform extracts, were able to inhibit CYP1A2, 3A4 and 2C9. The presence of relatively small, lipophillic yet slightly polar compounds within the GS extracts may be attributed for inhibition activities. These suggest that the herb or its extracts should be examined for potential pharmacokinetic drug interactions in vivo.

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      Rammohan, B., Samit, K., Chinmoy, D., Arup, S., Amit, K., Ratul, S., Sanmoy, K., Dipan, A., & Tuhinadri, S. (2016). Human Cytochrome P450 Enzyme Modulation by Gymnema sylvestre : A Predictive Safety Evaluation by LC-MS/MS. Pharmacognosy Magazine, 12(47s), 389–394. https://doi.org/10.4103/0973-1296.191441