Natural Products as Alternative Choices for P-Glycoprotein (P-gp) Inhibition

The present review aims to recapitulate the research findings on bioactive constituents of natural origin with P-gp inhibition characteristics

Saikat Dewanjee; Tarun Dua; Niloy Bhattacharjee; Anup Das; Moumita Gangopadhyay; Ritu Khanra; Swarnalata Joardar; Muhammad Riaz; Vincenzo Feo; Muhammad Zia-Ul-Haq

2017

Scholarcy highlights

  • LivMionlegculeos r2g01a7,n2i2s, m871s through constant evolution have developed defense mechani2somf 1s07against persistent attacks from environmental toxins as it is necessary for them to avoid the pernicious effects 1o.fInthtreosdeucctyiotnotoxic compounds
  • Quercetin could competitively inhibit the members of Multidrug resistance family, P-gp, MRP1 and BCRP and the metabolizing enzyme, CYP3A4
  • Numerous research studies were carried out on MDR during the last three to four decades since Ling et al, discovered the role of an efflux transporter named P-gp in colchicine resistance in CHO cells. This efflux transporter was found to play a pivotal role in drug pharmacokinetics and eventually interest started to accrue encompassing this transporter
  • In the earlier sections of this article, we have emphasized that P-gp is highly expressed in various tissues, and it is apparent that P-gp inhibition has great effects on drug pharmacokinetics
  • Most of the plant-based chemicals mentioned in this review could provide a vivid insight into a wide range of possibilities of using different techniques to improvise and develop effective P-gp inhibitors
  • Some plant-based molecules are active against microbial efflux systems and some are active in both humans and microbes, so there may be a probability those molecules that are active against microbial efflux systems may affect the efflux system in cancer cells
  • Modern experimental methodologies and techniques, such as structure-activity relationships, quantitative structure-activity relationships, 3-dimensional structure-activity relationships, and pharmacophore studies should be taken into consideration and should be regarded as an important guiding tool for the modern researchers in discovering very selective and potent P-gp inhibitors

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