Abstract

Sinensetin, a plant-derived polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacological benefits and promising potency in intended activities with minimal toxicity. This review aims to compile an up-to-date reports of published scientific information on sinensetin pharmacological activities, mechanisms of action and toxicity. The present findings about the compound are critically analyzed and its prospect as a lead molecule for drug discovery is highlighted. The databases employed for data collection are mainly through Google Scholar, PubMed, Scopus and Science Direct. In-vitro and in-vivo studies showed that sinensetin possessed strong anticancer activities and a wide range of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, anti-obesity, anti-dementia and vasorelaxant activities. The studies provided some insights on its several mechanisms of action in cancer and other disease states. However, more detail mechanistic studies are needed to understand its pharmacological effects. More in vivo studies in various animal models including toxicity, pharmacokinetic, pharmacodynamic and bioavailability studies are required to assess its efficacy and safety before submission to clinical studies. In this review, an insight on sinensetin pharmacological activities and mechanisms of action serves as a useful resource for a more thorough and comprehensive understanding of sinensetin as a potential lead candidate for drug discovery.

Highlights

  • Sinensetin is a polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus [syn: Orthosiphon stamineus Benth., Orthosiphon spicatus (Thunb.) Backer, Bakh.f. & Steenis] (Lambiaceae) and in many citrus fruits

  • When 19 citrus cultivar were investigated for their antitrypanosomal activities to tackle African trypanosomiasis such as Trypanosoma brucei, T. brucei gambiense and T. brucei rhodesiense, “Setoka” extract exhibited the most potent inhibitory effect (36%) on T. brucei proliferation with highest activity in its ethyl acetate extract (Nakanishi et al, 2019)

  • Selectivity was calculated for all these compounds based on IC50 values against T. brucei and 293T human embryonic kidney cells

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Summary

INTRODUCTION

Sinensetin is a polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus [syn: Orthosiphon stamineus Benth., Orthosiphon spicatus (Thunb.) Backer, Bakh.f. & Steenis] (Lambiaceae) and in many citrus fruits. Tezuka et al (2000) reported the isolation of 75 mg of sinensetin from 4 kg of plant material by subjecting its methanol extract to repeated column chromatography followed by preparative thin layer chromatography (TLC). Yuliana et al (2009) reported 3.03 mg of sinensetin was isolated from 500 g of O. aristatus using silica column, sephadex LH-20 column and preparative TLC. Another study reported that from 1 kg of O. aristatus, only 2.6 mg of the compound was isolated by repeated column chromatography followed by preparative TLC (Amzad Hossain and Mizanur Rahman, 2015). Out of 100 mg ethyl acetate extract of C. reticulata, 23.4 mg sinensetin was isolated by using sephadex LH-20 column chromatography and preparative TLC (Nakanishi et al, 2019).

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