Quantitative estimation of (-)-hinokinin, a trypanosomicidal marker in Piper cubeba, and some of its commercial formulations using HPLC-PDA

AbstractThe fruits of Piper cubeba have been used in Ayurvedic system of medicine for pain, tastelessness, painful urination and mouth diseases. Among its various chemical constituents, (-)-hinokinin, a trypanosomicidal dibenzylbutyrolactone lignan, is found in significant quantities. For quality evaluation of P. cubeba fruit and its commercial formulations, there is an urgent need to develop an analytical method based on (-)-hinokinin. For this purpose, an HPLC method was developed using photo diode array detector and Waters HR C18 column with gradient elution consisting of water and acetonitrile. The developed method was validated as per ICH-Q2B guidelines and found to be accurate, precise and linear over a wide range of concentrations (5–300µg/mL). (-)-Hinokinin contents were found to be in the range of 0.005–0.109%(m/m) in various P. cubeba samples. The developed method was extended to LC–MS for further identification and characterization of (-)-hinokinin in samples. The developed method is simple, rapid and specific, and can be used as a tool for quality control of P. cubeba fruits and its commercial formulations

Synthesis of some novel orsellinates and lecanoric acid related depsides as <i>α</i>-glucosidase inhibitors

<p>Sixteen novel orsellinic esters (<b>6a-l, 7a-d</b>) along with four lecanoric acid related depsides (3<b>a-c, 4</b>) were synthesized and confirmed their structures by spectroscopic data (¹H, ¹³C & HRMS). The synthesized compounds were evaluated for their <i>in vitro α</i>-glucosidase (<i>Saccharomyces cerevisiae</i>) inhibitory potential. Among the tested compounds, <b>3c</b> (IC₅₀: 140.9 μM) and <b>6c</b> (IC₅₀: 203.9 μM) displayed potent α-glucosidase inhibitory activity and found more active than the standard drug acarbose (IC₅₀: 686.6 μM). Both the test compounds were subjected to <i>in vivo</i> antihyperglycemic activity using sucrose loaded model in Wistar rats and found compound <b>3c</b> exhibited significant reduction in glucose levels.</p