@article {1904, title = {In Silico Analysis and ADMET Prediction of Flavonoid Compounds from Syzigium cumini var. album on α-Glucosidase Receptor for Searching Anti-Diabetic Drug Candidates}, journal = {Pharmacognosy Journal}, volume = {14}, year = {2022}, month = {December 2022}, pages = {736-743}, type = {Original Article}, chapter = {736}, abstract = {

Background: One of the causes of death is diabetes. Anti-diabetic drugs currently available do not work optimally because some have been reported to have side effect and resistance. Objective: This study aimed to flavonoid compounds from Syzygium cumini var. album with the greatest anti-diabetic activity and lower toxicity than acarbose. Materials and Methods: This research is an in silico study of nine flavonoid compounds from Syzygium cumini var. album, starting with PASS online was used to predict the activity spectrum of substances, drug-likeness prediction using DruLiTo, ADMET prediction (absorption, distribution, metabolism, excretion, and toxicity) using pkCSM online. Molecular docking was carried out by the AutoDock 4.2.6 program on α-glucosidase targeting. Visualization is done with the Discovery Studio Visualizer software. Results: From the data obtained, D-(+)-Catechin has a high affinity for α-glucosidase with a free energy of binding (ΔG) -5.94 kcal/mol and an inhibition constant (Ki) of 44270 nm. Conclusion: Based on the results of the study, it can be concluded that the flavonoid compounds from Syzygium cumini var. album has the potential as a promising anti-diabetic drug candidate, where the best candidate is D- (+)-Catechin. However, further studies of flavonoid compounds from Syzygium cumini var. album are needed.

}, keywords = {Flavonoid., Molecular docking, PASS, Pharmacokinetics, α-glucosidase}, doi = {10.5530/pj.2022.14.161}, author = {Yanu Andhiarto and Suciati and Ersanda Nurma Praditapuspa and Sukardiman} } @article {962, title = {A New LC/MS/MS Method for the Analysis of Phyllanthin in Rat Plasma and its Application on Comparative Bioavailability of Phyllanthin in Different Formulations after Oral Administration in Rats}, journal = {Pharmacognosy Journal}, volume = {11}, year = {2019}, month = {September 2019}, pages = {968-975}, type = {Original Article}, chapter = {968}, abstract = {

Introduction: A simple, short UPLC/MS/MS method for quantitation of phyllanthin in rat plasma in less than 2 minutes have been developed and fully validated. The validated method was used to investigate the pharmacokinetic properties of phyllanthin in PA extract and phospholipid complex of PA extract in rat. Methods: The separation was carried out on Acquity C18 (50 x 2.1 mm; 1.7 μm), with a mobile phase of 10 mM aqueous amonium acetate and acetonitrile (10:90; v/v), at a flow rate of 0.2 mL/min. Felodipin was used as internal standard. Phyllanthin is extracted from a small volume of rat plasma (100 μl) by means of liquid-liquid extraction method with tert butyl methyl ether. Electrospray ionization (ESI) mass spectrometry was applied in positive mode at capillary voltage of 4000 V for both phyllanthin and IS, cone voltage of 24 V for phyllanthin and 20 V for IS, desolvation temperature of 360oC, cone gas flow of 25 L/h, collision energy of 12 V for phyllanthin and 10 V for IS. Multiple reaction monitoring (MRM) was used to monitor the transitions at m/z (Q1/Q3) 436.41/355.36 for phyllanthin and 384.20/352.18 for IS. Results: The linear calibration curve of phyllanthin was obtained over the concentration range of 0.5 {\textendash} 100 ng/mL. The intra- and inter-day precisions were less than 7.08 \% and the accuracies were within {\textpm} 7.55\%. The Cmax values of phyllanthin from two different preparations in rat plasma after oral administration of 2.0 mg/kg were 11.44 and 31.44 ng/ml, and the AUC values were 18.07 and 41.43 h.ng/ml, respectively. Conclusion: A simple, short UPLC/MS/MS method for quantitation of phyllanthin in rat plasma in less than 2 minutes have been developed and fully validated. The bioavailability of phyllanthin from the phospholipid complex of PA extract in rat plasma was significantly improved compared with that of raw PA extract after oral administration.

}, keywords = {LC-MS/MS, Pharmacokinetics, Phospholipid, Phyllanthin, Plasma, Quantitation}, doi = {10.5530/pj.2019.11.153}, author = {Nguyen Van Long and Chu Van Men and Anh Vu Tuan and Nguyen Van Manh and Thanh Chu Duc and Ha Bui Thi Thu and Hoang Van Luong and Le Bach Quang and Pham Gia Khanh} } @article {1551, title = {Pharmacokinetic study of phyllanthin and hypophyllanthin after oral administration to rats}, journal = {Pharmacognosy Journal}, volume = {6}, year = {2014}, month = {18th Feb,2014}, pages = {124-130}, type = {Original Article}, chapter = {124}, abstract = {

Objective: The present study was carried out to develop a sensitive and cost effective HPLC method for the determination of bioactive lignans (phyllanthin and hypophyllanthin) and its application in a pharmacokinetic study. Methods: Identification of lignan compounds on C\–18 column was monitored at a range of 199\–400nm using photodiode array detector (PDA) with methanol-water (66:34, v/v) as mobile phase at a flow rate of 1ml/min. Carbamazepine was used as internal standard. Results: From the developed method LOD and LOQ values were found to be 56.14ng/ml and 169.99ng/ml for phyllanthin, and 56.04ng/ml and 169.82ng/ml for hypophyllanthin. The validated RP\–HPLC method herein was applied for pharmacokinetic studies and Cmax (ng/ml) values for administered three oral doses (2.5, 5 and 10mg/kg) of phyllanthin and hypophyllanthin were 0.28\±0.06, 0.53\±0.16, 0.98\±0.22 and 0.68\±0.76, 1.35\±0.23, 2.45\±0.33, respectively. Conclusion: In conclusion, developed HPLC\–PDA method effectively determined the phyllanthin and hypophyllanthin in various solvent and plasma samples. This method was successfully applied in conducting their oral pharmacokinetic studies.

Key words:Phyllanthus amarus, phyllanthin, hypophyllanthin, HPLC{\textendash}PDA, pharmacokinetics.

}, keywords = {HPLC{\textendash}PDA, hypophyllanthin, Pharmacokinetics, Phyllanthin, Phyllanthus amarus}, author = {Madhukiran Parvathaneni, and Ganga Rao Battu, and Ravikumar Jangiti, and Keerthana Diyya} }