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A chalcone-flavonone type biflavonoid, trichocladabiflavone A (1), along with eight known biflavonoids (2–9) were isolated from the 70% EtOH extract of Selaginella trichoclada. Their structures were elucidated by extensive spectroscopic analyses. Compound 1 was the first chalcone-flavonone type biflavonoid reported in the genus Selaginella. Moreover, compound 1 exhibited moderate cytotoxicity against DU145, MCF-7 and PC3 human cancer cell lines. [ABSTRACT FROM AUTHOR]

We designed a study to compare the newly developed 5‐mg flunarizine hydrochloride capsules (test) to that of its marketed counterpart (5‐mg; reference) among healthy adult Chinese volunteers. We performed an open‐label, single‐center study that consisted of 2 randomized, crossover trials, including a fasting trial and a fed trial. In each part of the study, the subjects were randomly assigned to either receive the test or reference products (5‐mg flunarizine) in a 1:1 ratio. Subjects then received the alternative products, following a 14‐day washout period. Concentrations of plasma flunarizine were analyzed using liquid chromatography–tandem mass spectrometry. Pharmacokinetic parameters (noncompartmental model) were evaluated using the WinNonlin software. The analysis of variance and Food and Drug Administration bioequivalence statistical criterion of 90% confidence interval for 80% to 125% range (set at P ≤.05) of geometric means ratios of test: reference product for peak plasma concentration, area under the plasma concentration–time curve (AUC) from time 0 to time t, and AUC from time 0 to infinity were determined. Tolerability was evaluated during the entire study period. Overall, 23 volunteers completed the fasting study, while 40 volunteers completed the fed study. The test formulation was found to be bioequivalent to the marketed formulation, as the 90% confidence interval for the ratio of geometric means of peak plasma concentration (fasting: 87.61%‐101.67%; fed: 87.38%‐104.06%), AUC from time 0 to time t (fasting: 89.44%‐99.92%; fed: 92.65%‐98.28%), and AUC from time 0 to infinity (fasting: 95.02%‐104.33%; fed: 90.41%‐96.96%) were within equivalence limits (80–125%) under both the fasting and fed conditions. When flunarizine was given alongside high‐fat meals, time to maximum concentration was delayed ≈3.5 hours compared to fasting conditions. Meantime, high‐fat meals increased its exposure by nearly 50%. Furthermore, there were no serious adverse events found among the subjects. This study confirmed that test and reference flunarizine hydrochloride capsules were bioequivalent under fasting and postprandial conditions. [ABSTRACT FROM AUTHOR]

Two new robustaflavones, (±)-trichocladabiflavone A (1) and uncinatabiflavone E (2), along with seven known biflavanoids (3–9) were isolated from the 70% EtOH extract of Selaginella trichoclada. Their structures and absolute configurations were established by extensive spectroscopic and circular dichroism (CD) analyses. Compound 1 was resoluted into optically pure enantiomers (+)-1 and (−)-1 by chiral-phase HPLC. Moreover, compounds 1 and 2 exhibited moderate cytotoxicity against A549 and HepG2 human cancer cell lines. [ABSTRACT FROM AUTHOR]

The aim of this study was to explore the bioequivalence of miglitol based on pharmacodynamic properties. The study was performed as a single‐dose, randomized, open‐label, 3‐period, 3‐way crossover trial over a 7‐day washout period. Forty‐eight subjects were randomly assigned into 3 groups: (1) miglitol test formulation/sucrose coadministration, (2) miglitol reference formulation/sucrose coadministration, and (3) sucrose administration alone. Serum glucose concentrations were measured by the hexokinase detection method. The peak serum glucose concentration (Cmax) and the area under the serum glucose concentration‐time curve through 4 hours (AUC0‐4h) were used as the main pharmacodynamic parameters to evaluate bioequivalence. The 90% confidence intervals for the geometric mean ratios of Cmax and AUC0‐4h were 94.81%‐101.07% and 98.82%‐100.72%, respectively, which were all within the bioequivalence range of 80.00%‐125.00%. The test and reference formulations of miglitol were pharmacodynamically bioequivalent during the trial. [ABSTRACT FROM AUTHOR]

Two new anthraquinone derivatives, selaginones A (1) and B (2), and one new triarylbenzophenone analog, selagibenzophenone B (3), were isolated from Selaginella tamariscina (Beauv.) Spring. Their structures were established by 1D-, 2D-NMR and HR-ESI-MS data. Compounds 1 and 2 represent the uncommon examples of aryl substituted anthraquinone derivatives. Especially, compound 2 is a unique anthranone with exceptional structural feature, in which a p-hydroxyphenyl moiety is attached to the C-10 position. Compound 3 is the second naturally occurring triarylbenzophenone and showed moderate activity against SMCC-7721 and MHCC97-H cell lines with IC50 values of 39.8, 51.5 μM respectively. [ABSTRACT FROM AUTHOR]

Three new neolignan derivatives (1–3), together with three known isolariciresinol derivatives (4–6) were isolated from Selaginella picta. Their structures were elucidated by spectroscopic methods (1D/2D NMR, HRESIMS and CD). All isolated compounds were assayed on the neuroprotective activity against the injury of HT-22 cells induced by L-Glutamate in vitro. All compounds displayed potent protective effect on HT-22 cells. [ABSTRACT FROM AUTHOR]

Phytochemical study on the n-BuOH extract of Selaginella delicatula lead to the isolation, characterization and structure elucidation of two new adenine analogues, delicatulines A (1) and B (2), one new pyrrole alkaloid (4), and five known compounds (3, 5–8). These new substances all contain an aliphatic chain in their parent nucleus, which were unusual to find in plants. In the present study, they were identified from Selaginellaceae for the first time. The structures and absolute configurations of these new compounds were determined by a combination of NMR and CD spectroscopic analyses. Compounds 1, 3 and 4 were evaluated for their inhibitory activities on HBV surface antigen and HBV DNA in HepAD38 cells. The results showed that these compounds had only weak or no inhibitive effects on HBV. [ABSTRACT FROM AUTHOR]

Abstract Four new trace alkaloids with lycodine-related structures, Lycocasuarinines A–D (1 – 4), together with seven known analogues (5 – 11), were isolated from the chloroform extract of Lycopodiastrum casuarinoides. The structures and stereochemistry of 1 – 4 were elucidated by spectroscopic analysis (IR, UV, MS, NMR, HRESIMS and CD) and comparison with known ones. The acetylcholinesterase (AChE) and butyrocholinesterase (BuChE) inhibitory activities of nine isolates were evaluated. Lycocasuarinine D (4) showed the most potent AChE inhibitory effect. In addition, a plausible biogenetic pathway of compound 4 was proposed. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Three new isobenzofuranone derivatives erinaceolactones D-F (1–3), together with four known ones (4–7), were isolated from the fruiting bodies ofHericium erinaceus. Their structures were determined on the basis of comprehensive spectroscopic analyses including UV, 1D, 2D NMR and HR-TOF-MS. The absolute configuration of erinaceolactone D (1) and erinaceolactone E (2) were assigned by comparing their specific rotation with those of analogs in literatures. The four known compounds were isomers with each other and were isolated simultaneously for the first time. [ABSTRACT FROM PUBLISHER]