Bioassay-guided isolation of α-Glucosidase inhibitory constituents from Hypericum sampsonii / 中国天然药物

This study employed the α-glucosidase inhibitory activity model as an anti-diabetic assay and implemented a bioactivity-guided isolation strategy to identify novel natural compounds with potential therapeutic properties. Hypericum sampsoniiwas investigated, leading to the isolation of two highly modified seco-polycyclic polyprenylated acylphloroglucinols (PPAPs) (1 and 2), eight phenolic derivatives (3-10), and four terpene derivatives (11-14). The structures of compounds 1 and 2, featuring an unprecedented octahydro-2H-chromen-2-one ring system, were fully characterized using extensive spectroscopic data and quantum chemistry calculations. Six compounds (1, 5-7, 9, and 14) exhibited potential inhibitory effects against α-glucosidase, with IC50 values ranging from 0.050 ± 0.0016 to 366.70 ± 11.08 μg·mL-1. Notably, compound 5 (0.050 ± 0.0016 μg·mL-1) was identified as the most potential α-glucosidase inhibitor, with an inhibitory effect about 6900 times stronger than the positive control, acarbose (IC50 = 346.63 ± 15.65 μg·mL-1). A docking study was conducted to predict molecular interactions between two compounds (1 and 5) and α-glucosidase, and the hypothetical biosynthetic pathways of the two unprecedented seco-PPAPs were proposed.

C. elegans-based screen identifies lysosome-damaging alkaloids that induce STAT3-dependent lysosomal cell death

Lysosomes are degradation and signaling centers within the cell, and their dysfunction impairs a wide variety of cellular processes. To understand the cellular effect of lysosome damage, we screened natural small-molecule compounds that induce lysosomal abnormality using Caenorhabditis elegans (C. elegans) as a model system. A group of vobasinyl-ibogan type bisindole alkaloids (ervachinines A-D) were identified that caused lysosome enlargement in C. elegans macrophage-like cells. Intriguingly, these compounds triggered cell death in the germ line independently of the canonical apoptosis pathway. In mammalian cells, ervachinines A-D induced lysosomal enlargement and damage, leading to leakage of cathepsin proteases, inhibition of autophagosome degradation and necrotic cell death. Further analysis revealed that this ervachinine-induced lysosome damage and lysosomal cell death depended on STAT3 signaling, but not RIP1 or RIP3 signaling. These findings suggest that lysosome-damaging compounds are promising reagents for dissecting signaling mechanisms underlying lysosome homeostasis and lysosome-related human disorders.

Alkaloids of Daphniphyllum angustifolium / 中国中药杂志

The alkaloids of Daphniphyllum angustifolium were investigated. The whole plant was extracted with 95% EtOH, six alkaloids were isolated and purified with column chromatography over silica gel, RP-18 and Sephadex LH-20. Based on spectral analysis, their structures were identified as daphnilactone B (1), zwitterionic alkaloid (2), yuzurine (3), dehydrodaphnigracilline (4), deoxyyuzurimine (5) and macrodaphniphyllidine (6). All of compounds were obtained from the plant for the first time.

Hasubanan type alkaloids in Stephania hernandifolia / 中国中药杂志

<p><b>OBJECTIVE</b>To study the hasubanan type alkaloids in Stephania hernandifolia.</p><p><b>METHOD</b>The dried herbs of S. hernandifolia. were extracted with 95% ethanol. After removal of the solvent, the residue was first partitioned between acid water and petroleum ether, then the aqueous layer was basified and extracted with chloroform to obtain crude alkaloids. Column chromatograghic methods with on silica gel, Rp-18, MCI CHP 20P, Sephadex LH-20 were applied for the isolation and purification of the crude alkaloid fraction. The structures were elucidated by their physicochemical properties and spectral data.</p><p><b>RESULT</b>Nine hasubanan type alkaloids were obtained and identified as aknadinine(1), longanone(2), stephasunoline (3), N-methylstephuline(4), epistephamiersine(5), prostephabyssine(6), aknadilactam(7), dihydroepistephamiersine(8), hasubanonine(9).</p><p><b>CONCLUSION</b>Compounds 2-8 were isolated from this plant for the first time.</p>

Water-soluble chemical constituents from fruits of Phellodendron chinense var. glabriusculum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the water-soluble chemical constituents from the fruits of Phellodendron chinense var. glabriusculum.</p><p><b>METHOD</b>Chemical constituents were purified by chromatographic methods and identified by spectroscopic analysis.</p><p><b>RESULT</b>Eight known compounds were obtained, whose structures were elucidated as sinapyl 9-O-beta-D-glucopyranoside (1), betulalbuside A (2), arbutin (3), adenosine (4), 3,5-dihydroxyphenethyl alcohol 3-O-beta-D-glucopyranoside (5), orcinol-3-O-beta-D-glucopyranoside (6), N-trans-p-coumaroyloctopamine (7), berberine (8) respectively.</p><p><b>CONCLUSION</b>Compounds 1-7 were obtained from Phellodendron chinense var. glabriusculum for the first time.</p>

Chemical constituents from involatile moiety of Pogostemon cablin / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of involatile moiety of Pogostemon cablin.</p><p><b>METHOD</b>Compounds were isolated and purified by repeated column chromatography, and their structures were elucidated by spectroscopic analysis.</p><p><b>RESULT</b>Nine compounds have been isolated and identified: epifriedelinol (1), 5-hydroxymethol-2-furfural (2), succinic acid (3), beta-sitosterol (4), daucosterol (5), crenatoside (6), 3'''-O-methylcrenatoside (7), isocrenatoside (8), and apigenin-7-O-beta-D-(6"-p-coumaryl)-glucoside (9).</p><p><b>CONCLUSION</b>Compounds 2, 3, 6-8 were isolated from Pogostemon genus for the first time.</p>

Diterpenoid alkaloids from roots of Aconitum recemulosum and their inhibitory effects on PAF-induced platelet aggregation / 中国中药杂志

<p><b>OBJECTIVE</b>To study diterpenoid alkaloids from the roots of Aconitum recemulosum, and their inhibitory effects on PAF-induced platelet aggregation.</p><p><b>METHOD</b>The root of A. recemulosum was extracted with 95% EtOH. The total alkaloids extracted were isolated and purified by several kinds of column chromatography over silica gel, RP-18, and Sephadex LH-20, and identified based on spectral analysis. And the inhibitory effects of isolated compounds on PAF-induced platelet aggregation were detected.</p><p><b>RESULT</b>Five alkaloids were isolated and identified as sachaconitine (1), 14-acetylsachaconitine (2), hemsleyanine C (3), circinasine A (4), and talatisamine (5). The results showed compounds 1 and 2 have moderate inhibition effect on PAF.</p><p><b>CONCLUSION</b>Compounds 1-5 were firstly isolated from this plant. Furthermore, compounds 1 and 2 possessed moderate inhibitory effects on PAF-induced platelet aggregation.</p>

Antitumor activities of chemical constituents of Cephalotaxus fortunei in Guizhou province / 中国药科大学学报

Aim: To study the antitumor activities of the constituents of Cephalotaxus fortunei distributed in Guizhou province. Methods: The constituents were isolated by column chromatography and identified by physical and spectral analysis. Meanwhile, the anti-tumor activities of some compounds were evaluated by sulforhodamine B( SRB) and MTT assay. Results: Eleven compounds were isolated and identified as apigenin (Ⅰ), β-sitosterol (Ⅱ), acetylcephalotaxine (Ⅲ), chrysoeriol (Ⅳ), drupacine ( Ⅴ), 1-hentriacontanol ( Ⅵ), 7, 3', 4' -trihydroxyfla-vone (Ⅶ), sugiol ( Ⅷ), cephalotaxine (Ⅸ), wllsonine (Ⅹ), and hainanolide (Ⅺ), respectively. Biological screening results demonstrated that some of the tested compounds exhibited the antitumor activities in vitro. Conclusion: Compounds Ⅱ, Ⅵ-Ⅷ were isolated from this plant for the first time. Compound Ⅺ has a better inhibitory activity on cell line A549 and K562 .

Studies on establishment of calli culture for rapid propagation of Spiraea japonica / 中草药

Object To establish a calli culture system for the rapid propagation of Speiraea japonica L. f.. Methods Callus and shoot induction were carried out on MS, 6, 7 V or B 5 media with different parts of the plant such as stem tip, tender leaves and petiole as explants. Results A calli culture system was established for the rapid propagation of S. japonica. Conclusion MS cultural medium was found to be most suitable for calli induction. MS with 2.0 mg/L 2,4 D+0.3 mg/L KT can induce calli when the explants were used for the induction, with stem tips being the most satisfactory explant. Clusters of seedlings can be induced on MS+2 mg/L BA+0.1 mg/L NAA and when these seedlings were transferred to 1/2 MS +0.25 mg/L BA+0.5 mg/L NAA medium, root were developed to give young seedlings.

Studies on chemical constituents of Callicarpa pedunculata / 中草药

Object To study the chemical constituents of whole plant of Callicarpa pedunculata R Brown Methods Various chromatographic techniques were employed for isolation and purification of its constituents; and their structures were identified by spectral analysis (IR, MS, 1HNMR, 13 CNMR) and chemical evidences Results Ten compounds were obtained from the chloroform extract of the whole plant Among them four were diterpenoids which were identified as: 14 ?-hydroxy-7, 15-isopimaradien-18-oic acid (Ⅰ), 16 ?, 17-dihydroxy-3-oxo-phyllocladanetriol (Ⅱ), 8, 11, 13, 15-abietetraen-18-oic acid (Ⅲ), and 6 ?-hydroxy nidorellol (Ⅳ); 2 flavonoids: 5-hydroxy-3, 4′, 7-trimethoxy-flavone (Ⅴ), and 3, 5-dimethyl kaempherol (Ⅵ); and the others were ursolic acid (Ⅶ), myoinositol (Ⅷ), ?-sitosterol (Ⅸ), and ?-amyrin (Ⅹ) Conclusion Compounds Ⅰ, Ⅱ, Ⅲ, Ⅳ were found in this plant for the first time and it was of interest to note that they were of different diterpenoid skeletons The content of ursolic acid attained to a high level up to 1%, which may be exploited as a natural resource for medical purposes