查看更多>>摘要：A phytochemical study on the MeOH extract of Lespedeza tomentosa roots led to the discovery of two new pterocarpans (labelled tomentocarpan A and B), along with three known pterocarpans and a flavanone. The structures of the two new compounds were found to be (6аR,1 laR)-1-methoxy-8-hydroxy-2',2'-dimethylpyrano[5',6':2,3]-2",2"-dimethylpyrano[6",5":9,10]pterocarpan (5), and l-methoxy-8-hydroxy-2',2'-dimethylpyrano[5',6':2,3]-2",2"-dimethylpyrano[6",5":9,10]pterocarp-6a(lla)-ene (6), based on comprehensive spectral and physical property analyses. Compounds 5 and 6 showed butyrylcholinesterase inhibitory activities with IC50 values of 0.50 and 0.62 mM, respectively.
查看更多>>摘要：A new cyclohexanone derivative (stipularone) was isolated from the leaves of Bridelia stipularis (L.) Blume and characterized using ID and 2D NMR spectroscopy (PMR, 13C NMR, HSQC, DEPT-135, COSY, and HMBC) and HR-ESI-MS. Four known compounds were also identified, 3- (4'-hydroxyphenyl)-2-propenoic acid (4"-carboxyl)-phenyl ester, p-amyrin, scopoletin, and 4- hydroxybenzoic acid, by comparing their PMR spectra with published results. The chemotaxonomic significance was discussed based on the structure of the isolated compounds.
查看更多>>摘要：A new s-truxillic acid derivative (1) and five known compounds (2-6) were isolated from the leaves of Palygala fallax. Their structures were elucidated by detailed spectroscopic analysis and comparison with literature data. All compounds were evaluated for their antiradical activities using in vitro DPPH radical scavenging assay. Compounds 5 and 6 showed moderate radical scavenging activity with EC50 value of 54.7 and 39.4 цМ.
查看更多>>摘要：Two new compounds (1 and 2), together with five known (3-7) stilbene derivatives, were isolated from the leaves and stems of Bletilla striata. Their structures were elucidated by spectroscopic methods, including extensive ID and 2D NMR techniques. Compounds 1 and 2 were evaluated for their cytotoxicity against ve human tumor cell lines. Compound 1 showed cytotoxicity against SHSY5Y and MCF7 cells with IC50 values of 2.8 and 2.2 uM. Compound 2 showed cytotoxicity against SHSY5Y and MCF7 cells with IC50 values of 2.2 and 2.4 uM, respectively. Moreover, Compound 1 was found to trigger both apoptosis and autophagy in Hela cells, as indicated by increased cleaved PARP and LC3B, respectively. The enhanced autophagy induced by compound 1 was further confirmed by imaging detection of more autophagosomes (mRFP-GFP-LC3+ puncta) and autolysosomes (mRFP-LC3+ puncta), as well as a low GFP/RFP fluorescence ratio of GFP-LC3-RFP. Signal pathway analysis indicated compound 1 might inhibit mTOR signaling to stimulate autophagy.
查看更多>>摘要：Crassine (1), Iiriodenine, (-)-anonaine, N-methylcorydaldine, p-hydroxybenzoic acid, p-hydroxybenzaldehyde, (+)-pinitol, P-sitosterol, stigmasterol, 11,13-dehydrolanuginolide, and costunolide were isolated from the roots of Michelia crassipes (Magnoliaceae). Among them, crassine is a new dimer of morpholine. The structure of crassine (1) was characterized and identified by spectral analyses.
jing-jin Wang Department of Biochemistry and Molecular Biology, School of Basic Medicine, Kunming MeLai-lai WongKe-Rong Jiang Department of Biochemistry and Molecular Biology, School of Basic Medicine, Kunming Me
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查看更多>>摘要：A new abietane diterpenoid, graciliflora A (1), was isolated from the aerial parts of Isodon lophanthoides var. graciliflorus. Its structure was elucidated by spectroscopic methods, including extensive ID and 2D NMR analysis. Compound 1 exhibited good anti-inflammatory and cytotoxic activities.
查看更多>>摘要：Получены новые производные изопимаровой кислоты по карбоксильной группе, исследована их анальгетическая активность на моделях висцеральной и термической боли. Амиды изопимаровой кислоты с фрагментом аминоэтанола и (2Я)-(гидроксиметил)пирролидина проявляют достоверную анальгетическую активность в тестах <<уксусные корчи>> (доза 5 и 25 мг/кг) и <<горячая пластина>> (доза 25 мг/кг), сравнимую с активностью препарата диклофенака натрия (доза 10 мг/кг). Новые агенты характеризуются низкой (LD50 > 1250 мг/кг) токсичностью in vivo. Выполнено молекулярное моделирование возможного взаимодействия наиболее активных соединений с трансмембранным G-протеинсвязанным каннабиноидным рецептором СВ2.
查看更多>>摘要：A new sterol, named 6p-methoxyergosta-7,9(11),22E-triene-3P,5a-dio! (1), together with seven known ones (2-8), was isolated from the fruiting bodies of Haddowia longipes. Their structures were identified on the basis of ID and 2D NMR spectroscopy as well as MS. The inhibitory activity of these isolates against acetylcholinesterase (AChE) showed that compound 1 exhibited weak inhibitory activity.
查看更多>>摘要：Взаимодействием производных тритерпеновых кислот лупанового и олеананового типа с гидразидами никотиновой и изоникотиновой кислот синтезированы С-17 и С-20 ацилгидразиды, дегидратация которых протекала с образованием соответствующих 1,3,4-оксадиазольных производных. Изучение цитотоксичности полученных соединений показало активность конъюгатов олеаноловой кислоты с ацилгидразидным и 1,3,4-оксадиазольным фрагментом (связанным с пиридин-4-ил- или пиридин-3-ильным заместителем) при атоме углерода С-17 тритерпенового остова. Наиболее активное соединение 3-оксо-28-нор-17-{2'-[Г,3',4'-оксадиазол-5'-(пиридин-4-ил)]ил}олеан-12(13)-ен ингибировало рост клеток лейкоза HL-60(TB), RPMI-8226, SR), рака толстой кишки (НСТ-116), почки (А498) и простаты (РС-3).
查看更多>>摘要：A facile total synthesis of tubifolidine has been developed, which is accomplished in an 11-step synthesis of the ABCDE pentacyclic of the strychnos alkaloids with an overall yield of 10%. The key steps are the cyclization reaction for starting tetrahydrocarbazoles bearing a nitrilealkyl side chain at the C-2 position, mediated by tetrachloro-l,4-benzoquinone (TCB) and the intramolecular addition of the amide as the nucleophile. This cyclization reaction was obtained with the relevant architecture, including strychnos skeletal-type alkaloids.
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