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1.
Molecules ; 26(21)2021 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-34770935

RESUMO

Catharanthus roseus is a well-known traditional herbal medicine for the treatment of cancer, hypertension, scald, and sore in China. Phytochemical investigation on the twigs and leaves of this species led to the isolation of two new monoterpene indole alkaloids, catharanosines A (1) and B (2), and six known analogues (3-8). Structures of 1 and 2 were established by 1H-, 13C- and 2D-NMR, and HREIMS data. The absolute configuration of 1 was confirmed by single-crystal X-ray diffraction analysis. Compound 2 represented an unprecedented aspidosperma-type alkaloid with a 2-piperidinyl moiety at C-10. Compounds 6-8 exhibited remarkable Cav3.1 low voltage-gated calcium channel (LVGCC) inhibitory activity with IC50 values of 11.83 ± 1.02, 14.3 ± 1.20, and 14.54 ± 0.99 µM, respectively.


Assuntos
Bloqueadores dos Canais de Cálcio/farmacologia , Canais de Cálcio Tipo T/química , Catharanthus/química , Alcaloides Indólicos/farmacologia , Monoterpenos/farmacologia , Extratos Vegetais/farmacologia , Bloqueadores dos Canais de Cálcio/química , Canais de Cálcio Tipo T/metabolismo , Relação Dose-Resposta a Droga , Alcaloides Indólicos/química , Conformação Molecular , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Monoterpenos/química , Extratos Vegetais/química , Relação Estrutura-Atividade
2.
Nat Prod Bioprospect ; 11(5): 557-564, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34089490

RESUMO

Three new clerodane-type diterpene glycosides, (5R,6S,8R,9S,10R)-6-O-[ß-D-glucopyranosyl-(1 → 4)-α-L-rhamnopyranosyl]cleroda-3,13(16),14-diene (1), (5R,6S,8R,9S,10R,13S)-6-O-[ß-D-glucopyranosyl-(1 → 4)-α-L-rhamnopyranosyl]-2-ox-oneocleroda-3,13-dien-15-ol (2), (5R,6S,8R,9S,10R)-6-O-[ß-D-glucopyranosyl-(1 → 4)-α-L-rhamnopyranosyl]-(13E)-2-oxoneocleroda-3,14-dien-13-ol (3), together with two known compounds 4 and 5 were isolated from Dicranopteris pedata. The structures of these compounds were elucidated by detailed spectroscopic analysis, and the absolute configuration of compound 2 was determined by ECD calculations. In addition, compound 1 exhibited weak inhibitory activities against SMMC-7721, MCF-7 and SW480.

3.
Des Monomers Polym ; 20(1): 344-350, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29491805

RESUMO

Through metal-free protocol, hypercrosslinked porous polyporphyrin with permanent porosity was obatined via the Friedel-Crafts alkylation of tetracarbazolylporphyrin using formaldehyde dimethyl acetal as an external cross-linker. Its chemical structure and porosity was well characterized and confirmed. The BET specific surface area value of HCP-TCPP is 1050 m2 g-1 and related dominant pore size is centered at 0.63 nm. The adsorption amount of methanol by HCP-TCPP is high up to 800 mg g-1 (about 25.0 mmol g-1) at its saturated vapor pressure, which is higher than that of toluene (600 mg g-1, 6.5 mmol g-1). Further study indicates that polymer HCP-TCPP, possessing the high BET specific surface area and total pore volume, exhibits good hydrogen uptake of 3.44 wt % (77 K) and high carbon dioxide uptake of 41.1 wt % (298 K) at 18.0 bar. Besides, the obtained porous polymer can also be used as an effective heterogeneous catalyst for the Knoevenagel condensation between various aldehydes and malononitrile.

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