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1.
Nat Prod Res ; : 1-9, 2021 Dec 22.
Artigo em Inglês | MEDLINE | ID: mdl-34937440

RESUMO

Four sesquiterpenoids A-D (1-4) were isolated from the ethanol extracts of the leaves and stems from Schisandra chinensis. Their structures and absolute configurations were elucidated by a combination of NMR, MS and ECD. Compounds 1-4 (10 µM) exhibited moderate hepatoprotective activities against APAP-induced LO2 cell damage with increasing cell viability by 18%, 17%, 16%, and 19% compared to the model group (bicyclol, 26%) at 10 µM, respectively. All the compounds displayed no cytotoxic activity against five human cell lines, which also suggested the safety of leaves and stems of S. chinensis as an edible vegetable in a degree.

2.
Nat Prod Res ; : 1-10, 2021 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-34758696

RESUMO

Euphorfinoids A and B (1 and 2), a pair of ent-atisane diterpenoid epimers with a vicinal 2,3-diol moiety, together with four known analogues (3-6), were isolated from the roots of wild Euphorbia fischeriana. Their structures were elucidated by spectroscopic analysis, including extensive NMR, HR-ESIMS, NMR calculations, X-ray diffraction, and comparison with structurally related known analogues. Our bioassays have established that compound 1 displayed moderate anti-proliferative effects on Hcc1806 cell line with IC50 15.53 ± 0.21 µM, and compound 5 showed remarkable inhibitory effects against AChE with IC50 32.56 ± 2.74 µM by an in vitro screened experiment.

3.
Bioorg Chem ; 116: 105395, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34628224

RESUMO

Seven new triterpenoids including two cycloartanes (1-2), a lanostane (3), a tirucallane (4), a dammarane (5), an ursane (6), and an oleanane (7), along with nineteen known triterpenoids (8-26), have been obtained from the roots of Euphorbia fischeriana. Their structures were established by NMR, HRESIMS, single-crystal X-ray diffraction analysis, Mosher's method, NMR calculations, ECD analysis, and comparison with structurally related known analogues. Among them, compounds 1 and 8 were a pair of cycloartane-type triterpenoids epimers. Our bioassays have established that compounds 1-5 and 10 displayed moderate cytotoxic effects, and the structure-activity relationships of cycloartane-type triterpenoids (CTTs) were further examined. Notably, some triterpenoids displayed moderate inhibitory effects against AChE by an in vitro screened experiment. Triterpenoid 7 (Euphorfistrine G, ETG) displayed the potent inhibitory effect with IC50 = 2.45 and Ki = 2.30 µM (inhibition kinetic). And, in silico docking analyses have been performed to investigate the inhibitory mechanism of compound 7.

4.
J Ethnopharmacol ; 281: 114534, 2021 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-34419609

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hanchuan Zupa Granule (HCZP) is a classic prescription of Uyghur medicine, that is used for cough and abnormal mucinous asthma caused by a cold and "Nai-Zi-Lai". AIM OF THE STUDY: This study aimed to explore the possible molecular mechanism of HCZP in the treatment of asthma, using a network pharmacology method and in vivo experiments. MATERIALS AND METHODS: First, we conducted qualitative analysis of the chemical composition of HCZP as a basis for network pharmacology analysis. Using network pharmacology tools, the possible signaling pathways of HCZP in the treatment of asthma were obtained. An OVA-sensitized asthma model was established, and HCZP was continuously administered for one week. BALF was collected for cell counting, and serum and lung tissues were collected to analyze the expression of IgE, IL-4, IL-5, IL-13 and IFN-γ. Hematoxylin & eosin (H&E) staining was performed to assess the pathological changes in the lung tissues. Related protein expression in the lung tissues was analyzed by Western blotting for molecular mechanism exploration. RESULTS: Fifty-six chemical compounds were identified by UPLC Q-TOF MS. According to the network pharmacology results, 18 active compounds were identified among the 56 compounds, and 68 target genes of HCZP in the treatment of asthma were obtained. A total of 19 pathways were responsible for asthma (P < 0.05) according to KEGG pathway analysis. In vivo results showed that OVA sensitivity induced increased respiratory system resistance and inflammatory responses, which included inflammatory cell infiltration and high levels of IgE, IL-4, IL-5 and IL-13 in serum and lung tissues. Furthermore, OVA upregulated p-PI3K, p-JNK and p-p38 expression in lung tissues. Moreover, HCZP treatment significantly downregulated respiratory system resistance, and the expression of IL-4, IL-5, IL-13 and IgE, as well as significantly improved inflammatory cell infiltration in lung tissues. Moreover, the protein expression of p-PI3K, p-JNK and p-p38 in lung tissues decreased after HCZP treatment. CONCLUSION: HCZP significantly inhibited the OVA-induced inflammatory response via the PI3K-Akt and Fc epsilon RI signaling pathways.

5.
Planta Med ; 2021 Aug 06.
Artigo em Inglês | MEDLINE | ID: mdl-34359084

RESUMO

The root Rhynchosia volubilis was widely used for contraception in folk medicine, although its molecular mechanism on antifertility has not yet been revealed. In human sperm, it was reported that the cation channel of sperm, an indispensable cation channel for the fertilization process, could be regulated by various steroid-like compounds in plants. Interestingly, these nonphysiological ligands would also disturb the activation of the cation channel of sperm induced by progesterone. Therefore, this study aimed to explore whether the compounds in R. volubilis affect the physiological regulation of the cation channel of sperm. The bioguided isolation of the whole herb of R. volubilis has resulted in the novel discovery of five new prenylated isoflavonoids, rhynchones A - E (1:  - 5: ), a new natural product, 5'-O-methylphaseolinisoflavan (6: ) (1H and 13C NMR data, Supporting Information), together with twelve known compounds (7:  - 18: ). Their structures were established by extensive spectroscopic analyses and drawing a comparison with literature data, while their absolute configurations were determined by electronic circular dichroism calculations. The experiments of intracellular Ca2+ signals and patch clamping recordings showed that rhynchone A (1: ) significantly reduced cation channel of sperm activation by competing with progesterone. In conclusion, our findings indicat that rhynchone A might act as a contraceptive compound by impairing the activation of the cation channel of sperm and thus prevent fertilization.

6.
Phytochemistry ; 190: 112867, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34304117

RESUMO

Eight undescribed diterpenoids, euphorfinoids E-L, together with twelve known analogues, were isolated from the roots of wild Euphorbia fischeriana. Their structures and absolute configurations were elucidated by a combination of NMR, MS, ECD, and X-ray diffraction analyses. The plausible biosynthetic pathway of 1 was also proposed. The isolated compounds displayed moderate inhibitory activity against acetylcholinesterase (AChE) with 50% inhibiting concentration (IC50) values of 6.23-192.38 µM.


Assuntos
Antineoplásicos Fitogênicos , Inibidores da Colinesterase , Diterpenos , Euphorbia , Acetilcolinesterase , Inibidores da Colinesterase/farmacologia , Diterpenos/farmacologia , Estrutura Molecular , Raízes de Plantas
7.
J Asian Nat Prod Res ; : 1-11, 2021 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-33871296

RESUMO

A novel ent-pimarane-type diterpenoid, sigesbeckia J (1), along with two known diterpenoids, siegesbeckia acid (2) and ent-18-acetoxy-16R,17-dihydroxykauran-19-oic acid (3), were isolated from the aerial parts of Sigesbeckia glabrescens Makino. Their chemical structures were elucidated based on extensive spectroscopic interpretation. The absolute configuration of ent-pimarane-type diterpenoid (1) was determined by comparing experimental and calculated ECD spectra. Compared with the positive control minocycline (IC50 32.84 µM), compound 1 exhibited moderate cell growth anti-inflammatory activities in vitro by testing their inhibition of LPS-induced NO production in BV2 microglial cells, with IC50 value of 58.74 µM.

8.
Nat Prod Res ; : 1-7, 2021 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-33678085

RESUMO

Sophora flavescens Ait. has been utilized as an anticarcinogen, antibacterial and insecticide. Two new prenylflavonoids, Sophoflavonoid A (1) and Sophoflavonoid B (2), together with four known analogues were isolated from the root bark of S. flavescens. The structures of these compounds were elucidated by the interpretation of spectroscopic data and chemical evidence. Their absolute configurations were determined by ECD analysis. The inhibitory effects of compounds 1-6 against three lung carcinoma cells were determined using the MTT assay. The results revealed that compound 3 displayed strong cytotoxic effect against H460 cell line (IC50, 4.67 µM), while compounds 1, 4-6 exhibited significant inhibitory effects against three tumor cells. Therefore, this study suggests that the isopentenyl flavonoid-rich products of S. flavescens, including the new compounds, could be valuable candidates for the development of pharmaceuticals in the prevention and treatment for tumors.

9.
Fitoterapia ; 148: 104799, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33301798

RESUMO

Six new lignanoids, Glalignin A-E (1-5) and Glaneolignin A (6), together with four analogues, (+)-isolariciresinol (7), (+)-syringaresinol (8), dihydrodehydrodiconiferyl alcohol (9) and tribulusamide A (10), were obtained from the aerial parts of Sigesbeckia glabrescens Makino and also isolated for the first time from the Sigesbeckia genus. The structures of these compounds were elucidated by the interpretation of HRESIMS, 1D NMR, 2D NMR data and chemical evidence. The cytotoxic activities of the compounds were evaluated by testing their inhibition in several tumor cells using the MTT assay. New compound 2 and 5 displayed cytotoxicity against the human cancer cell lines human lung adenocarcinoma cells (A549) with IC50 values of 32.89 ± 6.83 and 35.86 ± 6.83 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Asteraceae/química , Lignanas/farmacologia , Células A549 , Antineoplásicos Fitogênicos/isolamento & purificação , China , Células HeLa , Humanos , Lignanas/isolamento & purificação , Células MCF-7 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Componentes Aéreos da Planta/química
10.
Nat Prod Res ; 35(9): 1452-1458, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-31450985

RESUMO

Three new phenolic glycosides, intermedia A-C (1-3), one new acyclic alcohol glycoside, intermedia D (4), together with 3 known glycosides (5-7), were isolated from the dried roots of Paeonia intermedia C. A. Meyer. Their structures were established by means of extensive spectroscopic analysis (HRESIMS, NMR). Compound 1 have a rare benzo[1,5]dioxepine skeleton. The bioassay results showed that compound 3 exhibited inhibitory activity against proinflammatory cytokines nitric oxide (NO) secretion in LPS-activated RAW264.7 cells with an IC50 value of 85.76 ± 1.36 µM.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Paeonia/química , Raízes de Plantas/química , Animais , Anti-Inflamatórios/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Glicosídeos/química , Lipopolissacarídeos/farmacologia , Camundongos , Óxido Nítrico/biossíntese , Pós , Espectroscopia de Prótons por Ressonância Magnética , Células RAW 264.7
11.
Nat Prod Res ; : 1-6, 2020 Sep 23.
Artigo em Inglês | MEDLINE | ID: mdl-32962440

RESUMO

A new cytisine-type alkaloid, along with five known alkaloids was obtained from the seeds of Sophora alopecuroides. Their structures were determined to be (-)-N-(2'-hydroxy-3',5'-di-tert-butyl-toluene)-cytisine (1), (-)-lupanine (2), (+)-matrine (3), (+)-sophoramine (4), (+)-lehmannine (5) and (-)-sophocarpine (6). Their structures were established by NMR, ECD and HRESIMS data analyses. Their cytotoxicity effects against five human tumor cell lines were tested by MTT assay. Compound 1 has showed a wide range of cytotoxicity activities against varied tumor cells in vitro.

12.
J Org Chem ; 85(13): 8580-8587, 2020 07 02.
Artigo em Inglês | MEDLINE | ID: mdl-32501005

RESUMO

Four pairs of stereoisomeric indole alkaloids, (±)-baphicacanthcusines A-D (1-4), and one new indole alkaloid, baphicacanthcusine E (5), together with nine known compounds were identified from the leaves of Baphicacanthus cusia. (±)-1 and -2 possess an unprecedented skeleton in which two indole moieties are bridged by a phenylpropane unit. (±)-3 represents the first natural dispiro-oxazolidinone bisoxindoles. The absolute configurations in 1-5 were assigned based on quantum chemical calculations, including the calculated chemical shift with DP4plus analysis, the calculated optical rotation values, and the calculated electronic circular dichroism spectra. A plausible biosynthetic pathway for 1-5 was proposed. Compounds (±)-1, (-)-2, and 11 exhibited cytotoxicity against MCF-7 cells with IC50 values of 20.0-78.5 µM.


Assuntos
Acanthaceae , Alcaloides , Alcaloides/farmacologia , Vias Biossintéticas , Alcaloides Indólicos/farmacologia , Estrutura Molecular , Folhas de Planta
13.
Nat Prod Res ; : 1-6, 2020 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-32408767

RESUMO

A chemical investigation of Sophora flavescens Ait. identified 6 compounds. On the basis of spectroscopic data, they were determined to be flavonoids and their analogues, among which were two previously undescribed compounds, sophoflavanone G (1) and sophoflavanone H (2). The inhibitory effects of new compounds against five human tumour cell lines were evaluated in vitro by MTT assays, which revealed potential inhibitory effects with IC50 values < 20 mM, in particular, compound 1 has shown significant cytotoxicity for several tumour cells with IC50 values around 20 mM, which was similar to cisplatin and potential to be used as tumour drugs.

14.
Molecules ; 25(2)2020 Jan 19.
Artigo em Inglês | MEDLINE | ID: mdl-31963799

RESUMO

Three new isoflavone glucosides, kudonol A-C (1-3), two new ester derivatives of phenylpropanoid, kudolignan A and B (4-5) and five known compounds, (-)-maackiain (6), neoliquiritin (7), methyl 4-coumarate (8), methyl ferulate (9) and (+)-wikstromol (10), were isolated from an extract of dried seeds of the traditional Chinese medicinal plant Sophora alopecuroides L. Their structures were established by NMR and HRESIMS data analyses. The monosaccharide part's configuration of isoflavone glucosides was confirmed by acid hydrolysis and analyzed by a JAsco OR-4090 chiral detector, comparing it to standard substance D-glucose. The cytotoxicity effects against HeLa, Hep3B, MCF-7 and H1299 cells were tested by CCK-8 assay.


Assuntos
Sementes/química , Sophora/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Extratos Vegetais/farmacologia , Espectroscopia de Prótons por Ressonância Magnética
15.
J Asian Nat Prod Res ; 22(9): 823-829, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31583898

RESUMO

Two new alcohol glycosides, 1-O-ß-d-glucopyranosyl-deoxypaeonisuffrone (1) and 9-O-ß-d-apiofuranoyl-(1→6)-ß-d-glucopyranosyl-xanthoarnol (2), together with eight known compounds (3-10), have been isolated from the dried roots of Paeonia intermedia C. A. Meyer. Their structures were mainly elucidated on the basis of ESIMS, one- and two-dimensional NMR techniques. Antibacterial activities of compounds 1-10 were evaluated, and compounds 9 and 10 showed antibacterial activities against Staphylococcus argenteus CMCC26003 and Escherichia coli CMCC44103. [Formula: see text].


Assuntos
Glicosídeos , Paeonia , Estrutura Molecular , Raízes de Plantas , Staphylococcus
16.
Nat Prod Res ; 34(24): 3437-3443, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30835543

RESUMO

A chemical investigation of Cynanchum mongolicum (Maxim.) Kom. identified 8 compounds. On the basis of spectroscopic data, they were determined to be 3 alkaloids and 5 sinapoyl esters, among which were two previously undescribed compounds (1 and 2). The inhibitory effects of the isolated compounds against four human tumor cell lines were evaluated in vitro by MTT assays, which revealed moderate inhibitory effects with IC50 values < 50 mM, in particularly, three antofine analogues have showed significant antitumor activities with IC50 values < 0.1 mM, which was obviously better than the 5-fluorouracil and potential to be used as cancer drugs.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Cynanchum/química , Compostos Fitoquímicos/química , Alcaloides/química , Alcaloides/farmacologia , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Indóis/química , Indóis/farmacologia , Estrutura Molecular , Fenantrolinas/química , Fenantrolinas/farmacologia , Compostos Fitoquímicos/farmacologia
17.
J Asian Nat Prod Res ; 20(10): 992-1001, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28944681

RESUMO

The chemical characteristic of a well-known folk medicine Ganoderma lucidum has been investigated by a series of chromatographic technologies, which displayed the presences of 45 lanostane type triterpenoids, including two new nor-lanostane triterpenoids (40, 41). Their structures were identified on the basis of spectroscopic data analysis (UV, IR, HRESIMS, 1D, and 2D NMR). Notably, some triterpenoids displayed moderate inhibitory effects against AChE (acetylcholinesterase) by an in vitro screened experiment. Triterpenoid 2 displayed the potent inhibitory effect with IC50 10.8 and Ki 14.95 µM (inhibition kinetic). The preliminary SAR has been discussed by the docking analyses between ganoderic acids (1, 2) and AChE.


Assuntos
Inibidores da Colinesterase/farmacologia , Ganoderma/química , Triterpenos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Modelos Moleculares , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/farmacologia
18.
J Asian Nat Prod Res ; 20(10): 977-984, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28944698

RESUMO

Chemical investigation has been performed on the roots of Euphorbia fischeriana, a traditional Chinese medicine. Three diterpenoids were obtained using various chromatographic techniques, and their structures were determined by spectroscopic data including HRESIMS, 1D NMR, 2D NMR, ECD, and calculated ECD, which gave two new diterpenoids, daphnane type (1) and ent-pimarene type (3). Additionally, the isolated compounds (1-3) displayed moderate inhibitory effects against α-glucosidase in an in vitro bioassay.


Assuntos
Diterpenos/isolamento & purificação , Euphorbia/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Espectroscopia de Ressonância Magnética , Raízes de Plantas/química
19.
Phytochemistry ; 146: 82-90, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29253734

RESUMO

A chemical investigation of the roots of Euphorbia ebracteolata identified eighteen diterpenoids and glycosides. On the basis of spectroscopic data, they were determined to be ent-kauranes, ent-atisanes, tigliane derivatives, ingenane, and ent-abietanes, among which were eleven previously undescribed diterpenoids. The inhibitory effects of the isolated compounds against human carboxylesterase 2 (hCE-2) were evaluated in vitro, which revealed moderate inhibitory effects with IC50 values < 50 µM. Next, the inhibitory kinetics were evaluated for the putative hCE-2 inhibitor 4ß,9α,16,20-tetrahydroxy-14(13 → 12)-abeo-12αH-1,6-tigliadiene-3,13-dione (IC50 3.88 µM), and results indicated competitive inhibition with Ki 4.94 µM. Additionally, none of the diterpenoids showed cytotoxic effects against five human tumor cell lines as determined by MTT assays.


Assuntos
Carboxilesterase/antagonistas & inibidores , Diterpenos/farmacologia , Inibidores Enzimáticos/farmacologia , Euphorbia/química , Raízes de Plantas/química , Carboxilesterase/metabolismo , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Conformação Molecular , Estereoisomerismo , Relação Estrutura-Atividade
20.
Zhongguo Zhong Yao Za Zhi ; 42(15): 2995-2998, 2017 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-29139269

RESUMO

A variety of chromatographic methods were applied to research the chemical composition of the roots of Euphorbia ebracteolata. Meanwhile, the structures of these compounds were identified by spectroscopic data, such as 1D, 2D NMR and HR-ESI-MS. In the present research, a new phenolic acid compound, 1,3,4,5-tetrahydroxy-2-O-ß-D-[(6'-Gallic acyl)-glucopyranyl] isopentane(1), was isolated from the roots of E. ebracteolata, as well as three known compounds, isopropyl-2-O-ß-D-(6'-gallic acyl)-glucopyranoside(2), ellagic acid(3) and 3,4'-di-O-methylellagic acid(4) respectively. Additionally, compounds 2 and 4 were isolated from the Euphorbia genus for the first time.


Assuntos
Euphorbia/química , Hidroxibenzoatos/química , Raízes de Plantas/química , Estrutura Molecular , Compostos Fitoquímicos/química
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