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1.
Aster flaccidus bge has been used as traditional medicine in northwestern China. Two new phenylpropanoids (1–2) including one lignan: (7′R, 8S)-9′-lariciresinol-(α-methyl)-butanoate (1), 5,9-dimethoxyl-7-(α-methyl)-butanoxyl-phenyl-2E-propenol-(α-methyl)-butanoate (2) isolated from the chloroform extract of the root of Aster flaccidus bge were identified by means of extensive spectroscopic studies: 1D and 2D NMR spectra as well as HRMS analysis. They have not obvious anti-HIV-1 therapeutic activity (TI = 1.0–1.1) compared with AZT (TI = 55,556) as the result of the determination of their in vitro anti-HIV-1 activity while compound 2 displays strong antitumor activity against BEL 7402 (human liver carcinoma) with cisplatin as a positive control and the effect increases with the measuring-time going on (24 h, IC50: 106.67 ± 8.47 µM — 72 h, IC50: 50.51 ± 6.11 µM).  相似文献   

2.
The flavonoid pattern of an acetonic extract of Grindelia robusta Nutt. was investigated in detail. The flavonoids were enriched by CC. In addition to twelve known methylated exudate flavonols four compounds were identified for the first time in G. robusta. Several substances of the flavonoid complex, among them the main compounds quercetin-3-methylether and 6-OH-kaempferol-3,6-dimethylether, were tested for their activity to inhibit neutrophil elastase. Quercetin-3-methylether was shown to be most active with an IC50 of 19 µM, thus obviously contributing to the anti-inflammatory activity of the drug.  相似文献   

3.
The present study describes for the first time the in vitro properties of Iris pseudopumila flowers and rhizomes extracts and their constituents. The methanolic extract of rhizomes showed significant anti-inflammatory activity through inhibition of NO production in the murine monocytic macrophage cell line RAW 264.7. Among the isolated compounds, those which most effectively inhibited LPS-induced NO production were irisolidone and 7-methyl-tectorigenin-4′-O-[β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside], with IC50 values of 23.6 μM and 29.4 μM respectively. Isoorientin and isovitexin exhibited the most promising activity against AChE with IC50 of 26.8 μM and 36.4 μM, respectively. The same compounds exhibited also the higher activity against BChE.  相似文献   

4.
The methanol extract from aerial parts of the Peperomia blanda (Piperaceae) yielded two C-glycosyl-flavones. Their structures were elucidated on the basis of extensive spectroscopic analysis, including 1D and 2D NMR, chemical transformation and comparison with the related known compounds. The structure of the new flavonoids were established as 4′-methoxy-vitexin 7-O-β-d-xylopyranoside (1) (7-O-β-d-xylopyranosyl-8-C-β-d-glucopyranosyl-4′-methoxy-apigenin) and vicenin-2 (2). The antioxidant activity of both compounds was investigated using the DPPH assay. Both compounds showed only modest activity, with IC50 values of 357.2 µM for 1, and 90.5 µM for 2.  相似文献   

5.
In our efforts to find new whitening agent from natural resources, we focused on wood of Artocarpus heterophyllus which shows anti-melanogenesis activity. By activity-guided fractionation of A. heterophyllus wood extract, a new prenylated flavonoid, 3-prenyl luteolin (1) was isolated. The IC50 of mushroom tyrosinase inhibitotry activity of 1 was 76.3 µM. The results of the comparison with that of luteolin showed the prenyl substituent at C-3 position of 1 play an important role for revealing tyrosinase inhibition. In melanin formation inhibition on B16 melanoma cells, IC50 of 1 was 56.7 µM with less cytotoxicity.  相似文献   

6.
Ethanolic extract from the fruits of Pimpinella anisoides, an aromatic plant and a spice, exhibited activity against AChE and BChE, with IC50 values of 227.5 and 362.1 μg/ml, respectively. The most abundant constituents of the extract were trans-anethole, (+)-limonene and (+)-sabinene. trans-Anethole exhibited the highest activity against AChE and BChE with IC50 values of 134.7 and 209.6 μg/ml, respectively. The bicyclic monoterpene (+)-sabinene exhibited a promising activity against AChE (IC50 of 176.5 μg/ml) and BChE (IC50 of 218.6 μg/ml).  相似文献   

7.
Wu Y  Zhang ZX  Hu H  Li D  Qiu G  Hu X  He X 《Fitoterapia》2011,82(2):288-292
Two novel indole C-glycosides, which were the first reported alkaloids C-glycosides from Isatis indigotica, together with five known alkaloids were isolated. The novel alkaloids were elucidated to be indole-3-acetonitrile-4-methoxy-2-C-β-D-glucopyranoside (1) and N-methoxy-indole-3-acetonitrile-2-C-β-D-glucopyranoside (2) on the basis of spectroscopic analysis. 1 exhibited significant cytotoxic activities against human myeloid leukemia HL-60 and human liver cancer HepG2 cells with the IC50 of 1.3 ± 0.1 and 2.1 ± 0.3 μM, respectively. 2 showed potential cytotoxic activities against HL-60 and human myeloid leukemia Mata cells with the IC50 of 5.1 ± 0.4 and 12.1 ± 0.8 μM, respectively.  相似文献   

8.
A pair of new isomeric indole alkaloids, naucleaorals A (1) and B (2) were isolated from the roots of Nauclea orientalis. The structures of compounds 1 and 2 were fully characterized using spectroscopic data, and were tested for their cytotoxicity (HeLa and KB cells) and antimalarial activity. Compound 1 showed significant cytotoxicity to HeLa cells with an IC50 value of 4.0 µg/mL, while compound 2 exhibited very modest cytotoxicity to both cell lines with IC50 values of 7.8 and 9.5 µg/mL, respectively. Both compounds proved to be inactive in antimalarial assays (IC50 > 10.00 µg/mL).  相似文献   

9.
Eight steroidal alkaloids, puqienine A, puqienine B, puqienine C, puqienine D, puqienine E, puqietinone, puqiedine and peimisine were isolated from Fritillaria puqiensis G. D. Yu et. G. Y. Chen, and their anti-hypertensive effect were assessed in vitro based on the inhibition of the purified angiotensin converting enzyme (ACE) using high-performance liquid chromatography assay. The results showed that puqienine E, puqienine B and puqienine A exhibited better inhibitory activity against ACE than others, with inhibition ratios of 70.2 ± 0.5%, 24.7 ± 0.5% and 20.4 ± 2.8%, respectively at the concentration of 200 μM. The 50% inhibiting concentration of puqienine E was determined to be 68 µM.  相似文献   

10.
Callus and differentiated shoots initiated from Solanum tuberosum L. on MS media containing BA, IAA, and Kin. Glycoalkaloids are produced in callus and shoots in concentrations higher than original tubers using HPLC. Callus methanolic extract had promising anticancer activity with low IC50 values against human carcinoma cell lines of breast, lymphoplastic leukemia, larynx, liver, cervix, colon, and brain, IC50 (µg/mL) were 2.7, 3.7, 6, 6.7, 10, 13.6, and 22.3 respectively. Antioxidant capacity of the extract (76.4%) performed using ESR. Preliminary screening showed that the extract exhibited in vitro virucidal activity against Herpes simplex. The extract possessed in vitro schistomicidal and fasciolicidal activity.  相似文献   

11.
This investigation focuses on the in vitro neuroactive properties of pinostrobin, a substituted flavanone from Cajanus cajan (L.) Millsp. of the Fabaceae family. We demonstrate that pinostrobin inhibits voltage-gated sodium channels of mammalian brain (IC50 = 23 µM) based on the ability of this substance to suppress the depolarizing effects of the sodium channel-selective activator veratridine in a synaptoneurosomal preparation from mouse brain. The resting membrane potential of synaptoneurosomes was unaffected by pinostrobin. The pharmacological profile of pinostrobin resembles that of depressant drugs that block sodium channels.  相似文献   

12.
A 70% ethanol extract of the branches of Hippophae rhamnoides exhibited remarkable antitumor activity in an in vivo two-stage carcinogenesis test in mice using 7,12-dimethylbenz[a]anthracene as an initiator and 12-O-tetradecanoylphorbol-13-acetate (TPA) as a promoter. From the active fraction of the 70% ethanol extract, three phenolic compounds, (+)-catechin (1), (+)-gallocatechin (2), and (−)-epigallocatechin (3) and a tritepenoid, ursolic acid (4) were isolated and identified. These compounds were evaluated for their inhibitory effects on TPA-induced inflammation (1 µg/ear) in mice. Within the tested compounds, 3 and 4 showed marked anti-inflammatory effects, with a 50% inhibitory dose of 1.7 and 0.2 μmol/ear.  相似文献   

13.
Pistacia integerrima Stewart in traditionally used as folk remedy for various pathological conditions including diabetes. In order to identify the bioactive compound responsible for its folk use in diabetes, a phytochemical and biological study was conducted. Pistagremic acid (PA) was isolated from the dried galls extract of P. integerrima. Strong α-glucosidase inhibitory potential of PA was predicted using its molecular docking simulations against yeast α-glucosidase as a therapeutic target. Significant experimental α-glucosidase inhibitory activity of PA confirmed the computational predictions. PA showed potent enzyme inhibitory activity both against yeast (IC50: 89.12 ± 0.12 μM) and rat intestinal (IC50: 62.47 ± 0.09 μM) α-glucosidases. Interestingly, acarbose was found to be more than 12 times more potent an inhibitor against mammalian (rat intestinal) enzyme (having IC50 value 62.47 ± 0.09 μM), as compared to the microbial (yeast) enzyme (with IC50 value 780.21 μM). Molecular binding mode was explored via molecular docking simulations, which revealed hydrogen bonding interactions between PA and important amino acid residues (Asp60, Arg69 and Asp 70 (3.11 Å)), surrounding the catalytic site of the α-glucosidase. These interactions could be mainly responsible for their role in potent inhibitory activity of PA. PA has a strong potential to be further investigated as a new lead compound for better management of diabetes.  相似文献   

14.
Six new acylphloroglucinol derivatives, sampsonols A-F (1–6), were isolated from the petroleum ether extract of the aerial parts of Hypericum sampsonii. The structures and relative configurations of sampsonols A-F were elucidated by extensive spectroscopic analyses. All these compounds were tested for their in vitro cytotoxic and anti-inflammatory activities. Sampsonols A and B (1 and 2) showed significant cytotoxicity against four human tumor cell lines with IC50 values in the range of 13–28 μM, whereas sampsonols C and F (3 and 6) showed potent inhibitory activities against LPS-induced NO production in RAW 264.7 macrophages with IC50 values of 27.3 and 29.3 μM, respectively.  相似文献   

15.
Two new prenylated xanthones and a new prenylated tetrahydroxanthone, garcimangosxanthone A–C (1–3), along with fourteen known xanthones were isolated from the pericarp of Garcinia mangostana. Their structures were elucidated on the basis of spectroscopic data. Compounds 1 and 2 exhibited in vitro cytotoxicity against A549, LAC and A375 cell lines with IC50 values of 5.7–24.9 μM, which were comparable to those of doxorubicin.  相似文献   

16.
Two new benzofuran derivatives, 2-(4′-hydroxybenzyl)-5,6-methylenedioxy-benzofuran () and 2-(4′-hydroxybenzoyl)-5,6-methylenedioxy-benzofuran (), along with 8 known compounds were isolated from 60% EtOH extract of the fibrous roots of Liriope spicata var. prolifera. Their structures were elucidated on the basis of extensive spectroscopic analysis. In an in vitro bioactive assay, the two new benzofuran derivatives showed anti-inflammatory activity. Compounds 1 and 2 exhibited significant inhibitory activity against neutrophil respiratory burst stimulated by phorbol 12-myristate 13-acetate (PMA) with IC50 value of 4.15 ± 0.07 and 5.96 ± 0.37 μM, respectively.  相似文献   

17.
The occurrence of the two new cis-fused A/B rings furostanol saponins (25S)-26-O-β-d-glucopyranosyl-5β-furostan-1β,3β,22α,26-tetraol-1-O-β-d-glucopyranoside and (25S)-26-O-β-d-glucopyranosyl-5β-furostan-1β,2β,3β,5β,22α,26-hexaol and the known compounds (25S)-26-O-β-d-glucopyranosyl-5β-furostan-3β,22α,26-triol-3-O-α-l-rhamnopyranosyl-(1→2)-O-β-d-glucopyranosyl-(1→2)-O-β-d-glucopyranoside and (25S)-26-O-β-d-glucopyranosyl-5β-furostan-3β,22α,26-triol-3-O-β-d-glucopyranosyl-(1→2)-O-β-d-glucopyranoside, trans-resveratrol, (+) catechin and (−) epicatechin in the rhizomes of Smilax aspera is reported. All saponins have been isolated as their 22-OMe derivatives, which were further subjected to extensive spectroscopic analysis. The isolated furostanol saponins were evaluated for cytotoxic activity against human normal amniotic and human lung carcinoma cell lines using neutral red and MTT assays. In vitro experiments showed significant cytotoxicity in a dose dependent manner with IC50 values in the range of 32.98-94.53 µM.  相似文献   

18.
Feng S  Hao J  Xu Z  Chen T  Qiu SX 《Fitoterapia》2012,83(1):161-165
A rare naturally-occurring polyprenylated isoflavanone, designated ormosinol (1), and a new isoflavonoid glycoside, named ormosinoside (2), along with 21 known compounds were isolated from the root bark of Ormosia henryi Prain. The structures of compounds 1 and 2 were determined as 5,7,2′,4′-tetrahydroxyl-6,8,5′-tri-(γ,γ-dimethylallyl)isoflavanone and isoprunetin-7-O-β-d-xylopyranosyl-(1 → 6)-β-d-glucopyranoside on the basis of a combination of 1D-, 2D-NMR and mass spectroscopic measurements. Compound 1 showed significant anti-oxidation activity against DPPH radicals (IC50 28.5 μM) and cancer cell line (A549, LAC, and HepG2) growth inhibitory activity with IC50 ranging from 4.25 to 7.09 μM, while compound 2 found to be inactive to both testing systems.  相似文献   

19.
Cytochrome P450 (CYP) enzyme inhibitory properties of six chromenylated amide compounds (CAs) from Amyris plumieri are described. Inhibition of CYP microsomes (CYP1A1, CYP1A2, CYP1B1, CYP2D6, CYP3A4 and CYP2C19) was monitored using a fluorescent assay. Potent inhibition was found against CYP1A1 with IC50 and Ki for CA1 (acetamide), being the lowest at 1.547 ± 1.0 μM and 0.37 μM respectively, displaying non-competitive kinetics. The selectivity for CYP1A1 was increased in CA3 (butanamide), which also exhibited cytotoxicity against breast cancer cells, MCF7 with an IC50 of 47.46 ± 1.62 μM. Structure-activity relationship studies provide insight at a molecular level for CAs with implications in chemoprevention and chemotherapy.  相似文献   

20.
Methicillin-resistant Staphylococcus aureus (MRSA) is a major nosocomial pathogen which causes severe morbidity and mortality worldwide. Seventeen Thai medicinal plants were investigated for their activity against MRSA. Garcinia mangostana was identified as the most potent plant, and its activity was traced to the prenylated xanthone, α-mangostin (MIC and MBC values of 1.95 and 3.91 µg/ml, respectively).  相似文献   

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