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1.
Two new amide alkaloids, named 3-isopropyl-tetrahydropyrrolo [1,2-a] pyrimidine-2,4(1H,3H)-dione (1) and 1-acetyl-2,3,6-triisopropyl-tetrahydropyrimidin-4(1H)-one (2), were isolated from the roots of Aconitum taipeicum. Their chemical structures were characterized on the basis of MS, 1D- and 2D NMR. The anti-leukaemia activities of the compounds were also tested. The results indicated that the compounds exhibited more significant cell growth inhibitory activities against HL-60 cells than adriamycin, with the IC50 of 1.1 ± 0.03 μg/mL and 1.6 ± 0.07 μg/mL respectively. In addition, two compounds showed anti-tumor activities against K562 cells as well. 相似文献
2.
Inamullah Khan Muhammad Nisar Nematullah Khan Muhammad Saeed Said Nadeem Fazal-ur-Rehman Farooq Ali Nasiara Karim Waqar Ahmad Kaleem Mughal Qayum Hanif Ahmad Ihsan Ali Khan 《Fitoterapia》2010,81(8):1020-1025
The main aim of the current study was to explore molecular insights for potentially new dual cholinesterase inhibitor(s) from Asparagus adscendens via molecular docking. This medicinal plant is traditionally used as a nerve tonic and remedy for memory impairments. Conypododiol was isolated from the chloroform fraction of methanolic extract of A. adscendens, based on bioactivity guided isolation. Conypododiol exhibited significant inhibition of both acetylcholinesterase and butyrylcholinesterase, having the IC50 values 2.17 ± 0.1 μM and 11.21 ± 0.1 μM, respectively. IC50 values of the standard compound Galanthamine for both the enzymes were 0.537 ± 0.018 μM and 8.6 ± 0.27 μM, respectively. Based on MTT cytotoxicity assay, Conypododiol was found safe against LCMK-2 monkey kidney epithelial cells and mice hepatocytes. Molecular docking studies revealed the hydrogen bonding interactions of Conypododiol with His440 and Ser200 at esteratic site (ES), and also with Tyr334 at peripheral anionic site (PAS) of the aromatic gorge of acetylcholinesterase. Simultaneous contacts of Conypododiol with PAS and ES shows its significance as a bivalent ligand. This preliminary study highlighted the potential of Conypododiol to be further developed and modified as new lead compound identified by its folk use. 相似文献
3.
A new coumestan, 1,3,9-trihydroxy-8-methoxycoumestan, named flemicoumestan A 1 together with nine isoflavone-related compounds were isolated from the ethyl acetate extract of the roots of Flemingia philippinensis. Their structures were elucidated and confirmed by spectroscopic methods and literature data. Compounds 3 and 4 showed strong lymphocyte proliferation inhibitory activity with an IC50 value of 1.04-2.76 μM, and the low cytotoxicity with the CC50 value of 71.01 and 56.36 μM, respectively. 相似文献
4.
Yuji Tsutsumi Ayako Shimada Akiko Miyano Tomoaki Nishida Tohru Mitsunaga 《Journal of Wood Science》1998,44(6):463-468
Screening and isolation of angiotensin I-converting enzyme (ACE) inhibitors from Japanese cedar (Cryptomeria japonica) based on the in vitro ACE inhibitory assay were attempted. The ethanol extract from outer bark showed the highest inhibitory activity (IC50 is 16g/ml) among 24 extracts prepared from roots, leaves, heartwood, sapwood, inner bark, and outer bark by successive extraction with four solvents. The fractionation of the outer bark ethanol extract followed by the bioassay resulted in the isolation of two strong ACE inhibitors, catechin and dimeric procyanidin B3. The bioassay of three flavan-3-ols including (+)-catechin and six flavones revealed that most of these compounds have high ACE inhibitory activity. The results suggest that the phenolic hydroxyl group at the C7 position and heterocyclic oxygen atom of these compounds are important for expressing the inhibitory activity. 相似文献
5.
Luciane Anita Savi Thiago Caon Ana Paula de Oliveira Andrea Michel Sobottka Wolfgang Werner Flvio Henrique Reginatto Eloir Paulo Schenkel Clia Regina Monte Barardi Cludia Maria Oliveira Simes 《Fitoterapia》2010,81(8):1142-1146
Flavonoids are dietary components and the most ubiquitous phenolic compounds found in nature, showing a range of pharmacological activities including antiviral action. This study describes the antiviral screening of 60 different flavones and flavonols against human rotavirus (Wa-1 strain) as well as their cytotoxicity in MA104 cells. Cytotoxicity was investigated by cell morphology assessment and antirotavirus activity by cytopathic effect inhibition. Results were expressed as CC50 and IC50, respectively, in order to calculate the selectivity index (SI = CC50/IC50) of each compound. Structure–activity relationships (SAR) were proposed based on antirotavirus activity. 相似文献
6.
Federica Menichini Rosa TundisMonica R. Loizzo Marco BonesiMariangela Marrelli Giancarlo A. StattiFrancesco Menichini Filomena Conforti 《Fitoterapia》2009
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.
Yu-Mei Zhang Run-Ting Yin Rui-Rui Jia En-Hu Yang Han-Mei Xu Ning-Hua Tan 《Fitoterapia》2010,81(8):1202-1204
A new abietane diterpene, glypensin A (1) and four known compounds, 12-acetoxy-ent-labda-8(17), 13E-dien-15-oic acid (2), quercetin 3-O-α-L-arabinofuranoside (3), quercetin 3-O-β-D-galactopyranoside (4), β-sitosterol (5) were isolated from the branches and leaves of Glyptostrobus pensilis (Staut.) Koch. Their structures were determined by MS, 1D- and 2D-NMR means. Compound 1 showed cytotoxicity on human chronic myeloid leukemia cell line K562 (IC50 = 21.2 μM). 相似文献
8.
Peng F Tao Q Wu X Dou H Spencer S Mang C Xu L Sun L Zhao Y Li H Zeng S Liu G Hao X 《Fitoterapia》2012,83(3):568-585
Twenty-nine phenolic compounds were isolated from the root bark of fresh (Yunnan) ginger and their structures fully characterized. Selected compounds were divided into structural categories and twelve compounds subjected to in-vitro assays including DPPH radical scavenging, xanthine-oxidase inhibition, monoamine oxidase inhibition, rat-brain homogenate lipid peroxidation, and rat pheochromocytoma PC12 cell and primary liver cell viability to determine their antioxidant and cytoprotective properties. Isolated compounds were also tested against nine human tumor cell lines to characterize anticancer potency. Several diarylheptanoids and epoxidic diarylheptanoids were effective DPPH radical scavengers and moderately effective at inhibiting xanthine oxidase. An enone–dione analog of 6-shogaol (compound 2) was isolated and identified to be most effective at protecting PC12 cells from H2O2-induced damage. Almost all tested compounds inhibited lipid peroxidation. Three compounds, 6-shogaol, 10-gingerol and an enone-diarylheptanoid analog of curcumin (compound 6) were identified to be cytotoxic in cell lines tested, with KB and HL60 cells most susceptible to 6-shogaol and the curcumin analog with IC50 < 10 μM. QSAR analysis revealed cytotoxicity was related to compound lipophilicity and chemical reactivity. In conclusion, we observed distinct compounds in fresh ginger to have biological activities relevant in diseases associated with reactive oxygen species. 相似文献
9.
This study investigated the effect of tanshinones on rat liver microsomal CYP3A2 and 2C11 activity and explored the structure-activity relationship of tanshinones with CYP3A activity. Cryptotanshinone, tanshinone I and tanshinone IIA were competitive CYP3A2 inhibitors (Ki = 199-243 μM) and CYP2C11 inhibitors (Ki = 91-118 μM). Dihydrotanshinone was not only a noncompetitive inhibitor of CYP3A2 (Ki = 110 μM), but also a competitive CYP2C11 inhibitor (Ki = 55 μM). The structural difference between dihydrotanshinone and tanshinone I at C-15 position of furan ring resulted in the different modes of inhibition on CYP3A activity. 相似文献
10.
Nguyen Tien Dat Phung Thi Xuan Binh Le Thi Phuong Quynh Chau Van Minh Hoang Thanh Huong Jung Joon Lee 《Fitoterapia》2010,81(8):1224-1227
A phytochemical fractionation of the methanol extract of the Morus alba leaves led to the isolation of eleven flavonoids (1–11). The structure of the new 3′-geranyl-3-prenyl-2′,4′,5,7-tetrahydroxyflavone (1) was elucidated by means of spectroscopic methods. The cytotoxicity of the isolated compounds against human cervical carcinoma HeLa, human breast carcinoma MCF-7, and human hepatocarcinoma Hep3B cells was evaluated. Of note, morusin (9) was the most potent with an IC50 value of 0.64 μM against HeLa cells. 相似文献
11.
The present study examines the comparative cytotoxicity of knipholone (KP) and knipholone anthrone (KA) in leukaemic and melonocyte cancer cell lines. It was found that KA induces a rapid onset of cytotoxicity with IC50 values ranging from 0.5 to 3.3 μM. In comparison to KA, KP was 70–480-times less toxic to cancer cells. Morphological and biochemical studies revealed that the cytotoxicity of KA was coupled with a quick loss of membrane integrity leading to necrotic cell death. The study identified KA as a new class of natural potential anticancer agent with a wide range of toxicological and pharmacological implications. 相似文献
12.
Three new phenolic constituents, itolide A (1), itolide B (2), itoside P (3), and 1D-3-deoxy-3-hydroxymethyl-myo-inositol (4), which is described herein for the first time as a natural product, were isolated along with four other known compounds (5 to 8) from the methanol extract of the seeds of Itoa orientalis Hemsl by the activity-guided fractionation. Their structures were determined by spectroscopic means. Compounds 1 to 8 exhibited antifungal activities against Sclerotium rolfsii with IC50 values ranging from 60.12 to 240.00 μM and against Rhizoctonia solani with IC50 values ranging from 45.34 to 233.14 μM, respectively, and compounds 1, 2, 5 exhibited cytotoxic activity against Tn5B1-4 insect cell line with EC50 values of 203.68, 93.41 and 40.37 μM, respectively. 相似文献
13.
Yu Mei Zhang Ning Hua Tan Guang Zhi Zeng Abiodun Humphrey Adebayo Chang Jiu Ji 《Fitoterapia》2009,80(6):361-363
A new norlignan, (2R,3R,4S,5S)-2,4-bis(4-hydroxyphenyl)-3,5-dihydroxy-tetrahydropyran (1), together with 9 known compounds were isolated from the branches and leaves of Taxodium ascendens. Their structures were mainly determined on the basis of MS, IR, 1D and 2D NMR spectral evidences. Methanol extract showed inhibitory activity on carbonic anhydrase II with an IC50 value of 4.27 µg/ml, acetone extract and methanol extract inhibited activity of cathepsin B with IC50 values of 2.12 and 3.71 µg/ml, respectively. 相似文献
14.
A.A. da Silva Filho D.O. Resende M.J. Fukui F.F. Santos P.M. Pauletti W.R. Cunha M.L.A. Silva L.E. Gregrio J.K. Bastos N.P.D. Nanayakkara 《Fitoterapia》2009,80(8):478-482
Baccharis dracunculifolia (Asteraceae), the most important plant source of the Brazilian green propolis (GPE), displayed in vitro activity against Leishmania donovani, with an IC50 value of 45 µg/mL, while GPE presented an IC50 value of 49 µg/mL. Among the isolated compounds of B. dracunculifolia, ursolic acid, and hautriwaic acid lactone showed IC50 values of 3.7 µg/mL and 7.0 µg/mL, respectively. Uvaol, acacetin, and ermanin displayed moderate antileishmanial activity. Regarding the antiplasmodial assay against Plasmodium falciparum, BdE and GPE gave similar IC50 values (about 20 µg/mL), while Hautriwaic acid lactone led to an IC50 value of 0.8 µg/mL (D6 clone). 相似文献
15.
A new triterpenoid saponin, named semenoside A (1), was isolated from Semen Celosia cristatae. Its structure was elucidated on the basis of 1D, 2D NMR, HR-FAB-MS and ESI-MS techniques, and physicochemical properties. The hepatoprotective activity of semenoside A with an oral dose of 1.0, 2.0 and 4.0 mg/kg, respectively, were investigated by carbon tetrachloride (CCl4)-induced hepatotoxicity in mice. The results indicated that it had significant hepatoprotective effects (p < 0.01). 相似文献
16.
The β-carboline alkaloids of Peganum harmala L were extracted through a bioassay-guided fractionation and their antimicrobial activities were investigated. Results revealed significant differences (P > 0.05) between compounds depending on the microorganism tested and the application method. When examined individually, harmine was the most effective against Proteus vulgaris, Bacillus subtilis and Candida albicans where inhibition zones ranged between 21.2 and 24.7 mm. Potentiality of the alkaloids was increased when applied as binary mixtures suggesting a kind of synergistic interaction with inhibition zones reaching 31.5 mm with the total alkaloidal extract. We recommended the use of such compounds as new antimicrobial biorationals. 相似文献
17.
Jatropha curcas seed oil, which can be utilized for biodiesel production upon transesterification, is also rich in phorbol esters (PEs). In this study, PEs from J. curcas oil (Jatropha factors C1 and C2 (purified to homogeneity), Jatropha factors C3 and (C4 + C5) (obtained as mixtures) and PE-rich extract (containing all the above stated Jatropha factors) were investigated. The concentrations of Jatropha PEs were expressed equivalent to Jatropha factor C1. In the snail (Physa fontinalis) bioassay, the order of potency (EC50, μg/L) was: PE-rich extract < factor C3 mixture < factor C2 < factor C1 < factor (C4 + C5). In the Artemia salina bioassay, the order of potency (EC50, mg/L) was: factor C2 < factor C3 mixture < factor C1 < factor (C4 + C5) mixture. In addition, Jatropha PEs exhibited platelet aggregation (ED50, μM, factor C2 < factor C3 mixture < factor C1 < factor (C4 + C5) mixture. The stability of a PE-rich extract was evaluated and found to be low at room temperature but favourable in ethanol over a range of temperatures. By integrating the isolation methodology developed in this study in the Jatropha biodiesel industry, PEs could be obtained as value-added co-products. 相似文献
18.
The present study was aimed to investigate the possible interaction of the standardized extract of Acorus calamus (AC) with Cytochrome P450 enzyme, quantitative determination of the α-asarone in the AC rhizome was performed by RP-HPLC method. In vitro interaction of the plant extract was evaluated by CYP450-carbon monoxide complex (CYP450-CO) assay. Effect on individual isoforms such as CYP3A4 and CYP2D6 isozymes were analyzed through fluorescence product formation and respective IC50 values were determined. CYP450-CO assay showed moderate interaction potential. Extract showed higher IC50 values (46.84 ± 1.83-32.99 ± 2.21 μg/ml) comparing to the standard inhibitors and lower IC50 value than α-asarone (65.16 ± 2.37-42.15 ± 2.45 μg/ml). 相似文献
19.
Fraternale D Sosa S Ricci D Genovese S Messina F Tomasini S Montanari F Marcotullio MC 《Fitoterapia》2011,82(4):654-661
The topical anti-inflammatory, free radical scavenging and antifungal activities of essential oils and extracts of Commiphora erythraea (Ehrenb.) Engl. resin were investigated. The hexane extract significantly inhibited oedema when applied topically in Croton oil-induced ear oedema assay in mice. The same extract showed antioxidant activity in DPPH radical scavenging assay. A bioguided separation of the hexane extract led to the isolation of furanosesquiterpenoids 1 and 2 that showed a weak antifungal activity, while compounds 3-5 resulted to be antioxidant (EC50 4.28, 2.56 and 1.08 mg/mL, respectively) and anti-inflammatory (30, 26 and 32% oedema reduction, respectively). 相似文献
20.
Illicium verum is a well known spice in traditional Indian system for its therapeutic potential. The present study was aimed to evaluate the acetylcholinesterase (AChE) and butyrylcholinesterase inhibitory (BChE) activity of standardized extracts of I. verum and its oil. Present study confirmed that anethole contributed to the anticholinesterase activity of I. verum, with more specificity towards AChE. IC50 for AChE and BChE inhibitory activity of anethole was 39.89 ± 0.32 μg/mL and 75.35 ± 1.47 μg/mL, whereas for the oil, 36.00 ± 0.44 μg/mL and 70.65 ± 0.96 μg/mL respectively. Therefore I. verum can be a good lead as anti-cholinesterase agent from natural resources. 相似文献