Antiproliferation and cell apoptosis inducing bioactivities of constituents from Dysosma versipellis in PC3 and Bcap-37 cell lines

<p>Abstract</p> <p>Background</p> <p>Recently, interest in phytochemicals from traditional Chinese medicinal herbs with the capability to inhibit cancer cells growth and proliferation has been growing rapidly due to their nontoxic nature. <it>Dysosma versipellis </it>as Bereridaceae plants is an endemic species in China, which has been proved to be an important Chinese herbal medicine because of its biological activity. However, systematic and comprehensive studies on the phytochemicals from <it>Dysosma versipellis </it>and their bioactivity are limited.</p> <p>Results</p> <p>Fifteen compounds were isolated and characterized from the roots of <it>Dysosma versipellis</it>, among which six compounds were isolated from this plant for the first time. The inhibitory activities of these compounds were investigated on tumor cells PC3, Bcap-37 and BGC-823 <it>in vitro </it>by MTT method, and the results showed that podophyllotoxone (PTO) and 4'-demethyldeoxypodophyllotoxin (DDPT) had potent inhibitory activities against the growth of human carcinoma cell lines. Subsequent fluorescence staining and flow cytometry analysis indicated that these two compounds could induce apoptosis in PC3 and Bcap-37 cells, and the apoptosis ratios reached the peak (12.0% and 14.1%) after 72 h of treatment at 20 <it>μ</it>M, respectively.</p> <p>Conclusions</p> <p>This study suggests that most of the compounds from the roots of <it>D. versipellis </it>could inhibit the growth of human carcinoma cells. In addition, PTO and DDPT could induce apoptosis of tumor cells.</p

Antiviral Activity and Mechanism of Action of Novel Thiourea Containing Chiral Phosphonate on Tobacco Mosaic Virus

Using half-leaf method O,O’-diisopropyl (3-(L-1-(benzylamino)-1-oxo-3-phenylpropan-2-yl)thioureido)(phenyl)methyl phosphonate (2009104) was studied for its activity on tobacco mosaic virus (TMV). It showed good curative activity in vivo and the curative activity at 500 μg/mL was found to be 53.3%. In vivo treatment with the control agent Ningnanmycin at 500 μg/mL resulted in 51.2% inhibition and curative inhibition rates respectively. Dot-ELISA test was employed to verify the efficacy of activity of compound 200910 for anti-TMV activity. The mechanism of action of compound 2009104 to resist TMV was also studied. The results showed that the resistance enzymes PAL, POD, SOD activity and chlorophyll content after TMV inoculation K326 (Nicotiana tabacum K326) of tobacco plants followed by treatment with compound 2009104 were significantly enhanced. The study of the effect of compound 2009104 on TMV capsid protein (CP) showed that it inhibited the polymerization process of TMV-CP in vitro

Inorganic base-catalyzed formation of antivirally active <it>N</it>-substituted benzamides from α-amido sulfones and <it>N</it>-nucleophile

Abstract Background Heteronucleophiles as well as carbanionic reagents can be used to react with α-amido sulfones, thus giving the opportunity to prepare a large array of amino derivatives. Since, novel 1,3,4-oxadiazole-2-thiol derivatives can serve as potent nucleophiles, we employed 5-subsititued phenyl-1,3,4-oxadiazole-2-thiols as the nucleophilic source of nitrogen in the reaction with α-amido sulfones. Results A series of N-substituted benzamides bearing 1,3,4-oxadiazol unit were prepared for the first time by the reaction of in situ generated protected imine from α-amido sulfones with 5-subsititued phenyl-1,3,4-oxadiazole-2-thiols as the source of nitrogen nucleophile. Some of the synthesized products displayed favourable antiviral activity against cucumber mosaic virus (CMV) in preliminary antiviral activity tests. The title compounds 5c, 5o and 5r revealed curative activity of 42.2%, 48.7% and 40.5%, respectively against CMV (inhibitory rate) compared to the commercial standard Ningnanmycin (53.4%) at 500 μg/mL. Conclusion A practical synthetic route to N-benzoyl-α-amido sulfones by the reaction of 5-subsititued phenyl-1,3,4-oxadiazole-2-thiols as the source of nitrogen nucleophiles with in situ generated protected imine from N-benzoyl-α-amido sulfones is presented. The reaction catalyzed by an inorganic base has considerable significance to exploit the potential of α-amido sulfones in organic synthesis.</p

A facile and feasible method to evaluate and control the quality of Jatropha curcus L. seed oil for biodiesel feedstock: Gas chromatographic fingerprint

To establish a facile and feasible method to evaluate and control the quality of Jatropha curcus L. seed oil for biodiesel feedstock, Gas chromatographic (GC) fingerprint technology was introduced and employed. Initially, the chromatograms of the 13 oil samples from various plantation zones in Guizhou, China were obtained under optimized GC conditions. Ten common peaks were selected as the characteristic peaks for chemometrics, seven of which were identified and quantified by comparing with the standards. The mean chromatogram of S7 (n = 3) was selected as the reference spectrum for similarity analysis based on the influence of the fatty acid composition of the raw material on the fuel properties of resulting biodiesel. Furthermore, the result of SA was confirmed by hierarchical clustering analysis and principal component analysis. By this method, all samples can be classified into three groups. The similarity value of samples approaching 1.000 compared with sample 7 was indicative of the desired fuel properties of biodiesel, indicating the potential practical applications in the quality evaluation and control of biodiesel feedstock.Jatropha curcus L. seed oil Biodiesel Gas chromatographic fingerprint technology Quality

Asymmetric Synthesis of α-Aminophosphonates Using the Inexpensive Chiral Catalyst 1,1’-Binaphthol Phosphate

molecule

Synthesis and Antiviral Activity of 5‑(4‑Chlorophenyl)-1,3,4-Thiadiazole Sulfonamides

Starting from 4-chlorobenzoic acid, 10 new 5-(4-chlorophenyl)-N-substituted-N-1,3,4-thiadiazole-2-sulfonamide derivatives were synthesized in six-steps. Esterification of 4-chlorobenzoic acid with methanol and subsequent hydrazination, salt formation and cyclization afforded 5-(4-chlorophen-yl)-1,3,4-thiadiazole-2-thiol (5). Conversion of this intermediate into sulfonyl chloride 6, followed by nucleophilic attack of the amines gave the title sulfonamides 7a-7j whose structures were confirmed by NMR, IR and elemental analysis. The bioassay tests showed that compounds 7b and 7i possessed certain anti-tobacco mosaic virus activity