High-throughput screening identifies established drugs as SARS-CoV-2 PLpro inhibitors

A new coronavirus (SARS-CoV-2) has been identified as the etiologic agent for the COVID-19 outbreak. Currently, effective treatment options remain very limited for this disease; therefore, there is an urgent need to identify new anti-COVID-19 agents. In this study, we screened over 6,000 compounds that included approved drugs, drug candidates in clinical trials, and pharmacologically active compounds to identify leads that target the SARS-CoV-2 papain-like protease (PLpro). Together with main protease (M

Effects of cryptotanshinone on proliferation and apoptosis of Hela cell line of cervical cancer / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the proliferation effects and apoptosis induction of cryptotanshinone on Hela cell line of cervical cancer.</p><p><b>METHOD</b>The MTT assay was used to detect the growth inhibition rates of Hela cells at 24, 48, 72 h which cultured with cryptotanshinone in different concentrations. The cell cycle distribution and apoptosis were measured by flow cytometry. The protein expressions of E6, p53 and p21 were studied by Western blot.</p><p><b>RESULT</b>The different concentrations (0.5-16 mg x L(-1)) of cryptotanshinone had cytotoxicity on Hela cells, which were clearly dose and time-dependent. The IC50 of 24, 48, 72 h were 17.8, 8.17, 6.55 mg x L(-1), respectively. Cells were treated with cryptotanshinone which had significant effects on cell cycle of Hela cell, and induced apoptosis. Western blot showed cryptotanshinone decreased expressions of HPV E6 and increased expressions of p53 and p21 proteins.</p><p><b>CONCLUSION</b>Cryptotanshinone had significant cytotoic and radiosensitization effects on cervical cancer Hela cells. One of the mechanism may be that it might make significant G0/G1 phase arrest and induced apoptosis, a decrease in S phase, and restore the function of p53 to induce apoptosis in Hela cells to kill the tumor cell.</p>

Chemical constituents and bioactivity of Kalimeris indica / 中国中药杂志

<p><b>OBJECTIVE</b>To study the constituents of Kalimeris indica and its bioactivity.</p><p><b>METHOD</b>The constituents were isolated by various chromatographic techniques and their structures were elucidated by their physicochemical properties and the spectral data analysis. Use the disk diffusion method, see whether a sample can produce inhibition zone and its round size, semi-quantitatively evaluate the samples antimicrobial activity.</p><p><b>RESULT</b>Eight compounds were isolated and identified as succinic acid (1), glycerolmonopalmitate (2), protocatechuic acid (3), uracil (4), syringic acid (5), protocatechuic acid methyl ester (6), esculetin (7), medicagenic acid (8). The result of activity screening indicate that succinic and syringic acid have bacteriostasis to bacillus subtilis.</p><p><b>CONCLUSION</b>All Compounds were isolated from the genus Kalimeris for the first time, succinic acid (1) and syringic acid (5) have bacteriostasis to bacillus subtilis.</p>

Triterpenes from Kalimeris indica / 中国中药杂志

<p><b>OBJECTIVE</b>To study the constituents of Kalimeris indica.</p><p><b>METHOD</b>The constituents were isolated by various chromatographic techniques and their structures were elucidated by their physicochemical properties and the spectral data analysis.</p><p><b>RESULT</b>Eleven compounds were isolated and identified as dammaradienyl acetate(1), friedelin(2), friedelinol(3), beta-amyrin(4), alpha-amyrin(5), lupenyl acetate(6), beta-sitosterol(7), alpha-spinasterol(8), alpha-spinasterone(9), stigmasterol(10), daucosterol(11).</p><p><b>CONCLUSION</b>Compounds 4-6, 8-11 were isolated from the genus Kalimeris for the first time.</p>