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Phytochemical investigation on the stems of Schisandra glaucescens resulted into the isolation of three new lanostane triterpenoids, 12-hydroxyschiglausin B (1), 12-hydroxykadsuphilactone B (2), and 20R-hydroxyschinalactone C (3). Structural elucidation of all the compounds was accomplished by spectral methods. The isolated compounds were tested in vitro for cytotoxic activities. As a result, triterpenoids 1 and 2 showed cytotoxic activities for all six tested tumor cell lines with IC50 values less than 15 μM. [ABSTRACT FROM AUTHOR]

Two new C28 sterols with a cyclopentane ring at C-22 and 26, alkesterol A (1) and alkesterol B (2), along with β-sitosterol (3), were isolated from the berries of Physalis pubeacens L. (cape gooseberry). The structures of the new compounds were established by HR-EI-MS, 1D and 2D (1H-1H COSY, HSQC, HMBC) NMR experiments. The known compound was identified by comparison of spectral data with published references. The two new compounds showed some cytotoxic activities by MTT assay. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance: Lysimachia clethroides Duby is a traditional Chinese medicinal herb has been used in China to treat edema, jaundice diseases, hepatitis, tumor and inflammations, but the anti-tumor mechanisms are unclear. Aim of the study: The present study was undertaken to investigate if total flavonoids from Lysimachia clethroides Duby (ZE4) possesses anti-cancer effects through apoptotic pathways in human chronic myeloid leukemia K562 cells. Materials and methods: K562 cells were treated with different concentrations of ZE4 at different time intervals. Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cell apoptosis was assessed by flow cytometry, Hoechst 33258 staining and COMET assay. Western blot analysis was used to detect Bcl-2, Trail and DR5 expressions. Results: 15 flavonoids were isolated and identified from ZE4. ZE4 could inhibit the growth of K562 cells significantly by induction of apoptosis. Marked morphological changes of apoptosis, DNA fragmentation and single DNA strand breakages were observed clearly after treatment of ZE4. Bcl-2 expression was down-regulated remarkably while Fas, Trail and DR5 up-regulated when apoptosis occurred. Conclusions: This result suggests that total flavonoids of Lysimachia clethroides Duby exert potential anti-cancer activity through growth inhibition and apoptosis in K562 cells. [Copyright &y& Elsevier]

Eight new iridoids (1–8) and an ionone glucoside (9), together with 31 known compounds (10–40), were isolated from the whole plants of Rehmannia henryi. The structures of these compounds were elucidated on the basis of their spectroscopic data and chemical evidence. [ABSTRACT FROM AUTHOR]

Camellia oleifera C. Abel has been widely cultivated in China, and a group of bioactive constituents such as triterpeniod saponin have been isolated from C. oleifera C. Abel. In the current study, a new triterpeniod saponin was isolated from the EtOH extract of the roots of C. oleifera C. Abel, named as oleiferoside W, and the cytotoxic properties of oleiferoside W were evaluated in non-small cell lung cancer A549 cells. At the same time the inducing apoptosis, the depolarization of mitochondrial membrane potential (Δψ), the up-regulation of related pro-apoptotic proteins, such as cleaved-PARP, cleaved-caspase-3, and the down-regulation of anti-apoptotic marker Bcl-2/Bax were measured on oleiferoside W. Furthermore, the function, inducing the generation of reactive oxygen species (ROS) and apoptosis, of oleiferoside W could be reversed by N-acetylcysteine (NAC). In conclusion, our findings showed that oleiferoside W induced apoptosis involving mitochondrial pathway and increasing intracellular ROS production in the A549 cells, suggesting that oleiferoside W may have the possibility to be a useful anticancer agent for therapy in lung cancer. [ABSTRACT FROM AUTHOR]

Abstract: In this study, an effective Escherichia coli expression system was used to study the role of residues in the antitumor-analgesic peptide from Chinese scorpion Buthus martensii Karsch (BmKAGAP). To evaluate the extent to which residues of the toxin core contribute to its analgesic activity, nine mutants of BmKAGAP were obtained by PCR. Using site-directed mutagenesis, all of these residues were individually substituted by one amino acid. These were then subjected to a circular dichroism analysis, and an analgesic activity assay in mice. This study represents a thorough mapping and elucidation of the epitopes that underlie the molecular basis of the analgesic activity. The three-dimensional structure of BmKAGAP was established by homology modeling. Our results revealed large mutant-dependent differences that indicated important roles for the studied residues. With our ongoing efforts for establishing the structure and analgesic activity relationship of BmKAGAP, we have succeeded in pinpointing which residues are important for the analgesic activity. [Copyright &y& Elsevier]