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Diarylheptanoids, potential therapeutic agents and dietary supplements, are the main active compounds in the genus Curcuma, however, determination of the absolute configurations of the flexible polyhydric main chains in linear diarylheptanoids is still a challenge. In this study, an exploration of the phytochemical constituents of Curcuma phaeocaulis led to the isolation of eight novel linear diarylheptanoids (1–8). Enzymatic hydrolysis, preparation of acetonide derivatives, preparation of MTPA esters, and electronic circular dichroism calculations were comprehensively performed in order to determine their absolute configurations. In in vitro assays, compounds 2, 3, and 6 exhibited anti-angiogenic activities, and compounds 2, 3, and their aglycones inhibited the proliferation of HepG2 cells. These findings suggest that diarylheptanoid glucosides of C. phaeocaulis may be useful for suppression of hepatoma growth and metastasis.

Diarylheptanoids, potential therapeutic agents and dietary supplements, are the main active compounds in the genus Curcuma , however, determination of the absolute configurations of the flexible polyhydric main chains in linear diarylheptanoids is still a challenge. In this study, an exploration of the phytochemical constituents of Curcuma phaeocaulis led to the isolation of eight novel linear diarylheptanoids (1 – 8). Enzymatic hydrolysis, preparation of acetonide derivatives, preparation of MTPA esters, and electronic circular dichroism calculations were comprehensively performed in order to determine their absolute configurations. In in vitro assays, compounds 2 , 3 , and 6 exhibited anti-angiogenic activities, and compounds 2 , 3 , and their aglycones inhibited the proliferation of HepG2 cells. These findings suggest that diarylheptanoid glucosides of C. phaeocaulis may be useful for suppression of hepatoma growth and metastasis. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • One known and three novel glycoalkaloids were isolated from Solanum lyratum Thunb. • Tumor-derived vascular endothelial cells (Td-ECs) obtained from a co-culture system were used in this study. • Four compounds isolated from S. lyratum Thunb. indicated anti-angiogenic activities. Abstract We previously identified alkaloids as being the main antitumor constituents of Solanum lyratum Thunb. In this follow-up study to identify the specific active principles, three new glycoalkaloids (1 – 3) were isolated from S. lyratum with one known glycoalkaloid (4). The structures of the four compounds were determined by means of integrated spectroscopic techniques, as well as by comparison with those in literature. Furthermore, the effects of compounds 1 – 4 were investigated on repressed migration, invasion, and tube formation in vitro in tumor-derived vascular endothelial cells (Td-ECs) from a co-culture system established in the presence or absence of vascular endothelial growth factor (VEGF) at safe concentrations selected using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, indicating anti-angiogenic activities. [ABSTRACT FROM AUTHOR]

Soluble O -(2-hydroxyl)propyl-3-trimethyl ammonium chitooligosaccharide chloride (HTCOSC) was covalently conjugated to the 11-amino-acid peptide derived from amino terminus of endostatin (endostatin2, ES2, IVRRADRAAVP) to overcome its poor stability, low cell affinity and instable activity. Nuclear magnetic resonance spectroscopy and mass spectrometry was used to study the structure and molecular weight information. The anti-angiogenic activities were evaluated using cell counting Kit-8 assay, flow cytometry assay, wounding migration assay, transwell migration assay, chicken chorioallantoic membrane (CAM) assay and zebra fish angiogenesis assay. In contrast with ES2, the novel carbohydrate-polymer HTCOSC-ES2 displayed improved heat stability, higher cell affinity, better inhibition on endothelial cell proliferation, tube formation, 2-dimensional and 3-dimensional migration in vitro . According to the evaluation in CAM and zebra fish, HTCOSC-ES2 also displayed better anti-angiogenic activity than ES2 in vivo . These results indicate that HTCOSC has good properties as potential candidate for protein/peptide modifier and HTCOSC-ES2 has good potential in angiogenesis related diseases treatment. [ABSTRACT FROM AUTHOR]

Abstract: The paper reports the preparation, characterization and potential biological activities of a chemically sulfated polysaccharide isolated from Phellinus ribis. Four sulfated derivatives (PRP-SI–IV) with variable degrees of substitution were obtained by the chlorosulfonic acid method, without degradation of the polysaccharide (PRP). The sulfate groups were not regularly distributed along the polysaccharide chain with a multiple substitution pattern as determined by 13C NMR. The sulfated derivatives except for PRP-SI showed significant inhibition effects on HepG2 cells in comparison with the native non-sulfated polysaccharide (PRP). All sulfated derivatives could block new angiogenic vessel formation in zebrafish assay, however, the effects were less than PRP. [Copyright &y& Elsevier]