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In the search for new anti-tumor agents with higher potency than our previously identified compound 1 (25-OH-PPD, 25-hydroxyprotopanaxadiol), 12 novel sulfamic and succinic acid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay. Results showed that compared with compound 1, compounds 2, 3, and 7 exhibited higher cytotoxic activity on A-549 and BGC-823 cell lines, together with lower toxicity in the normal cell. In particular, compound 2 exhibited the best anti-tumor activity in the in vitro assays, which may provide valuable data for the research and development of new anti-tumor agents. [ABSTRACT FROM AUTHOR]

In this study, five novel triterpenes were isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum and identified as gypensapogenin H ( 1 ), gypensapogenin I ( 2 ), gypensapogenin L ( 3 ), gypensapogenin J ( 4 ) and gypensapogenin K ( 5 ), three of which ( 1 – 3 ) possess unprecedented ring A. All the isolated compounds were evaluated for cytotoxic activities in five cell lines and all the tested compounds showed significant anti-cancer activities against a series of human cancer cell lines, while having much weaker effect on the growth of normal cell. Among them, compound 1 showed strong inhibition toward MCF-7 human breast cancer cells (IC 50 values 6.85 μM). Further mechanistic study demonstrated that compound 1 significantly induced MCF-7 cell apoptosis. Our results indicated that compound 1 may be a promising lead agent for further study. [ABSTRACT FROM AUTHOR]

Two new compounds callistephus A ( 1 ) and callistephus B ( 2 ) together with 4,6-dihydroxyphenyl-1-butanone-2- β - d -O-glucopyranoside ( 3 ), were isolated and purified from the Callistephus chinensis flower. Their structures were identified by the interpretation of spectroscopic data. X-ray crystallographic and analysis of quantum chemical ECD calculation were applied to determine the absolute configuration. Of them, callistephus A represents a rare sesquiterpene with new carbon skeleton and also its possible biogenesis was proposed. [ABSTRACT FROM AUTHOR]

Three new triterpene saponins, lobatoside O ( 1 ), actinostemmoside I ( 2 ) and actinostemmoside J ( 3 ), were isolated from the herb of Actinostemma lobatum MAXIM. Their structures were elucidated by means of extensive chemical and spectroscopic methods. In addition, cytotoxic activities toward HCT-116, HT-29, MCF-7 and A549 cell lines were tested by the MTT method. [ABSTRACT FROM AUTHOR]

In the current work, 12 novel 25-hydroxyprotopanaxadiol (25-OH-PPD) derivatives were synthesized by reacting with chloroacetyl chloride. And their in vitro antitumor activities were evaluated on six human tumor cell lines by MTT assay. The results demonstrated that, as compared with 25-OH-PPD, compounds 4 , 6 and 7 exhibited higher cytotoxic activity on all tested cell lines. Of them, compound 4 showed strongly inhibition against MCF-7, HCT-116 and Lovo cells with IC 50 values of 1.7, 1.6 and 2.1 μM, respectively. The IC 50 values of compound 6 against HCT-116 and 7 against MCF-7 were the lowest (1.2 and 1.6 μM, respectively). It was also noted that compound 4 showed a 20- to 100-fold greater growth inhibition than ginsenoside-Rg 3 (an anti-cancer regular drug in China). In conclusion, the data revealed that compounds 4 , 6 and 7 were potential candidates for anti-tumor treatment and may be useful for the development of novel antiproliferative agents. [ABSTRACT FROM AUTHOR]

Abstract: A new lignan (7R,8S,8′R)-4,4′,9-trihydroxy-7,9′-epoxy-8,8′-lignan, and three new phenolics, carayensin-A, carayensin-B, and carayensin-C, together with 13 known compounds were isolated from the shells of Carya cathayensis. Their chemical structures were established mainly by 1D and 2D NMR techniques and mass spectrometry. All the compounds were evaluated for cytotoxicity against several human tumor types including human colorectal cancer cell lines (HCT-116, HT-29), human lung cancer cell line (A549), and human breast cancer cell line (MCF-7). The compounds 1, 5, 6, and 16 are considered to be potential as antitumor agents, which could significantly inhibit the cancer cell growth in a dose-dependent manner. [Copyright &y& Elsevier]

Abstract: Four new cucurbitane-type triterpene sapogenins, compounds 1–4, together with other eight known compounds were isolated from the acid-hydrolyzed fruits extract of Momordica charantia L. Their chemical structures were established by NMR, mass spectrometry and X-ray crystallography. Compounds 1–7 and 9–12 were evaluated for their inhibitory activities toward protein tyrosine phosphatase 1B (PTP1B), a tyrosine phosphatase that has been implicated as a key target for therapy against type II diabetes. Compounds 1, 2, 4, 7 and 9 were shown inhibitory activities of 77%, 62%, 62% 60% and 68% against PTP1B, respectively. All of these tested compounds were exhibited higher PTP1B inhibition activities than that of the Na3VO4, a known PTP1B inhibitor used as positive control in present study. Structure activity relationship (SAR) analysis indicated that the inhibition activity of PTP1B was associated with the presence and number of –OH groups. [Copyright &y& Elsevier]

Highlights: [•] A series of 25-OCH3-PPD analogues incorporating fatty acids have been synthesized. [•] The longer the fatty acid chain is, the lower the antitumor activity would be. [•] Some compounds displayed potent cytotoxic activity compared with 25-OCH3-PPD. [Copyright &y& Elsevier]

Abstract: Protein tyrosine phosphatase 1B (PTP1B) is an important factor in non-insulin-dependent diabetes mellitus (type-2 diabetes), and a promising target for treatment of diabetes and obesity. Therefore, the aim of this study is to investigate the inhibitory activities of constituents (three new together with twelve known triterpenes compounds) isolated from the hydrolyzate of total saponins from Gynostemma pentaphyllum. Their structures were accomplished mainly base on the spectroscopic methods, and then were further confirmed by X-ray crystal diffraction. All the compounds were evaluated for inhibitory activity against PTP1B. Current data suggested that the compounds 1, 3, 12, 13 and 14 were considered to be potential as antidiabetic agents, in which they could significantly inhibit the PTP1B enzyme activity in a dose-dependent manner. [Copyright &y& Elsevier]

Abstract: 30 novel compounds have been synthesized from 25-hydroxyprotopanaxadiol (25-OH–PPD) and their in vitro anti-tumor activities were tested on three cancer cell lines and one normal cell line (IOSE144) by standard MTT assay. The results showed that compound 27 exhibited the best anti-tumor activity in the in vitro assays. Compounds 1, 2, 16, 17, 18, 27, 28 and 29 have better anti-tumor activities against MCF-7 and A549 cancer cell lines than 25–OH–PPD, together with low toxicity in the normal cell. The results may provide useful data for researching and developing new antitumor agents. [Copyright &y& Elsevier]