ABSTRACT
@#Fifty-two methyl xestospongoate analogues were designed, synthesized and evaluated for the antiproliferative activity. Starting from alkynyl methyl ester and diyne, methyl xestospongoate analogues 4(a-m)-7(a-m)were synthesized by Cadiot-Chodkiewitz coupling and Sonogashira coupling reactions. Their structures were identified by 1H NMR, 13C NMR and HREI-MS. The cytotoxic inhibiton activities in vitro of some compounds were evaluated against human cancer cells A549 and P-388 by a CCK-8 method. Among them, compound 6k exhibited potent cell growth inhibitory activity against A549 and P-388 cancer cells, with IC50 values of 9. 36 and 9. 62 μmol/L, respectively.
ABSTRACT
Eight cembrane-type diterpenoids, namely, (+)-(6)-6-hydroxyisosarcophytoxide (), (+)-(6)-6-acetoxyisosarcophytoxide (), (+)-17-hydroxyisosarcophytoxide (), sarcomililatins A-D (-), and sarcomililatol (), were isolated from the soft coral collected from Weizhou Island, Guangxi Autonomous Region, together with 2 known related analogues, (+)-isosarcophytoxide () and (+)-isosarcophine (). The structures of these compounds were elucidated by a combination of detailed spectroscopic analyses, chemical methods, and comparison with reported data. The absolute configuration of compound was established by the modified Mosher׳s method, while the absolute configurations of compounds and were assigned by electronic circular dichroism (ECD) spectroscopy and that of compound was established by time-dependent density functional theory electronic circular dichroism (TD-DFT ECD) calculation. In bioassays, compound displayed significant cytotoxicity against the human cancer cell lines human promyelocytic leukemia cells (HL-60) and human lung adenocarcinoma cells (A-549) with IC values of 0.78±0.21 and 1.26±0.80 μmol/L, respectively. Compounds and also showed moderate inhibitory effects on the TNF-induced Nuclear factor kappa B (NF-B, a therapeutical target in cancer) activation, showing IC values of 35.23±12.42 and 22.52±4.44 μmol/L, respectively.
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A bicyclic depsipeptide, chromopeptide A (1), was isolated from a deep-sea-derived bacterium Chromobacterium sp. HS-13-94. Its structure was determined by extensive spectroscopic analysis and by comparison with a related known compound. The absolute configuration of chromopeptide A was established by X-ray diffraction analysis employing graphite monochromated Mo K α radiation (λ=0.71073 Å) with small Flack parameter 0.03. Chromopeptide A suppressed the proliferation of HL-60, K-562, and Ramos cells with average IC50 values of 7.7, 7.0, and 16.5 nmol/L, respectively.
ABSTRACT
The genus Xestospongia is one of the most widespread genera of sponges, containing abundant secondary metatolites with novel structures and potent bioactivities. The main structure types of secondary metatolites found in this genus are alkaloids, quinines, terpens, steroids, lipids, polyketones, etc. These metatolites exhibit a variety of bioactivities, such as cytotoxic, antibacterial and antiviral activities. This paper reviews the progress in the chemistry and pharmacological activities of the second metabolities from sponges of Xestospongia, especially for recent five years, with the aim for further research.
ABSTRACT
Xinxiang Medical college has attempted to reform the management system,share the resource,improve the resource utilization,exceed the limits of science,modify the contents of experimental courses,construct the comprehensive contents of experimental teaching,innovate the teaching methods,pay attention to teacher training and enhance the teaching materials.Through the longtime research and practice,we have gained the significant achievements.
ABSTRACT
Object To study the chemical constituents from leaves of Diplopanax stachyathus Hand Mazz aiming at searching for bioactive natural products Methods The compounds Ⅰ-Ⅹ were isolated by a combination of Sephedex LH 20 and silica gel column chromatographies, and their structures were identified by spectral methods Results Ten known compounds were isolated from leaves of D stachyathus Their structures were identified by means of spectroscopic analysis as: ? sitosterol (Ⅰ), betulinic acid (Ⅱ), oleanolic acid (Ⅲ), ursolic acid (Ⅳ), daucossterol (Ⅴ), quercetin 3 O ? D glucopyranoside (Ⅵ), 3,3′,4′ tri O methyellagic acid (Ⅶ), 3, 3′ di O methylellagic acid 4 O ? D xylopyranoside (Ⅷ), 3′ O methylellagic acid 4 O ? D xylopyranoside (Ⅸ), and 3, 3′,4′ tri O methylellagic acid O ? D glucopyranoside (Ⅹ) Conclusion Compounds Ⅰ-Ⅵ and Ⅸ are isolated from this plant for the first time