Eight new compounds, including four flavaglines (1 – 4) and four triterpenoids (5 – 8), together with 16 known compounds, were isolated from Aglaia perviridis collected in Vietnam. The new compounds 2 – 4 and seven known rocaglate derivatives (9 – 15) exhibited significant cytotoxicity against the HT-29 cell line. The cytotoxic compounds were further evaluated against a normal colon cell line, CCD-112CoN. In addition, the new compound perviridicin B (2) and four known compounds (9, 11, 12 and 17), showed significant NF-κB (p65) inhibitory activity in an ELISA assay.
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
The genus Cryptocarya belongs to the pantropical family Lauraceae, of which several species grow in Pacific Rim tropical rainforests. Previous studies have shown that cryptocaryone is the main cytotoxic compound of species of this genus, but a detailed phytochemical investigation about Cryptocarya rubra has not been reported. As an extension of a search for new natural product anticancer agents from diverse organisms, a small-scale sample of a dichloromethane partition of a methanol-soluble extract of C. rubra, collected in Hawaii, was found to be cytotoxic toward the HT-29 human colon cancer cell line and was selected as a lead. This extract repository was donated to IHVR by Merck Research Laboratories, Rahway, NJ. Using column chromatography guided by cytotoxicity to HT-29 cells, cryptocaryone and several new and known analogues, including cryptocaryanones A and B and bicaryanone A, were isolated. The structures of all isolates were established from their IR, UV, NMR, and mass spectra, and their absolute configurations were determined by analysis of their CD spectra and supported by the relative configuration determination of cryptocaryanones A and B using single-crystal X-ray diffraction. All isolates have been evaluated for their cytotoxicity against HT-29 cells, and several compounds were found to be active, with cryptocaryone (IC50, 0.32µM) being the most potently cytotoxic compound.
Indigofera spicata Forssk. (Leguminosae) has become widespread in tropical and sub-tropical countries as a ground cover plant. In the present investigation, the bioactivity-guided fractionation of a cytotoxic chloroform extract of the flowers, fruits, leaves, and twigs of I. spicata, collected in Vietnam, using the HT-29 human colon cancer, 697 human acute lymphoblastic leukemia, and the Raji human Burkitt's lymphoma cell lines, led to the isolation of seven compounds. Of the isolates, (+)-10-deacetyl-purpurin and (2S)-2,3-dihydrotephroglabrin are new compounds. The compounds, cis-(6aβ,12aβ)-hydroxyrotenone and rotenone, exhibit potent cytotoxicity for 697 and HT-29 cells with IC50 values of less than 1µM. Tephrosin was found to be cytotoxic and cytostatic for 697 cells. Compounds were also tested in a quinone reductase induction assay with tephrosin showing a CD value of 0.4µM. (Support in part by grant P01 CA125066 from the National Cancer Institute, NIH, Bethesda, MD, is acknowledged).
One compounds were isolated from the fruiting body of Ganoderma lucidum. Basis on chemical evidences and spectral analysis (MS, UV, IR, 1HNMR, 13CNMR), its structures were deduced as ergosta-7,22 E-dien-3-one.
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
C. macrocarpa and C. madagascariensis and C. fragrans (Cannelaceae) are endemic medicinal plants of Madagascar widely prescribed for many ailments. Our previous study demonstrated that their major drimane-type sesquiterpene constituents: capsicodendrin (1) and cinnamodial (2) display potent antiproliferative activity against murine leukemia (L1210/0, IC50 1.21, 0.58µM, respectively) and two human T-lymphocyte cell lines (Molt4/C8, IC50 0.94, 1.51µM, respectively and CEM/0, IC50 0.86, 1.61µM, respectively). To complete the bioactivity data of these compounds, we have recently evaluated compounds 1 and 2 together with other sesquiterpene-type drimanes isolated from the three plants and their chemical derivatives, against colon (HT-29), breast (MCF-7) and HeLa cancer cell lines. Our results showed that 1 and 2 together with cinnamosmolide (3) displayed strong antiproliferative activity against colon cancer (HT-29) cell line with IC50 values ranging from 0.64, 0.6 and 0.9µM, respectively. Several derivatives have been prepared for structure-antiproliferative study and the SAR of the natural products and their derivatives will be presented.
The genus Phyllanthus is a large plant group containing over 600 species, of which many have been used in traditional medicine to treat human diseases and have been studied phytochemically. However, there are no previous reports on the chemical constituents of Phyllanthus songboiensis N. N. Thin (Phyllanthaceae). As part of a search for new natural product anticancer agents from diverse organisms, the aerial parts of P. songboiensis, collected in Vietnam, were found to be cytotoxic toward the HT-29 human colon cancer cell line. Using column chromatography guided by cytotoxicity to HT-29 cells, a new dichapetalin-type triterpenoid, a new dibenzylbutyrolactone-type lignan, and several known compounds were isolated from this plant. The structures of all compounds isolated were established from their IR, UV, NMR, and mass spectra, and the absolute configurations of these compounds were determined by analysis of their CD spectra. The cytotoxicity toward HT-29 cells of all isolates and the natural killer (NK) cell stimulation of some compounds were tested. Several compounds showed cytotoxicity toward HT-29 cells, and a sterol glycoside was found to stimulate NK cells in the presence of interleukin-12. This study describes for the first time the cancer cell cytotoxic and NK cell stimulatory constituents of Phyllanthus songboiensis.
'%3e%3cpath fill='%23012169' d='M0 0v30h60V0z'/%3e%3cpath stroke='%23fff' stroke-width='6' d='m0 0 60 30m0-30L0 30'/%3e%3cpath stroke='%23C8102E' stroke-width='4' d='m0 0 60 30m0-30L0 30' clip-path='url(%23b)'/%3e%3cpath stroke='%23fff' stroke-width='10' d='M30 0v30M0 15h60'/%3e%3cpath stroke='%23C8102E' stroke-width='6' d='M30 0v30M0 15h60'/%3e%3c/g%3e%3c/svg%3e)