Constituents of Croton crassifolius roots.
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Biomedical subjects
Publications and source records attributed to N R Farnsworth.
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Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonstrated an ED50 of 8.5 micrograms/mL was isolated. On the basis of spectral analysis and chemical correlation with zeorin, the structure was shown to be 6 6 alpha-hydroxy-A'-neogermmacer-22(29)-en-30-oic acid (missourin).
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Several quassinoids, obtained by isolation and derivatization from Simaba multiflora and Soulamea soulameoides, were evaluated for growth inhibitory and insecticidal effects against the tobacco budworm (Heliothis virescens) and for antifeedant effects against H. virescens and the fall armyworm (Spodoptera frugiperda). The relative activity of the quassinoids as insect growth inhibitors generally paralleled their known relative potency as antileukemic and cytotoxic agents.
As part of a continuing effort to provide novel agents of potential value in cancer chemotherapy, 2-hydroxy-3-octadecyl-5-methoxy-1,4-benzoquinone (irisoquin) was identified as a component of Iris missouriensis. This novel species demonstrated cytotoxic activity with cultured KB and P-388 cells (ED50 = 1.8 and 0.03 microgram/mL, respectively). The structure was assigned on the basis of spectral analyses and The structure was assigned on the basis of spectral analyses and confirmed by chemical synthesis. The latter provides a facile method for the production of irisoquin and structural derivatives that may be of value for the examination of structure-activity relationships. A closely related compound, 3-octadecyl-5-methoxy-1,4-benzoquinone (deoxyirisoquin), was also isolated from Iris missouriensis, prepared synthetically, and found to be devoid of cytotoxic activity.
Research in natural products, not unlike many other fields of investigation, requires access to large amounts of prior experimental data relevant to specific projects. The most efficient method of identifying and analyzing these data currently employs computer handling of the information. The NAPRALERT database has been designed to meet this need relevant to the development of natural products. It has also been designed, through analysis of existing literature and its contained data, to provide a means to predictively identify taxonomic sources most promising from specific biological activities.
One of the prerequisites for the success of primary health care is the availability and use of suitable drugs. Plants have always been a common source of medicaments, either in the form of traditional preparations or as pure active principles. It is thus reasonable for decision-makers to identify locally available plants or plant extracts that could usefully be added to the national list of drugs, or that could even replace some pharmaceutical preparations that need to be purchased and imported. This update article presents a list of plant-derived drugs, with the names of the plant sources, and their actions or uses in therapy.
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Isocucurbitacin B (I), 3-epi-isocucurbitacin B (II), and cucurbitacin B (III) were identified as the principal cytotoxic constituents of Ipomopsis aggregata (Pursh) V. Grant (Polemoniaceae). The structure of the new compound, II, was determined through analysis of its spectrometric characteristics.
Extracts of the fruit of Phytolacca dodecandra (endod) demonstrate molluscicidal and other biological activities. Since this plant is indigenous to some countries where schistosomiasis is a common problem, it has been proposed that it may be socioeconomically feasible to employ endod as an aid in the control of this disease through its use to control the snail vector. As an initial step in the safety assessment of this substance, its mutagenic potential was determined utilizing Salmonella typhimurium strain TM677. The seeds and fruit of Phytolacca americana, also molluscicidal, were additionally evaluated for mutagenic potential. Using a variety of conditions, no mutagenic activity could be demonstrated for any of the extracts tested. Thus, subject to the results of future safety assessment, endod remains a viable candidate as a useful molluscicide.
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Two antileukemic daphnane esters, Pimelea factor P2 (I) and the new compound dircin (II), were isolated from the twigs and flowers of Dirca occidentalis A. Gray (Thymelaeaceae). Three lignans, (-)-medioresinol (III), (+)-syringaresinol (IV), and (-)-lariciresinol (V), as well as the coumarin daphnoretin (VI), were found to be additional cytotoxic constitents of this taxon.
Caraipa densifolia Mart. (Clusiaceae) has afforded the new lupene derivative 3 beta-hydroxy-28-p-coumarolyoxy-lup-20(29)-en-27-oic acid (8), whose structure was deduced by chemical correlation with betulin (6). Simiarenol (1), taraxerone (2), friedelin (3), lupeol (4), betulinic acid (5), betulin (6), and beta-sitosterol-beta-D-glucoside (7) were also isolated in this study.
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