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In Vitro Defined

Testing or action outside an organism (e.g. inside a test tube or culture dish.)

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Sat Jul 4

  • In Vitro - Comparative SAR Evaluations of Annonaceous Acetogenins for Pesticidal Activity - McLaughlin et al - 1996: The activities of 44 Annonaceous acetogenins, which were originally isolated by monitoring plant fractionations with the brine shrimp lethality test (BST), were evaluated in the yellow fever mosquito larvae microtiter plate (YFM) assay. The results clearly demonstrate that most acetogenins have pesticidal properties. The structure-acti vity relationships indicate that the compounds bearing adjacent bis-THF (tetrahydrofur an) rings with three hydroxyl groups are the most potent. Bullatacin (1) and trilobin (7) gave the best activities against YFM with LC50 values of 0·10 and 0·67 mg litre-1, respectively. Compounds showing LC50 values below 1·0 mg litre-1 in this assay are usually considered significant as new lead candidates for pesticidal development. In the BST, the corresponding LC50 values were 1·6×10-3 (1) and 9·7×10-3 (7) mg litre-1. Annonaceous acetogenins are known to act, at least in part, as potent inhibitors of mitochondrial NADH: ubiquinone oxidoreductase . © of SCI.
  • In Vitro - Isolation of new bioactive annonaceous acetogenins from Rollinia mucosa via LC/MS - McLaughlin et al. - 1997: Reversed-phase high-performan ce liquid chromatography (RP-HPLC) fractionation, monitored by liquid chromatography /electrospray mass spectrometry (LC/ESI-MS), led to the isolation of two new bioactive annonaceous acetogenins, rollidecin C (1) and rollidecin D (2), from the bioactive aqueous methanol fraction of the leaves of Rollinia mucosa (Annonaceae). The structures were confirmed by analyses of the 1H and 13C NMR data. In addition, a known adjacent bis-tetrahydro furan (THF) acetogenin, desacetyluvari cin (3), was isolated from this plant for the first time utilizing the LC/ESI-MS monitoring approach. Compound 1 exhibited selective cytotoxicity toward the colon tumor cell line (HT-29), while 2 showed only borderline cytotoxicity in a panel of six human tumor cell lines.

Thu Jun 25

Wed Jun 17

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Tue Jun 16

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Sat May 16

Sun May 3

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