3 resultados para HALOGENATED SESQUITERPENES

em Bioline International


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The herbaceous shrub Tetradenia riparia has been traditionally used to treat inflammatory and infectious diseases. Recently, a study showed that T. riparia essential oil (TrEO) obtained in summer has antileishmanial effects, although these results could be influenced by seasonal variation. This study evaluated the activity of the TrEO obtained in different seasons against Leishmania (Leishmania) amazonensis , in vitro and in vivo. The compounds in the TrEO were analysed by gas chromatography-mass spectrometry; terpenoids were present and oxygenated sesquiterpenes were the majority compounds (55.28%). The cytotoxicity and nitric oxide (NO) production were also tested after TrEO treatment. The TrEO from all seasons showed a 50% growth inhibitory concentration for promastigotes of about 15 ng/mL; at 30 ng/mL and 3 ng/mL, the TrEO reduced intracellular amastigote infection, independently of season. The TrEO from plants harvested in summer had the highest 50% cytotoxic concentration, 1,476 ng/mL for J774.A1 macrophages, and in spring (90.94 ng/mL) for murine macrophages. NO production did not change in samples of the TrEO from different seasons. The antileishmanial effect in vivo consisted of a reduction of the parasite load in the spleen. These results suggest that the TrEO has potential effects on L. (L.) amazonensis, consonant with its traditional use to treat parasitic diseases.

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Purpose: To determine borneol and other chemical compounds of essential oil derived from the exudate of Dryobalanops aromatica aromatica in Malaysia. Methods: Exudate was collected from D. aromatica and subjected to fractional distillation to obtain essential oil. Gas chromatography-mass spectrometry (GC-MS) was performed to characterize the composition of the isolated essential oil. Results: Essential oil (7.58 %) was obtained with the highest yield (3.24 %) in the first 2 h of fractional distillation. Thirty compounds which accounted for 97.56 % of total essential oil composition were identified by GC-MS, and they include sesquiterpenes (46.87 %), monoterpenes (31.05 %), oxygenated monoterpenes (16.76 %) and oxygenated sesquiterpenes (2.13 %). Borneol (0.74 %) was also detected in the essential oil. Conclusion: Borneol and other terpenoid compounds are present in the essential oil of the exudate of D. aromatica

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Purpose: To evaluate the antibacterial and cytotoxic activities of the secondary metabolites of Lobophytum sp. Methods: Maceration with methanol: chloroform (1:1) was applied to extract the coral material. Chromatographic and spectroscopic techniques were employed for fractionation, isolation and elucidation of pure compounds. Antibacterial activities were performed by well diffusion method against three Gram-positive and four Gram-negative bacteria. Brine shrimp lethality test was employed to predict toxicity, while antitumor activity were tested by 3-(4, 5-dimethylthiazol-2-yl)-2, 5- diphenyltetrazolium bromide (MTT) method against Ehrlich carcinoma cells. Results: Four sesquiterpenes, one cembranoid type diterpenes and two steroids were isolated. 1 exhibited significant antibacterial activity against four tested bacteria (P. aeruginosa, S. aureus, S. epidermis, and S. pneumonia) with MIC value of 15 μg/mL. Moreover, 1 showed high diameter zone of inhibition ranging from 16 - 18 mm against test bacteria. Compounds 4 and 5 displayed moderate antibacterial activity against all test bacteria with inhibition zone diameter (IZD) ranging from 11 – 15 mm and MIC values of 30 μg/mL. 2, 3, 6 and 7 exhibited weak antibacterial activity (IZD, 7 - 11 mm; MIC ≥ 30 μg/mL). In addition, only diterpene compound (4) showed high toxicity against A. Salina and antitumor activity against Erhlich carcinoma cells with the LD50 of 25 and 50 μg/mL, respectively. Conclusion: This study reveals the strong antibacterial activity of sesquiterpene alismol (1) and the potential antibacterial and antitumor activity of cembranoid type diterpene, cembrene A (4).