A fungal strain of Aspergillus niger was recovered from sediments collected in the Northeast coast of Brazil (Pecém’s offshore port terminal). Cultivation in different growth media yielded a new ester furan derivative, 1, along with malformin A1, malformin C, cyclo (trans-4-hydroxy-L-Pro-L-Leu), cyclo (trans-4-hydroxy-L-Pro-L-Phe), cyclo (L-Pro-L-Leu), cyclo (L-Pro-L-Phe), pseurotin D, pseurotin A, chlovalicin, cyclo (L-Pro-L-Tyr) and cyclo (L-Pro-L-Val). Compound 1 was cytotoxic against HCT-116 cell line, showing IC50 = 2.9 μg/mL (CI 95% from 1.8 to 4.7 μg/mL).
From roots of Hyptis martiusii Benth. two tanshinone diterpenes were isolated, the new 7β-hydroxy-11,14-dioxoabieta-8,12-diene (1) in addition to the known 7α-acetoxy-12-hydroxy- 11,14-dioxoabieta-8,12-diene (7α-acetoxyroyleanone) (2). Structures of 1 and 2 were established by spectroscopic means. The cytotoxic activity against five cancer cell lines was evaluated. Compounds 1 and 2 displayed considerable cytotoxic activity against several cancer cell lines with IC50 values in the range of 3.1 to 11.5 μg/ml and 0.9 to 7.6 μg/ml, respectively. The cytotoxic activity seemed to be related to inhibition of DNA synthesis, as revealed by the reduction of 5-bromo-2′-deoxyuridine incorporation and induction of apoptosis, as indicated by the acridine orange/ethidium bromide assay and morphological changes after 24 h of incubation in leukemic cells.
27 December 2022 in World Journal of Microbiology and Biotechnology