| Autor: |
Jin, Shengbin, Bruhn, David F., Childs, Cynthia T., Burkman, Erica, Moreno, Yovany, Salim, Angela A., Khalil, Zeinab G., Capon, Robert J. |
| Předmět: |
|
| Zdroj: |
Antibiotics (2079-6382); Oct2024, Vol. 13 Issue 10, p989, 13p |
| Abstrakt: |
An investigation of ×19 soil samples collected under the auspices of the Australian citizen science initiative, Soils for Science, returned ×559 chemically dereplicated microbial isolates, of which ×54 exhibited noteworthy anthelmintic activity against either the heartworm Dirofilaria immitis microfilaria and/or the gastrointestinal parasite Haemonchus contortus L1–L3 larvae. Chemical (GNPS and UPLC-DAD) and cultivation (MATRIX) profiling prompted a detailed chemical investigation of Streptomyces sp. S4S-00196A10, which yielded new anthelmintic polyketide goondapyrones A–J (1–10), together with the known actinopyrones A (11) and C (12). Structures for 1–12 were assigned on the basis of detailed spectroscopic and chemical analysis, with preliminary structure activity relationship analysis revealing selected γ-pyrones >50-fold and >13-fold more potent than isomeric α-pyrones against D. immitis mf motility (e.g., EC50 0.05 μM for 1; EC50 2.7 μM for 5) and H. contortus L1–L3 larvae development (e.g., EC50 0.58 μM for 1; EC50 8.2 μM for 5), respectively. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
|
