Four new depsidones, mollicellins O–R (compounds 1–4), along with three known compounds 5–7, were isolated from cultures of the fungus Chaetomium sp. Eef-10, an endophyte isolated from Eucalyptus exserta. The structures of the new compounds were elucidated by analysis of the 1D and 2D NMR and HR-ESI-MS spectra. The known compounds were identified by comparison of their spectral data with published values. Compounds 1–7 were evaluated for antibacterial activities against Staphylococcus aureus (sensitive and resistant strains), Escherichia coli, Agrobacterium tumefaciens, Salmonella typhimurium, Pseudomonas lachrymans, Ralstonia solanacearum, Xanthomonas vesicatoria and cytotoxic activities against two human cancer cell lines (HepG2 and Hela). Mollicellin H (6) displayed best antibacterial activity, with IC50 values of 5.14 µg/mL against S. aureus ATCC29213 and 6.21 µg/mL against S. aureus N50, MRSA, respectively. Mollicellin O (1) and mollicellin I (7) also exhibited antibacterial activities against S. aureus ATCC29213 and S. aureus N50. Mollicellin G (5) was active against both two human cancer cell lines, with IC50 values of 19.64 and 13.97 µg/mL while compounds 6 and 7 only showed cytotoxic activity against one cell line. In addition, mollicellin O (1) showed antioxidant activity based on DPPH radical scavenging, with an IC50 value of 71.92 µg/mL.
The striking rise of methicillin-resistant Staphylococcus aureus (MRSA) infections has become a serious threat to public health worldwide. In an effort to search for new anti-MRSA agents from natural products, a bioassay-guided phytochemical study was conducted on the semi-mangrove plant Myoporum bontioides A. Gray, which led to the isolation of two new sesquiterpene alkaloids (1 and 2) and six known furanosesquiterpenes (3–8). Their structures were elucidated on the basis of extensive analysis of their 1D, 2D NMR and mass spectroscopic data. These two new alkaloids (1 and 2) displayed potent anti-MRSA activity with MIC value of 6.25 μg/mL. This is the first report of sesquiterpene alkaloids from the plants of Myoporum genus and their anti-MRSA activity.
Ten pentacyclic triterpenoids including a new multiflorane triterpene acid, 2α,3β,23-trihydroxymultiflor-7-en-28-oic acid (1), and a new lupane triterpene monoglucoside named akebiaoside C (2), were obtained from the leaves ofAkebia trifoliata.
Eight thymol derivatives including three new ones (1–3) were obtained from the aerial parts of Ageratina adenophora, with most of them, in particular 1 and 5, showing notable in vitro antimicrobial and cytotoxic activity.
Four new germacrane sesquiterpene dilactones, 2β-hydroxyl-11β,13-dihydrodeoxymikanolide (1), 3β-hydroxyl-11β,13-dihydrodeoxymikanolide (2), 1α,3β-dihydroxy-4,9-germacradiene-12,8:15,6-diolide (3), and (11β,13-dihydrodeoxymikanolide-13-yl)-adenine (4), together with five known ones (5–9) were isolated from the aerial parts of Mikania micrantha. Their structures were elucidated on the basis of extensive spectroscopic analysis. Compound 4 is featured with an adenine moiety in the molecule, which is the first nitrogen-containing sesquiterpenoid so far isolated from this plant species. These compounds were evaluated for their in vitro antibacterial activity against four Gram-(+) bacteria of Staphyloccocus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), Bacillus cereus (BC) and Curtobacterium. flaccumfaciens (CF), and three Gram-(–) bacteria of Escherichia coli (EC), Salmonella. typhimurium (SA), and Pseudomonas Solanacearum (PS). Compounds 4 and 7–9 were found to show strong in vitro antibacterial activity toward all the tested bacteria with the MIC values ranging from 1.56 to 12.5 µg/mL. Notably, compounds 4 and 9 showed significant antibacterial activity against the drug-resistant bacterium of MRSA with MIC value 6.25 µg/mL, which was close to reference compound vancomycin (MIC 3.125 µg/mL). Compounds 4 and 7–9 were further revealed to show in vitro cytotoxic activity toward human tumor A549, HepG2, MCF-7, and HeLa cell lines, with IC50 values ranging from 8.97 to 27.39 μM. No antibacterial and cytotoxic activity were displayed for the other compounds. The present research provided new data to support that M. micrantha is rich in structurally diverse bioactive compounds worthy of further development for pharmaceutical applications and for crop protection in agricultural fields.
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