Chemical constituents from the medicinal herb-derived fungus Chaetomium globosum Km1226.

BACKGROUND: Endophytic fungi have proven to be a rich source of novel natural products with a wide-array of biological activities and higher levels of structural diversity. RESULTS: Chemical investigation on the liquid- and solid-state fermented products of Chaetomium globosum Km1226 isolated from the littoral medicinal herb Atriplex maximowicziana Makino resulted in the isolation of compounds 1-14. Their structures were determined by spectroscopic analysis as three previously undescribed C13-polyketides, namely aureonitol C (1), mollipilins G (2), and H (3), along with eleven known compounds 4-14. Among these, mollipilin A (5) exhibited significant nitric oxide production inhibitory activity in LPS-induced BV-2 microglial cells with an IC50 value of 0.7 ± 0.1 µM, and chaetoglobosin D (10) displayed potent anti-angiogenesis property in human endothelial progenitor cells (EPCs) with an IC50 value of 0.8 ± 0.3 µM. CONCLUSIONS: Three previously unreported compounds 1-3 were isolated and identified. Mollipilin A (5) and chaetoglobosin D (10) could possibly be developed as anti-inflammatory and anti-angiogenic lead drugs, respectively.

Anti-Epstein-Barr Viral Agents from the Medicinal Herb-Derived Fungus Alternaria alstroemeriae Km2286.

Chromatographic separation on the liquid-state fermented products produced by the fungal strain Alternaria alstroemeriae Km2286 isolated from the littoral medicinal herb Atriplex maximowicziana Makino resulted in the isolation of compounds 1-9. Structures were determined by spectroscopic analysis as four undescribed perylenequinones, altertromins A-D (1-4), along with altertoxin IV (5), altertoxin VIII (6), stemphyperylenol (7), tenuazonic acid (8), and allo-tenuazonic acid (9). Compounds 1-6 exhibited antiviral activities against Epstein-Barr virus (EBV) with EC50 values ranging from 0.17 ± 0.07 to 3.13 ± 0.31 µM and selectivity indices higher than 10. In an anti-neuroinflammatory assay, compounds 1-4, 6, and 7 showed inhibitory activity of nitric oxide production in lipopolysaccharide-induced microglial BV-2 cells, with IC50 values ranging from 0.33 ± 0.04 to 4.08 ± 0.53 µM without significant cytotoxicity. This is the first report to describe perylenequinone-type compounds with potent anti-EBV and anti-neuroinflammatory activities.

Isolation of endophytic fungi with antimicrobial activity from medicinal plant Zanthoxylum simulans Hance.

Fungal endophytes have been found to exist in many plant species and appear to be important to their plant hosts. However, the diversity and biological activities of these fungi remain largely unknown. Zanthoxylum simulans Hance, a popular natural spice and medicinal plant, commonly known as Szechuan pepper or Chinese-pepper, grows on Kinmen Island, Taiwan. In this study, leaf and stem samples of Z. simulans, collected in summer and winter, were screened for antimicrobial and anti-inflammatory metabolite-producing endophytic fungi. A total of 113 endophytic strains were isolated and cultured from Z. simulans, among which 23 were found to possess antimicrobial activity, belonging to six fungal genera: Penicillium (26.09%, 6), Colletotrichum (21.74%, 5), Diaporthe (21.74%, 5), Daldinia (17.39%, 4), Alternaria (8.70%, 2), and Didymella (4.34%, 1). We also found that the number of species with antimicrobial activity and their compositions differed between summer and winter. Our study demonstrated that Z. simulans might contain large and diverse communities of endophytic fungi, and its community composition varies seasonally. In addition, fungal endophytes produce antimicrobial agents, which may protect their hosts against pathogens and could be a potential source of natural antibiotics.

Antimicrobial and iNOS inhibitory activities of the endophytic fungi isolated from the mangrove plant Acanthus ilicifolius var. xiamenensis.

BACKGROUND: Acanthus ilicifolius var. xiamenensis (Acanthaceae) is an old world mangrove species and has long been used as a folk remedy for treating various ailments in traditional medicine. The nature source of A. ilicifolius var. xiamenensis is now in short supply because of the urban development and habitat destruction. To better utilize this resource, biodiversity and bioactivity of endophytic fungi isolated from A. ilicifolius var. xiamenensis were investigated. RESULTS: A total of 168 fungal isolates were cultured from leaves and stems of the mangrove plant collected in January (winter) and July (summer) 2014 at Kinmen County, Taiwan. Spent culture extract of 28 isolates were found to have bioactivities against one of the following pathogenic microorganisms: the bacteria Bacillus subtilis, Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative) and the fungi Candida albicans and Cryptococcus neoformans. These positive extracts were mostly active against the Gram-positive bacteria and C. albicans. Corynespora cassiicola NTOU4889 and Xylaria sp. NTOU4900 inhibited growth of all 3 test bacteria whereas Phellinus noxius NTOU4917 inhibited both test fungi. A further anti-inflammatory study of culture extracts of these 28 isolates revealed that extracts with a high iNOS inhibition caused a low viability of cells, and those with a low iNOS inhibition had a high cell viability. Three extracts showed low cytotoxicity (i.e. > 100% cell viability) and high iNOS inhibition (< 15% of NO production) of cells and they were Phoma sp. 2 NTOU4338, Nodulisporium sp. NTOU4868 and Guignardia sp. NTOU4871. CONCLUSION: These results indicate that the endophytic fungi associated with A. ilicifolius var. xiamenensis can be a potential source of novel natural active substance.