This study reports the chemical investigation and bioactivity of the secondary metabolites produced by the endophytic fungus Fusarium solani isolated from Cassia alata Linn. growing in Bangladesh. This plant was collected from conservation forest in Bangladesh and belongs to the Caesalpiniaceae family. The endophytic fungus Fusarium solani was isolated from the tissue of root of this plant. The fungal strain was identified by morphological characters and DNA sequencing. The crude organic extract of the fungal strain was proven to be active when tested for cytotoxicity against Brine Shrimp Lethality Bioassay, antimicrobial and antioxidant activity. The bioactivity guided fractionation of the ethyl acetate extract leads to the isolation of seven secondary metabolites in pure form. The structures of the isolated compounds were determined by the analysis of NMR and mass spectroscopic data. Bioassay investigation of the isolated secondary metabolites suggested aza-anthraquinones are more potent bioactive compounds as anticancer and antimicrobial agent.

As part of our continuous effort to find potential anti-inflammatory agents from endophytic fungi, a Fusarium solani strain, isolated from the plant Aponogeton undulatus Roxb., was investigated. Cerevisterol (CRVS) was identified from endophytic fungi, a Fusarium solani strain, and moreover exhibited anti-inflammatory activity. However, the underlying mode of action remains poorly understood. The aim of this study is to reveal the potential mechanisms of CRVS against inflammation on a molecular level in LPS-activated RAW 264.7 peritoneal macrophage cells. CRVS was isolated from F. solani and characterized based on spectral data analysis. The MTT assay was performed to measure cell viability in CRVS-treated macrophages. Anti-inflammatory activity was assessed by measurement of nitric oxide (NO) and prostaglandin E₂ (PGE₂) levels, as well as the production of various cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and -6 (IL-6) in LPS-stimulated macrophages. RT-PCR and immunoblotting analyses were done to examine the expression of various inflammatory response genes. A reporter gene assay was conducted to measure the level of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and activator protein-1 (AP-1) transactivation. CRVS suppresses the LPS-induced production of NO and PGE₂, which is a plausible mechanism for this effect is by reducing the expression of iNOS and COX-2. CRVS also decreases the expression of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β. CRVS halted the nuclear translocation of NF-κB by blocking the phosphorylation of inhibitory protein κBα (IκBα) and suppressing NF-κB transactivation. The mitogen-activated protein kinases (MAPK) signaling pathways are also suppressed. CRVS treatment also inhibited the transactivation of AP-1 and the phosphorylation of c-Fos. Furthermore, CRVS could induce the nuclear translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) by down-regulating Kelch-like ECH-associated protein 1 (Keap-1) and up-regulating hemeoxygenases-1 (HO-1) expression. The results suggest that CRVS acts as a natural agent for treating inflammatory diseases by targeting an MAPK, NF-κB, AP-1, and Nrf2-mediated HO-1 signaling cascade.

Endophytes have the potential to synthesize various bioactive secondary metabolites. The aim of the study was to find new cytotoxic and antibacterial metabolites from endophytic fungus, Cladosporium sp. isolated from the leaves of Rauwolfia serpentina (L.) Benth. ex Kurz. (Fam: Apocyanaceae). The endophytic fungus was grown on potato dextrose agar medium and extracted using ethyl acetate. Secondary metabolites were isolated by chromatographic separation and re-crystallization, and structures were confirmed by 1H NMR, 13C NMR and mass spectroscopic data. The cytotoxicity was determined by WST-1 assay and brine shrimp lethality bioassay, while antibacterial activity was assessed by disc diffusion method. Two naphthoquinones, namely anhydrofusarubin (1) and methyl ether of fusarubin (2), were isolated from Cladosporium sp. The isolated compounds 1 and 2, by WST-1 assay against human leukemia cells (K-562) showed potential cytotoxicity with IC50 values of 3.97 μg/mL and 3.58 μg/mL, respectively. Initial screening of crude ethyl acetate extract and column fractions F-8 and F-10 exhibited noticeable cytotoxicity to brine shimp nauplii with LC50 values of 42.8, 1.2 and 2.1 μg/mL, respectively. Moreover, the isolated compound 2 (40 μg/disc) showed prominent activities against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Bacillus megaterium with an average zone of inhibition of 27 mm, 25 mm, 24 mm and 22 mm, respectively and the activities were compared with kanamycin (30 μg/disc). Our findings indicate that anhydrofusarubin (1) and methyl ether of fusarubin (2) might be useful lead compounds to develop potential cytotoxic and antimicrobial drugs.

As a part of our ongoing research on endophytic fungi, we have isolated a sesterterpene mycotoxin, fusaproliferin (FUS), from a Fusarium solani strain, which is associated with the plant Aglaonema hookerianum Schott. FUS showed rapid and sub-micromolar IC₅₀ against pancreatic cancer cell lines. Time-dependent survival analysis and microscopy imaging showed rapid morphological changes in cancer cell lines 4 h after incubation with FUS. This provides a new chemical scaffold that can be further developed to obtain more potent synthetic agents against pancreatic cancer.

This study explored the great potential of endophytic fungi associated with red seaweed Gracilaria sp. and brown seaweed Sargassum sp. of the Bay of Bengal, Bangladesh, for the first time. Endophytic fungi were identified taxonomically by morphological features and molecular characterisation (ITS sequence). The identification of six fungal isolates revealed five different fungal species belonging to four genera, namely, Aspergillus subversicolor, A. terreus and Cladosporium halotolerans isolated from Gracilaria sp. and Chaetomium globosum, A. terreus and Curvularia perotidis isolated from Sargassum sp. The ethyl acetate extracts of fungal endophytes were evaluated for antimicrobial activity, DPPH radical scavenging activity, and brine shrimp lethality bioassay. Amongst all the fungal extracts evaluated in this study, four showed mild to moderate inhibitory activity (10–14 mm) against the tested bacterial strains. Exceptionally, Chaetomium globosum exerted significant antibacterial activity with the highest zone of inhibition (21 ± 0.3 mm) against the Gram-negative bacterial strain Pseudomonas aeruginosa and also showed moderate antifungal activity (13 ± 0.9 mm) against A. niger. Sargassum sp.-derived A. terreus exhibited the strongest DPPH radical scavenging activity (IC₅₀ value of 7.88 ± 0.09 µg/mL). All the fungal extracts have significant lethality against brine shrimp nauplii (LC₅₀ value of ≤ 20.39 ± 4.04 µg/mL), while Curvularia perotidis and Cladosporium halotolerans were the most effective (LC₅₀ values of 9.30 ± 2.96 µg/mL and 9.94 ± 3.49 µg/mL, respectively). Gas chromatography-mass spectrometry (GC-MS) analysis of the crude extracts identified the presence of several chemical compounds. These bioactive chemical constituents might contribute to the exhibited bioactivity in this study. The current study’s findings support the beneficial impacts of the fungal endophytes on exerting biological activities and consequently as valuable resources of bioactive compounds.

Nymphoides is an aquatic genus consisting about 50 species, of which few were accepted as traditional medicinal plants in Asia. The literature review revealed that Nymphoides species are widely used in Ayurvedic medicine as a popular drug, i.e. Tagara. They are also utilized by the traditional local healers of different Asian countries to treat various diseases, like convulsion, jaundice, fever, headache, etc. According to the in vivo and in vitro pharmacological studies, Nymphoides species have been claimed to possess major biological activities like anticonvulsant, antioxidant, hepatoprotective, cytotoxic, antitumor, etc. Biochemical profiling of different aquatic plants of this genus revealed the presence of some important phytochemicals as polyphenolic component, flavonoids, triterpenes, carbohydrates, glycosides, etc. Several valuable bioactive compounds including ephedrine, coumarin, secoiridoid glucosides, methyl quercetin, ferulic acid, foliamenthoic acid, etc. were also known to be isolated and identified from different Nymphoides species. The aim of this review is to analyze the published report based on the medicinal values of different Asian Nymphoides species, to provide the updated information about the ethnomedicinal, pharmacological as well as the phytochemical properties for the first time.