Natural Products Journal, The - Online First

Marine fungi have been recognized as new sources for the discovery of valuable secondary metabolites, providing lead compounds for drug discovery and development.

The objective of this study was to isolate and identify the secondary metabolites from the marine-derived fungus Trichoderma harzianum ZN-4 and evaluate their antifungal activity.

Fungus strain Trichoderma harzianum ZN-4 was initially fermentated using a PDB liquid medium. Subsequently, extensive chromatographic methods were applied to isolate the fermentation cultures of ZN-4, and the chemical structures of isolate compounds were elucidated by 1D and 2D NMR, ECD, and HRESIMS. The antifungal activity was evaluated using the broth microdilution method.

Three new butenolides, harzianolides H–J (1–3), were isolated from T. harzianum ZN-4, and cultivated on a sterilized PDB medium. Activity evaluation showed that compounds 1−3 exhibited potent antifungal activity with MIC values of 12.5−100 μg/mL against the phytopathogenic fungus Pestalotiopsis theae.

This study not only enriched the structural diversity of the harzianolide family but also revealed their anti-P. theae activity, which may be potential antifungal agents.

Plants have been employed for centuries to enhance human health due to their cost-effectiveness and minimal adverse effects. Numerous plants exhibit a wide spectrum of pharmacological activities, and various herbal medicines are currently being investigated for their memory-enhancing properties.

Cucumis trigonus (Roxb.), commonly known as Kachari or Bitter gourd, is one such plant with diverse pharmacological attributes. Historically, the fruits of C. trigonus have been utilized for addressing various conditions like leprosy, pyrexia, icterus, hyperglycemia, chronic cough, bronchitis, abdominal fluid accumulation, anemia, obstipation, diverse gastrointestinal disease, and cognitive impairment. The current investigation aims to explore the memory enhancement properties of C. trigonus, rooted in its traditional applications, particularly against scopolamine-induced amnesia in mice. Morris water maze and elevated plus maze paradigms were employed to evaluate cognitive performance. Furthermore, the research examined acetylcholine neurotransmission, oxidative stress markers, and cerebral histopathology.

The results showed that C. trigonus ethanol extract (dose- 150 or 300 mg/kg., p.o.), markedly (p<0.05) improved memory in scopolamine-induced amnesia in mice and significantly (p<0.05) elevated hippocampus acetylcholine concentration. These findings revealed that the ethanol extract of C. trigonus fruits mitigates memory deficits and demonstrates neuroprotective efficacy analogous to the reference drug Piracetam. Additionally, the extract showed notable in vivo antioxidant activity. The occurrence of flavonoids and phenols is likely to be responsible for its memory-enhancing effects due to their antioxidant properties, which help to prevent the loss of neurons.

These results support the efficacy and potential of C. trigonus ethanol extract as an affordable alternative form of herbal medicine for the treatment of Amnesia.

The Chinese medicine, Kanglao concoction has been used clinically to treat tuberculosis. However, its constituents and anti-inflammatory activity have not been fully understood.

In this study, HPLC-MS² has been employed to determine the main constituents in the concoction. The anti-inflammatory activity has been investigated by ELISA and Western Blot techniques. The MS analysis revealed that tigogenin and afzelin were two main constituents in Kanglao concoction.

Moreover, the result of ELISA experiments showed that Kanglao concoction significantly reduced the expression of TNF-α and IL-1β at 5 mg/mL and 10 mg/mL to inhibit inflammation.

The expression of Notch pathway-related proteins in A549 cells increased under the stimulation of Mycobacterium tuberculosis, and decreased dose-dependently upon the treatment of Kanglao concoction, which was deduced to inhibit Notch pathway expression to impose anti-inflammatory activity.

Three novel macrolactams, FW8-1 (1), FW8-4 (2), and FW60-20 (3), were isolated from a culture of Micromonospora sp. The structures of these compounds were elucidated using Mass Spectrometry (MS) and comprehensive Nuclear Magnetic Resonance (NMR) analyses.

The relative configurations of compounds 1-3 were assigned through theoretical calculations of their NMR spectra.

The isolation and determination of the relative configurations of these macrolactams have provided fresh perspectives on the biosynthetic pathways, leading to the formation of polyene macrolactams.

Further, virtual screening and bioactivity predictions have suggested compounds 1-3 to possess potential anti-tumor, anti-inflammatory, and neuroprotective properties.