Preliminary insight on diarylpentanoids as potential antimalarials: In silico, in vitro LDH and in vivo zebrafish toxicity assessment.

Malaria remains a major public health problem worldwide, including in Southeast Asia. Chemotherapeutic agents such as chloroquine (CQ) are effective, but problems with drug resistance and toxicity have necessitated a continuous search for new effective antimalarial agents. Here we report on a virtual screening of ∼300 diarylpentanoids and derivatives, in search of potential lactate dehydrogenase (LDH) inhibitors with acceptable drug-like properties.

Toxicity and teratogenicity effects of valproic acid on zebrafish (Danio rerio) embryos in relation to autism spectrum disorder.

Valproic acid (VPA) is a widely prescribed antiepileptic drug with various medicinal efficacies. Accumulated evidence implied that prenatal exposure to VPA is highly associated with autism spectrum disorder (ASD). In this study, the zebrafish were exposed to a set of VPA concentrations (0, 5, 10, 20, 40, 80, 160, 320, 640, 1280, and 2560 μM) at 5 h post fertilization (hpf) to 120 hpf.

Chemical Composition and Evaluation of the -Glucosidase Inhibitory and Cytotoxic Properties of Marine Algae , and .

Seaweed has tremendous potentials as an alternative source of high-quality food products that have attracted research in recent times, due to their abundance and diversity. In the present study, three selected seaweed species commonly found in the Malaysian Peninsular, , and were subjected to preliminary chemical screening and evaluated for -glucosidase inhibitory and cytotoxic activities against five cancer cell lines. Chemical composition of and methanolic extracts was evaluated by Gas Chromatography-Mass Spectrometry (GC-MS) analysis.

Development of diarylpentadienone analogues as alpha-glucosidase inhibitor: Synthesis, in vitro biological and in vivo toxicity evaluations, and molecular docking analysis.

A series of aminated- (1-9) and sulfonamide-containing diarylpentadienones (10-18) were synthesized, structurally characterized, and evaluated for their in vitro anti-diabetic potential on α-glucosidase and DPP-4 enzymes. It was found that all the new molecules were non-associated PAINS compounds. The sulfonamide-containing series (compounds 10-18) selectively inhibited α-glucosidase over DPP-4, in which compound 18 demonstrated the highest activity with an IC value of 5.

Antinociceptive activity of methanolic extract of Acmella uliginosa (Sw.) Cass.

Ethnopharmacological Relevance: Acmella uliginosa (Sw.) Cass. is a medicinal herbaceous plant that is commonly used by the Malay community in Malaysia to relieve pain often associated with mouth ulcers, toothache, sore throat, and stomach ache.