In vivo antimalarial evaluation of Gomphostenins

Area of Science:

• Pharmacology and Phytochemistry
• Infectious Diseases Research
• Medicinal Chemistry

Background:

• Malaria remains a significant global health challenge, necessitating the discovery of novel antimalarial agents.
• Gomphostemma niveum is a plant with potential medicinal properties.
• Clerodane diterpenes are a class of natural products with diverse biological activities.

Purpose of the Study:

• To evaluate the in vivo antimalarial potential of Gomphostemma niveum leaf extract.
• To assess the efficacy of two isolated compounds, Gomphostenin (GN-6) and acetyl Gomphostenin (GN-10), against Plasmodium berghei.
• To determine the dose-dependent effects of these compounds in a murine malaria model.

Main Methods:

• Oral administration of Gomphostemma niveum leaf extracts (GN-W, GN-C) and purified compounds (GN-6, GN-10) to Plasmodium berghei infected mice.
• Evaluation of blood schizontocidal activity in early and established infections.
• Comparison with chloroquine as a positive control and saline/tween-80 as a negative control.

Main Results:

• Both leaf extracts and purified compounds exhibited dose-dependent chemosuppression.
• Acetyl Gomphostenin (GN-10) achieved the highest chemosuppression rate (92.65%) at 200 mg/kg/day.
• GN-10 significantly prolonged the survival period of infected mice in curative tests.

Conclusions:

• Clerodane diterpenes, GN-6 and GN-10, possess significant in vivo antimalarial properties.
• These compounds show promise for the development of new antimalarial drugs.
• Gomphostemma niveum is a potential source for novel antimalarial chemotherapy agents.