The subject invention provides fungal extracts, fungal metabolites, pharmaceutical compositions comprising the fungal extracts, and/or fungal metabolites, methods of preparation, and therapeutic uses thereof. The subject invention also provides a bioactive agent and a composition comprising the bioactive agent, and therapeutic uses thereof. The subject invention further provides methods for treating, inhibiting and/or preventing malaria infection and transmission by using the fungal extracts, fungal metabolites, bioactive agents, and pharmaceutical compositions comprising the fungal extracts, fungal metabolites, and/or bioactive agent.