Datura stramonium is one of the most intriguing, in part because of its well-known therapeutic and psychoactive properties in the treatment of many diseases. Datura species have been found to exhibit a variety of biological activity. Insecticide, fungicide, antioxidant, antibacterial, hypoglycemic, and immune response boosting properties have been linked to the genus' species. These effects are linked to the existence of secondary metabolites such as terpenoids, flavonoids, with anolides, tannins, phenolic compounds, and tropane alkaloids, which are the most prevalent atropine and scopolamine in the genus Datura. Ingestion of jimson weed produces the toxidrome of anticholinergic intoxication. Understanding and recognizing the classic signs and symptoms of anticholinergic intoxication can help clinicians evaluate persons presenting with jimson weed poisoning. Moreover, this review is to identify the most important phytochemical substances extracted from the jimsonweed and to characterize their biological activity for health effect and biopesticide application. This is because bio-pesticides are less harmful than chemical pesticides because they do not leave harmful residues, generally target one specific pest or a small number of related pests versus broad spectrum chemical pesticides that affect, in addition to the pest, other beneficial insects, birds, mammals, or non-target species, are effective in smaller quantities, decompose quickly and do not cause environmental problems, and are often cheaper than chemical pesticides. In conclusion, Datura stramonium, beside its medicinal value, can applicable for biopesticide application and for post-harvest loss control of insects such as weevil.