Andrographolide: A Novel Antimalarial Diterpene Lactone Compound fromAndrographis paniculataand Its Interaction with Curcumin and Artesunate

Abstract

Andrographolide (AND), the diterpene lactone compound, was purified by HPLC from the methanolic fraction of the plant Andrographis paniculata. The compound was found to have potent antiplasmodial activity when tested in isolation and in combination with curcumin and artesunate against the erythrocytic stages of Plasmodium falciparum in vitro and Plasmodium berghei ANKA in vivo. IC50s for artesunate (AS), andrographolide (AND), and curcumin (CUR) were found to be 0.05, 9.1 and 17.4 μM, respectively. The compound (AND) was found synergistic with curcumin (CUR) and addictively interactive with artesunate (AS). In vivo, andrographolide-curcumin exhibited better antimalarial activity, not only by reducing parasitemia (29%), compared to the control (81%), but also by extending the life span by 2-3 folds. Being nontoxic to the in vivo system this agent can be used as template molecule for designing new derivatives with improved antimalarial properties.

Effects of andrographolide and 14-deoxy-11,12-didehydroandrographolide on cultured primary astrocytes and PC12 cells

“…For example, intraperitoneal injection affording doses of 50 mg/kg of body weight (roughly 143 μM) in mice (Mishra et al, 2011) or intraperitoneal doses equal to 4 mg/kg of andrographolide (roughly 11.4 μM) (Iruretagoyena et al, 2005) or LD50 for intraperitoneal administration of 11.6 g/kg (33.1 mM) (Handa and Sharma, 1990) have been investigated. Considering that the absolute bioavailability of andrographolide is 2.67% (Ye et al, 2011), the estimated available concentration for nonintravenous administration tested ranges from 0.3 μM to 883.8 μM.…”

Andrographolide and Its Derivative - A Story of Antimalarial Drug Design and Synthesis

“…1) is the major secondary metabolite in an Indonesian herb, Sambiloto (Andrographis paniculata) [6]. It was found to have a moderate antimalarial activity against a chloroquine-resistant strain of PF [7], making it an interesting lead for new antimalarial drugs.…”

Particulate Delivery System of Chitosan - Diterpene Lactone Fraction of Sambiloto (Andrographis Paniculata Nees): Preparation, Characterization and in Vitro Drug Release

“…Sambiloto (Andrographis paniculata Nees) is a medicinal plant that has many activities such as analgesic, antipyretic, anti-inflammatory, hepatoprotective, antiviral, antithrombotic, and anticancer [9,10]. The diterpene lactone compound of sambiloto is andrographolide, which has low oral bioavailability due to its high lipophilicity (log P=2.632), low solubility in water (3.29±0.73 mg/L), and short biological halflife [11,12].…”