Loganin was found in parts of some trees and shrubs including bark of Mastixia arborea (Cornaceae family), Corni fructus and A. boonei (Apocynaceae), a West African herbal medicinal plant traditionally used for its antimalarial, aphrodisiac, antidiabetic, antimicrobial properties. A key intermediate in the biosynthesis of indole alkaloids loganin was synthesized in 1971 by carboxyl group methylation of loganic acid. It has been shown, that loganin possesses anti-shock effects, anti-oxidant, glucose-lowering and neuroprotective properties. Loganin exhibits an anti-inflammatory effect in cases of acute pancreatitis and its pulmonary complications through inhibition of NF-κB activation. It is an active ingredient of a new herbal formula KBMSI-2 which has been through Phase 4 clinical trial for the efficacy and safety in the treatment of Erectile Dysfunction. Loganin inhibits β-secretase in vitro and increases performance in Morris water maze and Y-maze tests in vivo, suggesting potential benefit in memory impairment and Alzheimer’s disease. In addition, it also modulates ERK signaling to decrease connective tissue growth factor (CTGF) and downregulates expression of MCP-1, NF-κB, and iNOS in animal models. Inhibition of CTGF may be a potential target in diabetic nephropathy (DN) therapy, which highlights the possibility of using loganin to treat DN.