Drug intelligence / Profile preview

kolaviron

Development stage
Preclinical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Kolaviron is a **biflavonoid complex** isolated from the seeds of *Garcinia kola* (bitter kola), composed primarily of kolaflavanone, Garcinia biflavonoid GB1, and GB2[1][3][5]. It is not a conventional pharmaceutical but a patented natural product mixture used in traditional medicine. **Kolaviron exhibits a wide spectrum of pharmacological activities** including antioxidant, anti-inflammatory, hepatoprotective, antigenotoxic, neuroprotective, antihyperglycemic, antimicrobial, antidiabetic, and potentially anticancer effects[1][3][7][8]. Mechanistically, kolaviron acts mainly by modulating oxidative stress pathways, boosting antioxidant enzyme activity (e.g., glutathione-S-transferase, superoxide dismutase, catalase), suppressing proinflammatory cytokines (e.g., IL-1β, TNF-alpha, IL-6), and regulating lipid and glucose metabolism[1][3][8][12]. Its precise molecular targets are multiple and include both direct antioxidative actions and modulation of inflammatory signaling pathways, such as nuclear factor-kappa B (NF-κB) and Nrf2[3]. Most evidence comes from preclinical animal and cell models, with emerging interest in its use for liver diseases, diabetes, and inflammation-associated conditions[4][7][11]. No regulatory-approved pharmaceutical formulation or large-scale clinical trials are reported as of the current date.

Brand names
kolaviron
Other names
kolaflavanoneGarcinia biflavonoid GB1Garcinia biflavonoid GB2kolaflavanone (for mixture)biflavonoid complex of Garcinia kola
02

Targets

ALDH1A1 (Aldehyde dehydrogenase 1 family member A1)IL1B (Interleukin-1 beta)GST (Glutathione S-transferase alpha 3)TNFA (Tumor necrosis factor alpha (soluble))IL-6 (Interleukin 6)NOS2 (Nitric Oxide Synthase 2)

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