Potential Anticancer Properties of Osthol: A Comprehensive Mechanistic Review

Abstract

Cancer is caused by uncontrolled cell proliferation which has the potential to occur in different tissues and spread into surrounding and distant tissues. Despite the current advances in the field of anticancer agents, rapidly developing resistance against different chemotherapeutic drugs and significantly higher off-target effects cause millions of deaths every year. Osthol is a natural coumarin isolated from Apiaceaous plants which has demonstrated several pharmacological effects, such as antineoplastic, anti-inflammatory and antioxidant properties. We have attempted to summarize up-to-date information related to pharmacological effects and molecular mechanisms of osthol as a lead compound in managing malignancies. Electronic databases, including PubMed, Cochrane library, ScienceDirect and Scopus were searched for in vitro, in vivo and clinical studies on anticancer effects of osthol. Osthol exerts remarkable anticancer properties by suppressing cancer cell growth and induction of apoptosis. Osthol’s protective and therapeutic effects have been observed in different cancers, including ovarian, cervical, colon and prostate cancers as well as chronic myeloid leukemia, lung adenocarcinoma, glioma, hepatocellular, glioblastoma, renal and invasive mammary carcinoma. A large body of evidence demonstrates that osthol regulates apoptosis, proliferation and invasion in different types of malignant cells which are mediated by multiple signal transduction cascades. In this review, we set spotlights on various pathways which are targeted by osthol in different cancers to inhibit cancer development and progression.

Osthole stimulates bone formation, drives vascularization and retards adipogenesis to alleviate alcohol‐induced osteonecrosis of the femoral head

“…For the next 6 weeks, in ethanol group, rats had an ethanol‐containing Lieber‐DeCarli liquid diet, containing 8% (w/v) ethanol (36% of daily calories) . The rats in the ethanol + osthole group had the same ethanol diet but were co‐treated with osthole (100 mg/kg/d) by intraperitoneal injection, and the rats in control group had the normal Lieber‐DeCarli liquid diet without ethanol (the ethanol was displaced by maltodextrin, with the same amount of calories). All rats were free access to the diets which were refreshed every day.…”

“…Previous studies have found several herbs, and their monomers could ameliorate alcohol‐induced ONFH in animal models . Osthole, a coumarin bioactive derivative, obtained from many medical plants, is commonly used as ingredients in herbal medicine and functional foods . With the in‐depth investigations, osthole is revealed to possess a wide range of different pharmacological effects, including hepatoprotective, vasorelaxant, antileishmanial, neuroprotective, spasmolytic and antimicrobial properties .…”

Osthole, a Natural Plant Derivative Inhibits MRGPRX2 Induced Mast Cell Responses

“…Osthole is a natural coumarin present in the medicinal plant Cnidium monnieri. Because osthole demonstrates significant protective effects in animal models of hepatic diseases (30,31), cancer (54), diabetes (27,28), osteoarthritis (55), cardiovascular (56,57) and allergic diseases (18,34), it is a promising natural lead compound for drug discovery. Herein we demonstrate that osthole inhibits mast cell activation via MRGPRX2.…”

Osthole: A Traditional Chinese Medicine for Ocular Anti-Angiogenic Therapy

“…Osthole has shown great potential in the treatment of several disorders through their anti-inflammatory, anti-bacterial, and anti-allergic properties [29]. Previous studies have shown that osthole inhibits the proliferation of cancer via the suppression of neovascularization [24]. There are some similarities between corneal neovascularization and tumor angiogenesis.…”

“…It has potential therapeutic applications because of its significant and diverse pharmacological (anti-cancer, anti-osteoporotic, and anti-proliferative) activities[21-23]. Previous studies have demonstrated that osthole exerts anti-cancer activity by inhibiting angiogenesis, suggesting a potential role of osthole in anti-angiogenesis [24]. However, the role of osthole in corneal neovascularization is still unclear.…”