Pharmacological effects of harmine and its derivatives: a review
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Online ISSN 1976-3786 Print ISSN 0253-6269
REVIEW
Pharmacological effects of harmine and its derivatives: a review Liang Zhang1 · Dengchang Li1 · Shenglan Yu1
Received: 18 March 2020 / Accepted: 29 October 2020 © The Pharmaceutical Society of Korea 2020
Abstract Harmine is isolated from the seeds of the medicinal plant, Peganum harmala L., and has been used for thousands of years in the Middle East and China. Harmine has many pharmacological activities including anti-inflammatory, neuroprotective, antidiabetic, and antitumor activities. Moreover, harmine exhibits insecticidal, antiviral, and antibacterial effects. Harmine derivatives exhibit pharmacological effects similar to those of harmine, but with better antitumor activity and low neurotoxicity. Many studies have been conducted on the pharmacological activities of harmine and harmine derivatives. This article reviews the pharmacological effects and associated mechanisms of harmine. In addition, the structure–activity relationship of harmine derivatives has been summarized. Keywords Harmine · Derivatives · Pharmacological effects · Neuroprotective effects · Antidiabetic · Anti-tumor Harmine is isolated from the seeds of the medicinal plant, Peganum harmala L., which grows in arid areas, such as the Middle East and some provinces of China, and has been widely used in folk medicine for a long time. Over thousands of years, diverse native plant species in South America have been used for their healing and psychoactive properties. A chemical trace of harmine was identified in a 1000-year-old ritual bundle from a rock shelter, which was situated at an elevation of 3900 m above sea level in southwestern Bolivia * Shenglan Yu [email protected] 1
College of Animal Pharmaceutical Sciences, Jiangsu AgriAnimal Husbandry Vocational College, Taizhou 225300, People’s Republic of China
(Miller et al. 2019). Harmine is one of two primary ingredients in the drink, ayahuasca, which has antianxiety and antidepressive effects in humans, and has been used by native people in South America for centuries. In China, harmine has been used for a long time by ethnic minorities such as the Uygur, Mongolian, and Kazak populations. Harmine (7-methoxy-1-methyl-9H-pyrido[3,4-b] indole) (Fig. 1) is a β-carboline alkaloid with broad-spectrum antiinflammatory and antitumor activities. In recent years, harmine has shown great potential in the treatment of diabetes (Wang et al. 2015). However, although harmine possesses notable pharmacological properties, its low bioavailability and side effects severely limit its clinical use. According to the China Food and Drug Administration databases, harmine has not been approved as a single agent so far. Uygur medicine in China uses some compound preparations containing harmine, such as muniziqi granules and harmel ointment, to treat rheumatoid arthritis. Harmine derivatives have been synthesized by several researchers to identify new compounds with low neurotoxicity and more potent antitumor activity than that of harmine. This article reviews the
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