Berberine: A Potential Multipotent Natural Product to Combat Alzheimer’s Disease

Abstract

With the accelerated aging of human society Alzheimer’s disease (AD) has become one of the most threatening diseases in the elderly. However, there is no efficient therapeutic agent to combat AD. Berberine is a natural isoquinoline alkaloid that possesses a wide range of pharmacological effects. In the present paper, we review the multiple activities of berberine, including antioxidant, acetylcholinesterase and butyrylcholinesterase inhibitory, monoamine oxidase inhibitory, amyloid-b peptide level-reducing and cholesterol-lowering activities, which suggest that berberine may act as a promising multipotent agent to combat AD.

Possible role of P-glycoprotein in the neuroprotective mechanism of berberine in intracerebroventricular streptozotocin-induced cognitive dysfunction

“…Extensive literature supporting the anti-inflammatory and antioxidant activity of berberine against various diseases is available (Kulkarni and Dhir 2010;Ji and Shen 2011;Singh and Chopra 2013). There is a renewed interest in berberine because of its possible clinical benefits in central nervous system (CNS) disorders including AD (Zhu and Qian 2006), depression (Peng et al 2007), psychosis (Tarrago et al 2007), and anxiety (Peng et al 2004).…”

Immunomodulatory effects of barberry’s (Berberis integerrima) ingredients on macrophages: an in-vitro study

“…Some barberry's components which are responsible for this plant effects are alkaloids such as berberine, oxyacanthine, berbamine, and palmatine [5,8]. Berberis species are worldwide used for various purposes to alleviate central nervous system disorders [9], Alzheimer [10], liver disorder, bronchial diseases, and urinary discomforts [11]. It has also been used for the treatment of diarrhea [12], lowering blood glucose in type 2 diabetes mellitus [13].…”

Synthesis of C3/C1-Substituted Tetrahydroisoquinolines

“…However, since 2 did not inhibit more than 50% any of the enzymatic activities, continuous assays were not performed according to our standard policy. (10)(11) The approach used to generate the C3/C1-substituted THIQ core was based on the preparation of 4-(2-acetamidobutyl)-2-methoxyphenyl acetate 13 and the subsequent Bischler-Napieralski cyclodehydration (Scheme 1). Our synthesis began with the Henry condensation reaction between vanillin and nitropropane, performed in the presence of a catalytic amount of ammonium acetate, in a solventless system and under microwave irradiation (Scheme 1).…”

“…The 1,2,3,4-tetrahydroisoquinoline (THIQ) skeleton is an important structural motif commonly encountered in naturally-occurring alkaloids of vegetal origin with interesting biological/pharmacological properties, including inhibition of cell proliferation/anticancer activity [1], multiple cardiovascular activities related to different mechanisms of action [2][3][4], anti-inflammatory [5], antimicrobial [6,7], antiplasmodial activities [8,9] and acetylcholinesterase inhibitory effects [10,11]. A variety of THIQ derivatives has been found also in mammals, especially in human brain, suggesting a role of these molecules in neurons under physiological and pathological conditions [12].…”