Background: Alzheimer’s disease (AD) and vascular dementia (VaD) are major types of
dementia, both of which cause heavy economic burdens for families and society. However, no currently
available medicines can control dementia progression. Rhizoma coptidis, a Chinese herbal medicine, has
been used for >2000 years and is now gaining attention as a potential treatment for AD and VaD.
Methods: We reviewed the mechanisms of the active ingredients of Rhizoma coptidis and Rhizoma
coptidis-containing Chinese herbal compounds in the treatment of AD and VaD. We focused on studies
on ameliorating the risk factors and the pathological changes of these diseases.
Results: The Rhizoma coptidis active ingredients include berberine, palmatine, coptisine, epiberberine,
jatrorrhizine and protopine. The most widely studied ingredient is berberine, which has extensive therapeutic
effects on the risk factors and pathogenesis of dementia. It can control blood glucose and lipid
levels, regulate blood pressure, ameliorate atherosclerosis, inhibit cholinesterase activity, Aβ generation,
and tau hyperphosphorylation, decrease neuroinflammation and oxidative stress and alleviate cognitive
impairment. Other ingredients (such as jatrorrhizine, coptisine, epiberberine and palmatine) also regulate
blood lipids and blood pressure; however, there are relatively few studies on them. Rhizoma
coptidis-containing Chinese herbal compounds like Huanglian-Jie-Du-Tang, Huanglian Wendan Decoction,
Banxia Xiexin Decoction and Huannao Yicong Formula have anti-inflammatory and antioxidant
stress activities, regulate insulin signaling, inhibit !-secretase activity, neuronal apoptosis, tau hyperphosphorylation,
and Aβ deposition, and promote neural stem cell differentiation, thereby improving
Conclusion: The “One-Molecule, One-Target” paradigm has suffered heavy setbacks, but a “multitarget-
directed ligands” strategy may be viable. Rhizoma coptidis active ingredients and Rhizoma coptidiscontaining
Chinese herbal compounds have multi-aspect therapeutic effects on AD and VaD.