Piperine is a natural amide compound extracted from the pepper. It has a wide range of biological activities such as anti-infection, anti-oxidation, and immune regulation. The structure of piperine can be divided into three parts: aromatic heterocyclic ring, aliphatic hydrocarbon chain, and piperidine ring. These three parts are considered to be essential groups for the biological activity of piperine, and the above structural changes will affect its biological activity.
1 Anti-tumor effect
Piperine analog piperine can selectively inhibit the growth of tumor cells but has little effect on normal cells.
2 Suppress parasites
Inhibition of trypanosomal action
There are three types of trypanosomes: upper flagellum, amastigotes, and trypanosomes due to different parasitic environments. Piperine has different inhibitory effects on different types of trypanosomes, and the inhibitory effects of chemical structure changes are also changed. The structural modification is mainly in the diene. , Carryout on the amide bond.
- Inhibition of Leishmania
Leishmania, also known as kala-azar, can cause kala-azar. Leishmania Donovan is the main epidemic in my country. CARRARA et al. synthesized a series of piperine analogs with shorter hydrocarbon chains. Among them, compounds with aniline substituents have the strongest effect against Leishmania. After replacing the methylenedioxy group on the benzene ring with fluorine atoms and trifluoromethoxy groups, the anti-Leishmania activity decreased, indicating that a methylenedioxy group is an essential group for activity. The inhibitory effect of piperine on Leishmania after the combination of different amino acids is also enhanced. Among them, the binding activity of valine methyl ester is the strongest, and the IC50 of 1 μmol·L － 1 can inhibit the amastigotes. Grow. If the double bond in the compound is saturated, the inhibitory effect on the promastigote will be enhanced. Reducing the number of double bonds can also increase the inhibitory effect of piperine on the promastigotes, while the inhibitory effect on the amastigotes is significantly reduced. If the amide bond is hydrolyzed, the activity of inhibiting Leishmania is greatly reduced or even disappeared.
3 NorA efflux pump inhibition
Piperine can be used as a NorA efflux pump inhibitor to inhibit the development of bacterial resistance.
4 Lipid-lowering effect
Piper longiflorum as a folk Mongolian medicine has a wide range of biological activities, and its extract piperine has been proven to have good lipid-lowering activity.
5 Regulation of the central nervous system
Inhibit the activity of monoamine oxidase
Studies by ALBAGHDADI et al. have shown that short-chain piperine and its derivatives (33-36) can inhibit the activity of monoamine oxidase (MAO), and have the ability to treat Parkinson’s disease.
At present, many experiments have shown that piperine has antidepressant activity.