Research Progress of Tetrahydrocurcumin

Tetrahydrocurcumin (THC), as the most active and main metabolite produced in the metabolism of curcumin in vivo, can be isolated from the cytoplasm of the small intestine and liver after curcumin administration in human or mouse. Tetrahydrocurcumin can effectively inhibit tyrosinase, inhibit the generation of Oxygen Free Radicals and scavenge the formed free radicals. It has obvious antioxidant effect and has been used as a natural functional whitening raw material for cosmetics research and development.

In 1978, Holder et al. proved that tetrahydrocurcumin has similar pharmacological effects to curcumin. So far, studies have found that it has anti-metastasis and anticancer activities, antioxidant, free radical scavenging, hypoglycemic, hypolipidemic and other pharmacological activities, and a large number of experimental results show that its biological activities are better than curcumin, such as antioxidant chloroquine-induced kidney damage, antioxidant azo-methane induced colon cancer, etc. In addition, our previous study also found that tetrahydrocurcumin has a good therapeutic effect on metabolic syndrome, obesity type 2 diabetes, hypertension, insulin resistance syndrome and other related diseases, and has a wide range of application prospects.

1.Hypoglycemic Effect

Murugan P et al. induced type 2 diabetes mouse model with streptozocin, and then treated with tetrahydrocurcumin. The results showed that tetrahydrocurcumin could significantly reduce the blood sugar of diabetic mice and significantly improve insulin level, and the hypoglycemic effect of tetrahydrocurcumin on diabetic mice was even stronger than curcumin itself. In addition, niacinamide induced diabetic rats were given a certain amount of tetrahydrocurcumin by intragastric administration. The results showed that tetrahydrocurcumin could significantly reduce the blood glucose of diabetic rats and improve the plasma insulin level, indicating that tetrahydrocurcumin has a good hypoglycemic effect on type 2 diabetes.

2.Anti-oxidative Stress Effect

Murugan P et al. used niacinamide to induce diabetic rats, and the results showed that tetrahydrocurcumin could significantly improve the activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione - S-transferase, reduced glutathione, vitamin C and vitamin E in the liver and kidney of diabetic rats. These results indicated that tetrahydrocurcumin could protect and prevent cell membrane damage caused by lipid peroxidation. The results of the present study also suggest that the antioxidant effect of tetrahydrocurcumin may be related to the increase of oxidative stress.

3.Anti-fatty Liver Effect

Pan Xuefeng et al. studied the anti-fatty liver effect of tetrahydrocurcumin on human liver cell line L02 induced by oleic acid in vitro and in vitro, and the results showed that tetrahydrocurcumin could reduce the lipid droplets in human liver cell line L02 cells. In vivo experimental results of mice showed that tetrahydrocurcumin could reduce liver index, lipid, ALT, AST, and improve liver pathophysiology, and showed an obvious dose-effect relationship.

4.Hypolipidemic Effect

Karthikesan K et al. confirmed that tetrahydrocurcumin has a hypolipidemic effect on experimental diabetic rats induced by streptohomycin (STZ) -niacinamide (NA), and can restore the regulatory enzymes involved in lipid and lipoprotein metabolism, and its mechanism may be related to the increase of insulin secretion and antioxidant activity. Pari L et al. used STZ to induce diabetic rat model, and administered tetrahydrocurcumin inadministratively to diabetic rats for 45 days. The results showed that tetrahydrocurcumin has therapeutic effect on diabetes, and can reduce the contents of cholesterol, triglyceride, free fatty acid and phospholipid in serum and liver tissue, indicating that tetrahydrocurcumin can reduce the level of lipid in diabetic animals.

5.Effect of Lowering Blood Pressure

Nakmareong S et al. used L-NAME (L-arginine analog, the most commonly used nitric oxide synthase inhibitor in the laboratory) to induce a rat hypertensive model, and created a persistent hypertensive model 5 weeks later. After the success of the model, rats were treated with different doses of tetrahydrocurcumin, which showed obvious blood-pressure lowering effect 2 weeks after administration. And showed a dose-dependent relationship. There was no significant effect on blood pressure in the normal group.

6.Anti-inflammatory effect

Mukhopadhyay A et al. compared the effects of compounds such as curcumin (C), diacetate curcumin (DAH), triethyl curcumin (TEC), tetrahydrocurcumin (THC), and phenylbutazone (PB) on carrageenan. The anti-inflammatory effect of induced edema, the results show that curcuminoids can reduce edema at low doses, but show pro-inflammatory effects at high doses, indicating that curcuminoids have dual effects of anti-inflammatory and pro-inflammatory, and their activity was THC>C>PB>TEC, while DAH showed no anti-inflammatory activity.

7.Anticancer Effect

Lai C S et al. regularly injected azoxymethane subcutaneously into colon cancer mice to induce colon cancer in mice, then continued to feed curcumin and tetrahydrocurcumin, and evaluated the tumor after the experiment. The results showed that both curcumin and tetrahydrocurcumin could inhibit the formation of degenerative crypt foci and polyps, but tetrahydrocurcumin showed a better inhibitory effect. Another study also confirmed that tetrahydrocurcumin has anti-tumor activity in vivo and in vitro, can effectively reduce colon cancer carcinogenesis, increase leukemia cell death, and inhibit cancer cell metastasis.

8.Antidepressant Effects

Wen Caixia et al. studied the antidepressant effect of tetrahydrocurcumin by forcing mice to swim, and the results showed that different doses of tetrahydrocurcumin had different degrees of antidepressant effect. Ku Baoshan et al. studied the preparation of tetrahydrocurcumin solid dispersion, and the results also showed that tetrahydrocurcumin and its solid dispersion have anti-depressive effects, which may be related to the monoamine neurotransmitter system.

9.Protective Effect of Renal Function

Osawa T et al. found that tetrahydrocurcumin has a better effect than curcumin in improving the contents of urea, uric acid and creatinine in diabetic mice, and can simultaneously reduce albumin and urinary output, so as to prevent and treat the complications of diabetes. Its mechanism of action mainly lies in its ability to eliminate ROS, induce antioxidant enzymes related to detoxication, and promote the production of GSH.

Tetrahydrocurcumin, as a product extracted from natural plants and metabolized in vivo, has the advantages of low toxicity, low price and sufficient drug sources, so it is a promising drug. Huateng Pharma is a leading pharmaceutical intermediates supplier that can supply Tetrahydrocurcumin in large quantities with reasonable price.