Ursolic acid is a phytochemical found in various plants, but the most common is apple peel.
Although the scientific research is preliminary, it seems to reduce fat accumulation and increase muscle mass when eating, and induce fat burning and maintain muscle mass when fasting.
Earlier, in the case of streptozotocin induced diabetic mice, ursolic acid as a single therapy noted that compared with the control, 0.05% of the diet (about 10mg/kg) could reduce blood sugar by 12.3% in 4 weeks. Another study used 4 times (0.2%) of the dose in 11 weeks. The blood glucose level was reduced to 53% in the high-fat diet control group (although it was still two times that of the healthy control group). Ursolic acid tends to reduce blood glucose in a dose-dependent manner (because some studies have tested graded intake of ursolic acid in the range of 0.05-0.2%), which has similar efficacy to oleanolic acid.
It appears to be resistant to saccharification and may reduce the side effects of diabetes associated with hyperglycemia. In addition to the protective effect of glycosylation, low dose ursolic acid (0.01% of rat feed) has been noted to reduce the incidence rate of diabetic nephropathy, which may be secondary to anti-inflammatory properties and has been noted that ursolic acid has less atherosclerosis. It provides slightly more protection than an equal dose (0.2% of the diet) of resveratrol.
Ursolic acid appears to increase lipolysis in vitro through protein kinase A activation and downstream of hormone sensitive lipase (HSL) and lipid droplet coated protein A activity. The up regulation of adipose tissue lipase (ATGL) has been noted in adipocytes, which is not related to PKA.
In rats, 100 mg / kg ursolic acid seems to attenuate the increase of triglycerides in response to fat meal, which is considered to be achieved by inhibiting pancreatic lipase; The estimated human equivalent dose is 16 mg / kg.
Ursolic acid 10mg / kg (rat dose) reduced the weight gain of healthy rats fed a high-fat diet from 24% to 10.7% within 15 weeks, which was not significantly different from the active control (sibutramine) 10mg / kg. The study noted that high-fat induced changes in adipokines (ghrelin, leptin) and liver histology were normalized in both intervention groups, and ursolic acid was associated with increased insulin levels relative to high-fat controls and relatively reduced glucose levels.
The rat model of benign prostatic hyperplasia with oral administration of 5 mg / kg ursolic acid and injection of testosterone showed that the inhibition of prostate growth was similar to that of the active control (10 mg / kg finasteride), and the magnitude of inhibition of testosterone and DHT was equivalent to that of finasteride, but finasteride was more effective in reducing the serum level of prostate specific antigen (PSA).
Ursolic acid (and related compounds hawthorn acid and oleanolic acid) is known as angiogenesis inhibitor, which can prevent large blood vessels from forming new blood vessels. In vascular cells, ursolic acid appears to act by inhibiting PI3K Akt pathway and nitric oxide induction, inhibiting cellular changes before angiogenesis. These results have been observed in vivo with non-toxic doses of ursolic acid, which also inhibits the expression of MMP2 and MMP9 (intermediates required for the final stage of angiogenesis to enter new tissues).
Because new tumor cells need blood flow and angiogenesis to survive, the anticancer therapeutic potential of this angiogenesis inhibition is currently being studied. Previous studies on rats tested with ursolic acid showed that the degree of vascularization of melanoma in the ursolic acid 4.25mg/kg (50uml / kg) for 5 days was 42.03% of that in the control group (untreated group).
When rats were fed with 5mg / kg body weight, ursolic acid caused infertility by inhibiting spermatogenesis. Specifically, it breaks the bridge between the cells that are about to become sperm, and then the damaged cells gather to form symbionts in the seminiferous tubules associated with male infertility. But it doesn't seem to cause long-term damage to the testicles.
One study pointed out that ursolic acid can induce cell death in endothelial cells when the concentration exceeds 12.5um, and the death mechanism is related to apoptosis; DNA strand breaks were noted after 6 hours of incubation with p53.
Low dose ursolic acid (0.2% diet) was given to diabetic mice induced by streptozotocin and lacking LDL receptor. It was found that ursolic acid could reduce the inherent lesions in the diabetic endothelium by 53%. It suggests that it has protective but not necessarily rehabilitative effect. This protective effect is more effective than 0.2% resveratrol. Ursolic acid can also reduce the migration of monocytes to the endothelium, which is regarded as an inflammatory response.
At 50-100 μ At the concentration of M, ursolic acid can act as an insulin simulant and act on the receptor in 10 μ M has no inherent effect. One of the only studies to note the acute hypoglycemic effect of ursolic acid was an injection of 200 mg / kg, which may act on insulin receptors in this range.
Ursolic acid is a drug that resists the genetic response caused by fasting and mediates muscle decomposition. When mice were fed at 0.14% and 0.27% by weight (total intake unknown), ursolic acid was able to prevent muscle decomposition through genetic signals opposite to those that mediate muscle decomposition. It can increase the stress of skeletal muscle by increasing the transcription of anabolic genes, most notably the transcription of IGF-1. It does not seem to increase the expression of IGF-1 in adipose tissue, indicating that this activity is specific to skeletal muscle. This synthesis has been replicated in vitro, showing protein accumulation and increasing muscle cell size, but does not affect muscle cell differentiation.
One study pointed out that ursolic acid can induce cell death in endothelial cells when the concentration exceeds 12.5um, and the death mechanism is related to apoptosis; DNA strand breaks were noted after 6 hours of incubation with p53. DNA strand breaks were later observed in ApoE deficient mice when 10 um or 30 um ursolic acid was added to water.
Xi'an Haoze Biology is a professional supplier of nutritional supplement, plant extracts, fruit and vegetable powder, food additives, Cosmetic raw materials,etc., with quality assurance, competitive prices, and customer satisfaction as its tenet. If you have any requirements of ursolic acid or other product, please send an email to: haozebio2014@gmail.com