piplartine and Hyperlipidemias

Spice and spice-derived compounds have been identified and explored for their health benefits since centuries. One of the spice long pepper has been traditionally used to treat chronic bronchitis, asthma, constipation, gonorrhea, paralysis of the tongue, diarrhea, cholera, malaria, viral hepatitis, respiratory infections, stomach ache, diseases of the spleen, cough, and tumors.. In this review, the evidences for the chemopreventive and chemotherapeutic potential of piperlongumine have been described.. The active component piperlonguime has shown effective against various ailments including cancer, neurogenerative disease, arthritis, melanogenesis, lupus nephritis, and hyperlipidemic. These beneficial effects of piperlongumine is attributed to its ability to modulate several signaling molecules like reactive oxygen species, kinases, proteasome, proto-oncogenes, transcription factors, cell cycle, inflammatory molecules and cell growth and survival molecules. Piperlongumine also chemosensitizes to drugs resistant cancer cells.. Overall the consumption of long peppers is therefore recommended for the prevention and treatment of various diseases including cancer, and thus piperlongumine may be a promising future candidate drug against cancer.

Topics: Arthritis; Brain Diseases; Dioxolanes; Humans; Hyperlipidemias; Lupus Nephritis; Neoplasms; Spices

Non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) are a growing epidemic and the most common liver diseases. Consumption of a western diet with high fats alters redox status, induces inflammation, and impairs the physiological function of hepatocytes. However, the pharmacological market lacks anti-NAFLD/NASH drugs. Long pepper (Piper longum L) is used in traditional Mongolian medicine for treating hyperlipidemia. Piperlongumine (PL) is a bioactive compound of Piper longum L, which usually possesses anticancer activities due to its ROS elevation property. However, when PL was demethylated they behave as an antioxidant. Previously, we found dihydroxy piperlongumine (DHPL) possesses high antioxidant activity among the hydroxy piperlongumines, which makes us curious to reveal the anti-NAFLD effect. A high-cholesterol diet (HCD) was chosen to induce NAFLD zebrafish model, and the antioxidant and lipid-lowering effects of DHPL were evaluated. Histological alterations of NAFLD were also scored along with gene expression to explore the molecular mechanism. DHPL reduced lipid accumulation in both short-term and long-term feeding trials. DHPL increases antioxidant activity and lipid-lowering gene expression and decreases hepatic triglyceride, oxidative stress, and lipogenic genes. In conclusion, DHPL halted the progression of HCD-induced NAFLD in the zebrafish model.

Topics: Animals; Antioxidants; Cholesterol; Diet, High-Fat; Hypercholesterolemia; Hyperlipidemias; Liver; Non-alcoholic Fatty Liver Disease; Triglycerides; Zebrafish

A novel thermostable form of piperlonguminine (GB-N) was extracted from medicinal plant Piper longum in efforts to explore the bioactive components underlying the mechanism of Piper longum in reducing plasma lipids. In vitro, HepG2 cells were employed to investigate the effects of GB-N on regulating cellular total cholesterol and low-density lipoprotein (LDL) receptor (LDLR) mRNA abundance, while high-fat and high-cholesterol diet-induced hyperlipidemic Wistar rats were used to investigate in vivo effects of GB-N. Cellular total cholesterol assay showed that GB-N dose-dependently reduced cellular total cholesterol in HepG2 cells in the presence and absence of elevated plasma cholesterol levels by 25% and 32%, respectively. Reverse transcription PCR assay showed that LDLR mRNA abundance was up-regulated dose-dependently by 142% via GB-N treatment in HepG2 cells. Animal experiment revealed that GB-N dose-dependently reduced serum total cholesterol by 26%, triglyceride by 47%, LDL cholesterol by 30%, while increased serum high-density lipoprotein (HDL) cholesterol by 524% in diet-induced hyperlipidemic Wistar rats. In conclusion, the results suggest the potential therapeutic uses of GB-N in the prevention and treatment of hyperlipidemia and related diseases.

Topics: Animals; Cell Line, Tumor; Cholesterol, Dietary; Diet, High-Fat; Dioxolanes; Hep G2 Cells; Humans; Hypercholesterolemia; Hyperlipidemias; Hypolipidemic Agents; Polymerase Chain Reaction; Rats; Rats, Wistar; Receptors, LDL; RNA, Messenger