curcumin and naringin

The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy. Herbal bioenhancers play a crucial role in enhancing the bioavailability and bioefficacy of different classes of drugs, such as antihypertensives, anticancer, antiviral, antitubercular and antifungal drugs at low doses. This paper highlights various natural compounds that can be utilized as an efficient bioenhancer. Several herbal compounds including piperine, quercetin, genistein, naringin, sinomenine, curcumin, and glycyrrhizin have demonstrated capability to improve the pharmacokinetic parameters of several potent API. This article also focuses on various United States patents on herbal bioenhancers, which has proved to be beneficial in improving oral absorption of nutraceuticals like vitamins, minerals, amino acids and certain herbal compounds. The present paper also describes proposed mechanism of action, which mainly includes absorption process, drug metabolism, and action on drug target. The herbal bioenhancers are easily available, safe, free from side effects, minimizes drug toxicity, shortens the duration of treatment, lowers the drug resistance problems and minimizes the cost of treatment. Inspite of the fact that herbal bioenhancers provide an innovative concept for enhancing the bioavailability of several potent drugs, there are numerous bioenhancers of herbal origin that are yet to be explored in several vital areas. These bioenhancers must also be implied to enhance the bioavailability and bioefficacy through routes other than the oral route of drug delivery. There is a vast array of unexploited plants which can be investigated for their drug bioenhancing potency. The toxicity profiles of these herbal bioenhancers must not be overlooked. Researches must be carried out to solve these issues and to deliver a safe and effective dose of drugs to attain desired pharmacological response.

Topics: Adjuvants, Pharmaceutic; Alkaloids; Benzodioxoles; Biological Availability; Carum; Cuminum; Curcumin; Ergolines; Flavanones; Genistein; Glycyrrhizic Acid; Humans; Morphinans; Piperidines; Plant Extracts; Polyunsaturated Alkamides; Quercetin; Zingiber officinale

Among obesity-associated disorders, low-grade inflammation has been described. The putative therapeutic properties of citrus and curcumin polyphenols could be associated with their anti-inflammatory properties. Two diets supplemented either with hesperidin (0.05 %) and naringin (0.1 %) from citrus extract or with highly bioavailable curcumin from Curcuma longa extract (0.09 %) were fed to eight obese cats for two 8-week periods (cross-over study design) while maintaining animals in an obese state. Plasma acute-phase protein (APP; α1-acid glycoprotein (AGP), serum amyloid A and haptoglobin) levels were assessed before and at the end of each test period. TNF-α, IL-1β, IL-2, IL-4, IL-5, IL-10, IL-12, IL-18, transforming growth factor-β, interferon (IFN)-γ mRNA levels were determined in peripheral blood mononuclear cells (PBMC) by real-time PCR. Compared with pre-study values, supplementation with citrus polyphenols resulted in lower plasma AGP and haptoglobin concentrations, while that with curcumin resulted in lower plasma AGP concentration. There were no differences between the supplementations. TNF-α, IL-1β, IL-4, IL-5, IL-10, IL-12, IL-18, transforming growth factor-β, mRNA levels remained unaffected by either dietary supplementation. In contrast, IFN-γ and IL-2 mRNA levels were lower at the end of the citrus and the curcumin supplementation, respectively. There were no differences between the supplementations. The present study results show a slight effect of citrus and curcumin supplementation on inflammatory markers expressed by PBMC, and a decreased concentration of APP, which are mainly expressed by the liver. This would confirm that hesperidin and naringin or highly bioavailable curcumin extract have beneficial effects, targeted in the liver and could improve the obesity-related inflammatory state.

Topics: Acute-Phase Proteins; Animals; Cat Diseases; Cats; Citrus; Cross-Over Studies; Curcumin; Cytokines; Female; Flavanones; Gene Expression Regulation; Hesperidin; Inflammation; Leukocytes, Mononuclear; Male; Obesity; RNA, Messenger

Clinical translation of BCRP inhibitors have failed due to neurotoxicity and novel approaches are required to identify suitable modulators of BCRP to enhance CNS drug delivery. In this study we examine 18 compounds, primarily phytochemicals, as potential novel modulators of AhR-mediated regulation of BCRP expression and function in immortalised and primary porcine brain microvascular endothelial cells as a mechanism to enhance CNS drug delivery. The majority of modulators possessed a cellular viability IC

Topics: Animals; ATP Binding Cassette Transporter, Subfamily G, Member 2; Blood-Brain Barrier; Cell Culture Techniques; Cell Line; Cell Survival; Cells, Cultured; Curcumin; Endothelial Cells; Estradiol; Flavanones; Gene Expression; Mice; Microvessels; Phytochemicals; Quercetin; Receptors, Aryl Hydrocarbon; Swine

The use of biocompounds as agents with potential anti-obesity effects might be a feasible alternative to the prescription of traditional drugs in the near future. The goal of the present study was to screen five different compounds in relation to their ability to prevent body weight gain and ameliorate obesity-associated metabolic impairments, namely insulin resistance. For this purpose, seventy Wistar rats were randomly assigned into seven experimental groups. A standard diet-fed control group (control, n=10); a high-fat, high-sucrose diet-fed group (HFS, n=10) and five experimental groups which were fed the HFS diet supplemented with one of the following biocompounds; curcumin (100 mg/kg bw, n=10), chlorogenic acid (50 mg/kg bw, n=10), coumaric acid (100 mg/kg bw, n=10), naringin (100 mg/kg bw, n=10) and leucine (1% of diet, n=10). These results confirm the effectiveness of all the compounds to reduce significantly food efficiency, despite the significant higher food intake. Moreover, visceral fat mass percentage was significantly decreased after naringin and coumaric acid supplementation. In fact, this finding might be related to the considerable amelioration of HOMA-IR index detected in naringin-treated animals. A significant reduction in serum insulin levels and an improvement in the intraperitoneal glucose tolerance test and AUC were found in leucine- and coumaric acid-treated rats, respectively. In summary, the tested biocompounds, particularly naringin, coumaric acid and leucine, showed potential benefits in the prevention of obesity-related complications in rats, at least at the proved doses.

Topics: Animals; Blood Glucose; Chlorogenic Acid; Coumaric Acids; Curcumin; Diet, High-Fat; Dietary Fats; Dietary Supplements; Flavanones; Humans; Insulin Resistance; Leucine; Male; Obesity; Rats; Rats, Wistar; Sucrose

Biologically active compounds from several useful plants were enriched using foam fractionation, a separatory method belonging to the adsorptive bubble separation (ABS). Nonpolar humulones (1-6) from Pilsener beer, curcuminoids (7-9) from turmeric, and carotenoids (16 and 17) from carrot juice were enriched fast and quantitatively, depending on the process parameters, whereas more polar compounds such as catechins from green tea (11, 12, 14, and 15) and naringin (18) and hesperidin (19) from orange and grapefruit juices could not be enriched.

Topics: Carotenoids; Chemical Fractionation; Chromatography, High Pressure Liquid; Citrus; Curcuma; Curcumin; Cyclohexenes; Daucus carota; Flavanones; Hesperidin; Molecular Structure; Plant Extracts; Tea; Terpenes; Water