(Honeybush) Induces Uncoupling Protein 1 and Peroxisome Proliferator-Activated Receptor Alpha Expression in Obese Diabetic Female db/db Mice.

Previously, we reported that a crude polyphenol-enriched fraction of (CPEF), a plant consumed as the herbal tea, commonly known as honeybush, reduced lipid content in 3T3-L1 adipocytes and inhibited body weight gain in obese, diabetic female leptin receptor-deficient (db/db) mice. In the current study, the mechanisms underlying decreased body weight gain in db/db mice were further elucidated using western blot analysis and in silico approaches. CPEF induced uncoupling protein 1 (UCP1, 3.

Identification of a novel di-C-glycosyl dihydrochalcone and the thermal stability of polyphenols in model ready-to-drink beverage solutions with Cyclopia subternata extract as functional ingredient.

Heat processing of ready-to-drink beverages is required to ensure a microbiologically safe product, however, this can result in the loss of bioactive compounds responsible for functionality. The objective of this study was to establish the thermal stability of a novel dihydrochalcone, 3',5'-di-β-d-glucopyranosyl-3-hydroxyphloretin (2), 3',5'-di-β-d-glucopyranosylphloretin (3) and other Cyclopia subternata phenolic compounds, in model solutions with or without citric acid and ascorbic acid. The solutions were heated at 93, 121 and 135 °C, relevant to pasteurisation, commercial sterilisation and ultra-high temperature (UHT) pasteurisation, respectively.

Physicochemical Stability of Enriched Phenolic Fractions of Cyclopia genistoides and ex vivo Bi-directional Permeability of Major Xanthones and Benzophenones.

Fractions of an ultrafiltered extract, respectively enriched in xanthones and benzophenones, were previously shown to inhibit mammalian -glucosidase The present study investigated intestinal transport of these fractions, using excised porcine jejunal tissue, to determine whether the gut could be a predominant site of action. The major bioactive compounds, the xanthones (mangiferin, isomangiferin) and benzophenones (3--D-glucopyranosyliriflophenone, 3--D-glucopyranosyl-4---D-glucopyranosyliriflophenone) exhibited poor permeation in the absorptive direction with a relatively high efflux ratio (efflux ratio > 1). The efflux ratio of 3--D-glucopyranosyl-4---D-glucopyranosyliriflophenone (3.

Wound Healing Effects of : In Vitro Investigations Using Immortalized Human Keratinocytes (HaCaT).

The traditional use of spp. for the purpose of wound healing has a long history and is widespread internationally. Recently, a hybrid aloe plant () has been cultivated by cross pollination between and .

In vitroα-glucosidase inhibition by honeybush (Cyclopia genistoides) food ingredient extract-potential for dose reduction of acarbose through synergism.

Extracts of Cyclopia species are used as food ingredients. In vitroα-glucosidase (AG) inhibition by ultrafiltered C. genistoides extract, fractions enriched in xanthones (XEF) and benzophenones (BEF), as well as mangiferin, isomangiferin, 3-β-d-glucopyranosyliriflophenone (I3G) and 3-β-d-glucopyranosyl-4-O-β-d-glucopyranosyliriflophenone (IDG) was determined with acarbose as positive control.

Adipose tissue as a possible therapeutic target for polyphenols: A case for Cyclopia extracts as anti-obesity nutraceuticals.

Obesity is a significant contributor to increased morbidity and premature mortality due to increasing the risk of many chronic metabolic diseases such as type 2 diabetes, cardiovascular disease and certain types of cancer. Lifestyle modifications such as energy restriction and increased physical activity are highly effective first-line treatment strategies used in the management of obesity. However, adherence to these behavioral changes is poor, with an increased reliance on synthetic drugs, which unfortunately are plagued by adverse effects.

Membrane selection and optimisation of tangential flow ultrafiltration of Cyclopia genistoides extract for benzophenone and xanthone enrichment.

Ultrafiltration of Cyclopia genistoides extract was optimised to increase its benzophenone and xanthone content as quantified using HPLC-DAD. Regenerated cellulose (RC) and polyethersulphone membranes with molecular weight cut-offs of 10 and 30 kDa were evaluated in terms of compound enrichment, permeate flux and permeate yield, using dead-end ultrafiltration. Compound enrichment was subsequently optimised using the 10 kDa RC membrane and tangential flow ultrafiltration (TFU).

Cyclopia Extracts Enhance Th1-, Th2-, and Th17-type T Cell Responses and Induce Foxp3+ Cells in Murine Cell Culture.

, one of the traditional South African medicinal plants, and other species of the same genus offer noteworthy phenolic profiles, in particular high levels of the anti-allergic xanthone mangiferin. Hot water and 40% ethanol-water (v/v) extracts, prepared from , and were tested for immune-regulating activity using murine splenocytes and mesenteric lymph node cells. The 40% ethanol-water extracts of significantly enhanced production of several types of cytokines, including IL-4, IL-17, and IFN-, by antigen-stimulated splenocytes.

Polyphenol-Enriched Fractions of Cyclopia intermedia Selectively Affect Lipogenesis and Lipolysis in 3T3-L1 Adipocytes.

species are increasingly investigated as sources of phenolic compounds with potential as therapeutic agents. Recently, we demonstrated that a crude polyphenol-enriched organic fraction (CPEF) of , currently forming the bulk of commercial production, decreased lipid content in 3T3-L1 adipocytes and inhibited body weight gain in obese db/db mice. The aim of the present study was to determine whether a more effective product and/or one with higher specificity could be obtained by fractionation of the CPEF by purposely increasing xanthone and benzophenone levels.

Intestinal transport and absorption of bioactive phenolic compounds from a chemically characterized aqueous extract of Athrixia phylicoides.

Ethnopharmacological Relevance: Athrixia phylicoides, popularly known as "bush tea", is an indigenous aromatic shrub found in mountainous and grassland areas of the northern and eastern parts of southern Africa. The plant is traditionally used for the treatment of several ailments, including coughing, treating infected wounds, treating boils and sore throat, hypertension and heart disease. Potential anti-diabetic effects have also been demonstrated in vitro.

Potential of rooibos, its major C-glucosyl flavonoids, and Z-2-(β-D-glucopyranosyloxy)-3-phenylpropenoic acid in prevention of metabolic syndrome.

Risk factors of type 2 diabetes mellitus (T2D) and cardiovascular disease (CVD) cluster together and are termed the metabolic syndrome. Key factors driving the metabolic syndrome are inflammation, oxidative stress, insulin resistance (IR), and obesity. IR is defined as the impairment of insulin to achieve its physiological effects, resulting in glucose and lipid metabolic dysfunction in tissues such as muscle, fat, kidney, liver, and pancreatic β-cells.

Isolation of aspalathin and nothofagin from rooibos (Aspalathus linearis) using high-performance countercurrent chromatography: sample loading and compound stability considerations.

Aspalathin and nothofagin, the major dihydrochalcones in rooibos (Aspalathus linearis), are valuable bioactive compounds, but their bioactivity has not been fully elucidated. Isolation of these compounds using high-performance countercurrent chromatography (HPCCC), a gentle, support-free, up-scalable technique, offers an alternative to synthesis for obtaining sufficient amounts. An HPLC-DAD method was adapted to allow rapid (16 min from injection to injection) quantification of the four major compounds (aspalathin, nothofagin, isoorientin, orientin) during development of the isolation protocol.

Benzophenone C- and O-glucosides from Cyclopia genistoides (Honeybush) inhibit mammalian α-glucosidase.

An enriched fraction of an aqueous extract prepared from the aerial parts of Cyclopia genistoides Vent. yielded a new benzophenone di-C,O-glucoside, 3-C-β-d-glucopyranosyl-4-O-β-d-glucopyranosyliriflophenone (1), together with small quantities of a known benzophenone C-glucoside, 3-C-β-d-glucopyranosylmaclurin (2). The isolated compounds showed α-glucosidase inhibitory activity against an enzyme mixture extracted from rat intestinal acetone powder.

Modeling of the total antioxidant capacity of rooibos (Aspalathus linearis) tea infusions from chromatographic fingerprints and identification of potential antioxidant markers.

Models to predict the total antioxidant capacity (TAC) of rooibos tea infusions from their chromatographic fingerprints and peak table data (content of individual phenolic compounds), obtained using HPLC with diode array detection, were developed in order to identify potential antioxidant markers. Peak table data included the content of 12 compounds, namely phenylpyruvic acid-2-O-glucoside, aspalathin, nothofagin, isoorientin, orientin, ferulic acid, quercetin-3-O-robinobioside, vitexin, hyperoside, rutin, isovitexin and isoquercitrin. The TAC values, measured using the oxygen radical absorbance capacity (ORAC) and DPPH radical scavenging assays, could be predicted from the peak table data or the chromatographic fingerprints (prediction errors 9-12%) using partial least squares (PLS) regression.

Iriflophenone-3-C-glucoside from Cyclopia genistoides: isolation and quantitative comparison of antioxidant capacity with mangiferin and isomangiferin using on-line HPLC antioxidant assays.

The benzophenone, iriflophenone-3-C-glucoside, was isolated from Cyclopia genistoides using a combination of fluid-fluid extraction, high performance counter-current chromatography (HPCCC) and semi-preparative high performance liquid chromatography (HPLC). The microplate oxygen radical absorbance capacity (ORAC) assay, with fluorescein as probe, was adapted for use in an on-line HPLC configuration. The method was validated using a mixture of authentic standards including iriflophenone-3-C-glucoside, and the xanthones, mangiferin and isomangiferin.

Food ingredient extracts of Cyclopia subternata (Honeybush): variation in phenolic composition and antioxidant capacity.

Cyclopia subternata plants are traditionally used for the production of the South African herbal tea, honeybush, and recently as aqueous extracts for the food industry. A C. subternata aqueous extract and mangiferin (a major constituent) are known to have anti-diabetic properties.

Occurrence and sensory perception of Z-2-(β-d-glucopyranosyloxy)-3-phenylpropenoic acid in rooibos (Aspalathus linearis).

Z-2-(β-d-glucopyranosyloxy)-3-phenylpropenoic acid (PPAG), a compound postulated to contribute to the taste and mouthfeel of fermented rooibos tea (Aspalathus linearis), was isolated from unfermented rooibos plant material. Its structure was unequivocally confirmed by LC-MS, -MS(2), FT-IR and NMR of the underivatised natural product, and optical rotation measurements of the hydrolysed sugar moiety. A similar compound, postulated to be E-2-(β-d-glucopyranosyloxy)-3-phenylpropenoic acid, was also detected.

Variation in phenolic content and antioxidant activity of fermented rooibos herbal tea infusions: role of production season and quality grade.

Data are required to calculate the dietary exposure to rooibos herbal tea flavonoids and phenolic acids. Representative content values for the principal phenolic compounds and total antioxidant capacity of fermented rooibos infusion, taking into account variation caused by production seasons (2009, 2010, and 2011) and quality grades (A, B, C, and D), were determined for samples (n = 114) from different geographical areas and producers. The major phenolic constituents were isoorientin and orientin (>10 mg/L), with quercetin-3-O-robinobioside, phenylpyruvic acid glucoside, and aspalathin present at >5 mg/L.

Development of on-line high performance liquid chromatography (HPLC)-biochemical detection methods as tools in the identification of bioactives.

Biochemical detection (BCD) methods are commonly used to screen plant extracts for specific biological activities in batch assays. Traditionally, bioactives in the most active extracts were identified through time-consuming bio-assay guided fractionation until single active compounds could be isolated. Not only are isolation procedures often tedious, but they could also lead to artifact formation.

Mangiferin glucuronidation: important hepatic modulation of antioxidant activity.

Mangiferin displays an extensive spectrum of pharmacological properties, including antioxidant activity. Its phase II metabolism in the presence of Aroclor 1254-induced and un-induced microsomal and cytosolic fractions from rat liver and the antioxidant potency of the glucuronidated conjugates were investigated. Mangiferin was not a substrate for the cytosolic sulphotransferases.

Phenylethanoid glycosides as major antioxidants in Lippia multiflora herbal infusion and their stability during steam pasteurisation of plant material.

Lippia multiflora, a perennial, aromatic shrub commonly known as bush tea has recently been identified as an African plant with high commercial potential due to its medicinal properties. The plant material was subjected to steam pasteurisation to improve its microbial quality. The major compounds of L.

Use of countercurrent chromatography during isolation of 6-hydroxyluteolin-7-O-β-glucoside, a major antioxidant of Athrixia phylicoides.

Athrixia phylicoides, an indigenous South African herbal tea, has potential as a source of nutraceutical antioxidant extracts. Countercurrent chromatography (CCC) was employed as part of a multi-step process to isolate one of the major antioxidant compounds in A. phylicoides extracts.

Use of green rooibos (Aspalathus linearis) extract and water-soluble nanomicelles of green rooibos extract encapsulated with ascorbic acid for enhanced aspalathin content in ready-to-drink iced teas.

Heat-induced changes in aspalathin, iso-orientin, and orientin content of ready-to-drink (RTD) green rooibos iced tea formulations were investigated. An organic-solvent-based aspalathin-enriched extract prepared from green rooibos was used "as-is" or encapsulated with ascorbic acid in a water-soluble nanomicelle-based carrier system. The common iced tea ingredients, ascorbic acid, and/or citric acid were added to the iced tea containing green rooibos extract.

In vitro hepatic biotransformation of aspalathin and nothofagin, dihydrochalcones of rooibos (Aspalathus linearis), and assessment of metabolite antioxidant activity.

Aspalathin (2',3,4,4',6'-pentahydroxy-3'-C-beta-d-glucopyranosyldihydrochalcone) is the major flavonoid present in the South African herbal tea rooibos. In vitro metabolism of aspalathin and a structural analogue nothofagin, lacking the A ring catechol group, was investigated by monitoring the formation of glucuronyl and sulfate conjugates using Aroclor 1254 induced and uninduced rat liver microsomal and cytosolic subcellular fractions. Following glucuronidation of both aspalathin and nothofagin, HPLC-DAD, LC-MS, and LC-MS/MS analyses indicated the presence of two metabolites: one major and one minor.