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Polysaccharide from Aspalathus linearis with strong anti-HIV activity.

Polysaccharide that has been extracted with 1% sodium carbonate from Rooibos leaves (Aspalathus linearis) showed strong anti-HIV activity. Du-Zhong leaves also showed anti-HIV activity, although lower than the extract of Aspalathus linearis, but Japanese tea leaves and a hot water extract of Aspalathus linearis did not. The anti-HIV activity of the alkaline extract from Aspalathus linearis was recovered mainly in the 25-75% ethanol-precipitated fraction. The polysaccharide almost completely inhibited the binding of HIV-1 to MT-4 cells. It is inferred from these results that the polysaccharide from Aspalathus linearis is involved in the mechanism for virus binding to T cells.

Anti-HIV Agents↗

Antioxidant activity and protective effect on DNA strand scission of Rooibos tea (Aspalathus linearis).

Rooibos tea (Aspalathus linearis) was extracted by refluxing with water and 75% ethanol as a solvent. Antioxidant activity and protective effect on DNA strand scission were investigated by using different antioxidant assay systems and DNA strand nicking assay, respectively. 75% Ethanol extract has higher content of total soluble phenolics and flavonoid than water extract. Antioxidant activities such as hydrogen donating capacity and scavenging activity of hydrogen peroxide were higher in 75% ethanol extract than in water extract except the rate constant with hydroxyl radical. Peroxyl radical induced DNA strand scission was prevented by both 75% ethanol and water extract and hydroxyl radical induced DNA strand scission was not. This result indicates that total soluble phenolics, specially flavonoid, of Rooibos tea are responsible for several kinds of antioxidant activities and preventive activity on peroxyl radical induced DNA strand scission.

Antioxidants↗

A review of the bioactivity of South African herbal teas: rooibos (Aspalathus linearis) and honeybush (Cyclopia intermedia).

Rooibos (Aspalathus linearis) and honeybush (Cyclopia intermedia) are popular tisanes in their native South Africa and have a growing worldwide market. Both herbal teas are used traditionally for medicinal purposes and are rich in polyphenols with rooibos a rare source of the dietary dihydrochalcones, aspalathin and nothofagin. The principal polyphenols in honeybush include the xanthone mangiferin and the flavonones hesperitin and isokuranetin. Despite their divergent phytochemical and nutrient compositions, rooibos and honeybush share potent antioxidant and antimutagenic activities in vitro. Animal model studies indicate both herbal teas possess potent antioxidant, immune-modulating and chemopreventive actions. However, human studies of rooibos are limited and of honeybush are absent. No adverse effects of rooibos or honeybush consumption as tisanes have been reported.

Animals↗

Selective bronchodilatory effect of Rooibos tea (Aspalathus linearis) and its flavonoid, chrysoeriol.

BACKGROUND: Rooibos tea (Aspalathus linearis) is commonly used for hyperactive gastrointestinal, respiratory and cardiovascular disorders. AIM OF STUDY: The aqueous extract of Rooibos tea (RT) was studied for the possible bronchodilator, antispasmodic and blood pressure lowering activities in an attempt to rationalize some of its medicinal uses. METHODS: Isolated tissue preparations, such as rabbit jejunum, aorta and guinea-pig trachea and atria were set up in appropriate physiological salt solutions and aerated with carbogen. For in vivo studies rats were anesthetized with pentothal sodium and blood pressure was measured through carotid artery cannulation. RESULTS: In jejunum, RT caused a concentration-dependent relaxation of low K(+) (25 mM)-induced contractions, with mild effect on the contractions induced by high K(+) (80 mM). In presence of glibenclamide, the relaxation of low K(+)-induced contractions was prevented. Similarly, cromakalim caused glibenclamide-sensitive inhibition of low K(+), but not of high K(+), while verapamil did not differentiate in its inhibitory effect on contractions produced by the two concentrations of K(+). Like in jejunum, RT caused glibenclamide-sensitive relaxation of low K(+)-induced contractions in trachea and aorta, but with a 20 times higher potency in trachea. In atria, RT was least potent with weak inhibitory effect on atrial force and rate of contractions. RT caused a dose-dependent fall in arterial blood pressure in rats under anesthesia. Among the tested pure compounds of Rooibos, chrysoeriol showed selective bronchodilator effect. Chrysoeriol (luteolin 3'-methyl ether) is a bioactive flavonoid known for antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities. CONCLUSION: These results indicate that the bronchodilator, antispasmodic and blood pressure lowering effects of Rooibos tea are mediated predominantly through K(ATP) channel activation with the selective bronchodilatory effect. This study provides a sound mechanistic basis for the wide medicinal use of Rooibos tea, with the therapeutic potential to be developed for congestive respiratory ailments.

Animals↗

Inhibition of tumour promotion in mouse skin by extracts of rooibos (Aspalathus linearis) and honeybush (Cyclopia intermedia), unique South African herbal teas.

The modulating effect of ethanol/acetone (E/A) soluble fractions, prepared from methanolic extracts of processed and unprocessed rooibos (Aspalathus linearis) and honeybush (Cyclopia intermedia) as well as green (Camellia sinensis) teas was established in a two-stage mouse skin carcinogenesis assay. Topical application of the tea fractions prior to the tumour promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA), on ICR mouse skin initiated with 7,12-dimethylbenz[a]anthracene (DMBA) suppressed skin tumorigenesis significantly (P<0.001) with the green tea E/A fraction exhibiting a 100% inhibition, unprocessed honeybush 90%, processed honeybush 84.2%, processed rooibos 75% and unprocessed rooibos 60%. The green tea fraction, with the highest flavanol/proanthocyanidin content, also exhibited the highest protective activity (99%) against hepatic microsomal lipid peroxidation, and completely inhibited skin tumour formation. Differences in the flavanol/proanthocyanidin and flavonol/flavone composition and/or non polyphenolic constituents are likely to be important determinants in the inhibition of tumour promotion by the herbal tea E/A fractions in mouse skin.

Animals↗

A comparative study on the antimutagenic properties of aqueous extracts of Aspalathus linearis (rooibos), different Cyclopia spp. (honeybush) and Camellia sinensis teas.

Antimutagenic activity of aqueous extracts of the South African herbal teas, Aspalathus linearis (rooibos) and Cyclopia spp. (honeybush) was compared with that of Camellia sinensis (black, oolong and green) teas in the Salmonella mutagenicity assay using aflatoxin B(1) (AFB(1)) and 2-acetylaminofluorene (2-AAF) as mutagens. The present study presents the first investigation on antimutagenic properties of C. subternata, C. genistoides and C. sessiliflora. The herbal teas demonstrated protection against both mutagens in the presence of metabolic activation, with the exception of "unfermented" (green/unoxidised) C. genistoides against 2-AAF, which either protected or enhanced mutagenesis depending on the concentration. Antimutagenic activity of "fermented" (oxidised) rooibos was significantly (P<0.05) less than that of Camellia sinensis teas against AFB(1), while for 2-AAF it was less (P<0.05) than that of black tea and similar (P>0.05) to that of oolong and green teas. Antimutagenic activity of unfermented C. intermedia and C. subternata exhibited a similar protection as fermented rooibos against AFB(1). Against 2-AAF, fermented rooibos exhibited similar protective properties than unfermented C. intermedia and C. sessiliflora. Unfermented rooibos was less effective than the C. sinensis teas and fermented rooibos, but had similar (P>0.05) antimutagenicity to that of fermented C. sessiliflora against AFB(1) and fermented C. subternata against 2-AAF. Fermented C. intermedia and C. genistoides exhibited the lowest protective effect against 2-AAF, while fermented C. intermedia exhibited the lowest protection when utilising AFB(1) as mutagen. Aspalathin and mangiferin, major polyphenols in rooibos and Cyclopia spp., respectively, exhibited weak to moderate protective effects when compared to the major green tea catechin, (-)epigallocatechin gallate (EGCG). Antimutagenic activity of selected herbal tea phenolic compounds indicated that they contribute towards (i) observed antimutagenic activity of the aqueous extracts against both mutagens and (ii) enhancement of the mutagenicity of 2-AAF by unfermented C. genistoides. Antimutagenic activity of the South African herbal teas was mutagen-specific, affected by fermentation and plant material, presumably due to changes and variation in phenolic composition.

2-Acetylaminofluorene↗

In situ flavonoid analysis by FT-Raman spectroscopy: identification, distribution, and quantification of aspalathin in green rooibos (Aspalathus linearis).

FT-Raman spectroscopy was used for the first time for in situ identification of aspalathin and quantification of the dihyrochalcones in dried, green rooibos (Aspalathus linearis). With the support of two-dimensional correlation spectroscopy, characteristic key bands of aspalathin, the main flavonoid and antioxidant occurring in rooibos, were localized and identified in the spectra obtained from various plant samples. Application of Raman mapping revealed the spatial distribution of this valuable dihydrochalcone within the intact dried leaves. Based on the spectral data and reference HPLC values, reliable multivariate calibration models were developed for quantification of aspalathin, nothofagin, and the combined dihydrochalcone contents of dried, green rooibos.

Antioxidants↗

Phytoestrogens from Aspalathus linearis.

From the leaves of Aspalathus linearis, 24 known compounds and a new one, aspalalinin (25), were isolated. The structures of the compounds were determined mainly based on spectral evidence. The absolute configuration of aspalalinin was presented on the basis of X-ray analysis. Each isolate was assessed for its estrogenic activity by an estrogen ELISA assay. Compounds 12, 15, and 24 showed the estrogenic activity.

Aspalathus↗

Hepatoprotective effect of rooibos tea (Aspalathus linearis) on CCl4-induced liver damage in rats.

Hepatoprotective properties of rooibos tea (Aspalathus linearis) were investigated in a rat model of liver injury induced by carbon tetrachloride (CCl(4)). Rooibos tea, like N-acetyl-L-cysteine which was used for the comparison, showed histological regression of steatosis and cirrhosis in the liver tissue with a significant inhibition of the increase of liver tissue concentrations of malondialdehyde, triacylglycerols and cholesterol. Simultaneously, rooibos tea significantly suppressed mainly the increase in plasma activities of aminotransferases (ALT, AST), alkaline phosphatase and billirubin concentrations, which are considered as markers of liver functional state. The antifibrotic effect in the experimental model of hepatic cirrhosis of rats suggests the use of rooibos tea as a plant hepatoprotector in the diet of patients with hepatopathies.

Acetylcysteine↗

Regeneration of coenzyme Q9 redox state and inhibition of oxidative stress by Rooibos tea (Aspalathus linearis) administration in carbon tetrachloride liver damage.

The effect of rooibos tea (Aspalathus linearis) on liver antioxidant status and oxidative stress was investigated in rat model of carbon tetrachloride-induced liver damage. Synthetic antioxidant N-acetyl-L-cysteine (NAC) was used for comparison. Administration of carbon tetrachloride (CCl4) for 10 weeks decreased liver concentrations of reduced and oxidized forms of coenzyme Q9 (CoQ9H2 and CoQ9), reduced -tocopherol content and simultaneously increased the formation of malondialdehyde (MDA) as indicator of lipid peroxidation. Rooibos tea and NAC administered to CCl4-damaged rats restored liver concentrations of CoQ9H2 and alpha-tocopherol and inhibited the formation of MDA, all to the values comparable with healthy animals. Rooibos tea did not counteract the decrease in CoQ9, whereas NAC was able to do it. Improved regeneration of coenzyme Q9 redox state and inhibition of oxidative stress in CCl4-damaged livers may explain the beneficial effect of antioxidant therapy. Therefore, the consumption of rooibos tea as a rich source of natural antioxidants could be recommended as a market available, safe and effective hepatoprotector in patients with liver diseases.

Acetylcysteine↗

Inhibitory effects of Rooibos tea, Aspalathus linealis, on X-ray-induced C3H10T1/2 cell transformation.

Oncogenic transformation of mouse C3H10T1/2 cells induced by X-rays was suppressed in the presence of extract of Rooibos tea, Aspalathus linealis. Transformation was reduced with increased concentration of the extract, so that at an extract concentration of 10%, transformation incidence was similar to the spontaneous level. Suppression was also dependent on treatment time with the extract and was maximal when present during the entire incubation period. In contrast, green tea extract at an equitoxic concentration showed no detectable effect on transformation incidence.

Animals↗

The suppression of age-related accumulation of lipid peroxides in rat brain by administration of Rooibos tea (Aspalathus linearis).

The protective effects of Rooibos tea (RT), Aspalathus linearis, against damage to the central nervous system (CNS) accompanying aging were examined by both the thiobarbituric acid reaction (TBA) and magnetic resonance imaging (MRI) methods in brains of chronically RT-treated rats. Ad libitum administration of RT was begun with 3-month-old Wistar female rats and continued for 21 months. The contents of TBA reactive substances (TBARS) in the frontal cortex, occipital cortex, hippocampus and cerebellum in 24-month-old rats after administration with water were significantly higher than those in young rats (5 weeks old). However, no significant increase of TBARS was observed in RT-administered aged rats. When MR images of the brains of 24-month-old rats with and without RT as well as 5-week-old rats were taken, a decrease of the signal intensity was observed in the cerebral cortex, hippocampus and cerebellum in MR images of aged rats without RT, whereas little change of the signal intensity was observed in MR images of the same regions of 24-month-old rats treated with RT, whose images were similar to those of young rats. These observations suggested that (1) the age-related accumulation of lipid peroxides in the brain was closely related to the morphological changes observed by MRI, and (2) chronic RT-administration prevented age-related accumulation of lipid peroxides in several regions of rat brain.

Administration, Oral↗

Quantitative characterization of flavonoid compounds in Rooibos tea (Aspalathus linearis) by LC-UV/DAD.

Rooibos tea originates from the leaves and stems of the indigenous South African plant Aspalathus linearis. It has gained much attention for clinical purposes in the case of nervous tension, allergies (dermatitis), and various indigestive problems. Recently, antioxidative activity was also attributed to the tea on the basis of its flavonoid content. Therefore, an HPLC method using a C(18) reversed phase column was developed for the assay of 10 flavonoids in aqueous and methanolic infusions. Main compounds determined were the dihydrochalcone aspalthin, rutin, and orientin, and their content was in the range of 1.0 to 1.3 mg/g. The identity of detected flavonoids was confirmed by comparing their retention times and UV and MS spectra with those of corresponding standards. In addition, the MS analysis showed evidence of the presence of other compounds such as nothofagin, dihydroisoorientin, and dihydroorientin.

Beverages↗

Anti-human immunodeficiency virus activity of oligosaccharides from rooibos tea (Aspalathus linearis) extracts in vitro.

The active substances, acid polysaccharides, were extracted with 1% sodium hydroxide from the leaves of rooibos tea (Aspalathus linearis), Du Zhong Cha (Eucommia ulmoides Oliv.) and Japanese tea leaves (Camellia sinensis var. sinensis). The alkaline extracts of Rooibos tea and Du-Zhong tea leaves, but not Japanese tea leaves suppressed the HIV-induced cytopathicity using HIV (HTLV-III) infected MT-4 cells, having extremely low cytotoxicity: Its 50% effective concentration (EC50) was 12-67 micrograms/mL, white 50% cytotoxic concentration (CC50) was higher than 1.0 mg/mL. The active substances were purified with ethanol precipitation. The substances were composed of 27% of reducing sugar, 46% of neutral sugars and 22% of uronic acid. A LD50 of the alkaline extracts from rooibos tea was higher than 1.2 g/kg body weight. Acid degradated substances composed of disaccharides and trisaccharides, were also suppressed the HIV-induced cytopathicity. From these results, it is probable that acid polysaccharides from rooibos tea were extremely safe, and that HIV infection may be suppressed by daily intake of the alkaline extracts of rooibos tea and Du-Zhong tea.

Anti-HIV Agents↗

Modulation of hepatic drug metabolizing enzymes and oxidative status by rooibos (Aspalathus linearis) and Honeybush (Cyclopia intermedia), green and black (Camellia sinensis) teas in rats.

Rooibos and honeybush teas significantly (P < 0.05) enhanced the activity of cytosolic glutathione S-transferase alpha. A significant (P < 0.05) to marginal (P < 0.1) increase in the activity of the microsomal UDP-glucuronosyl transferase was obtained with unprocessed rooibos and honeybush teas, respectively. Oxidized glutathione (GSSG) levels were significantly (P < 0.05) reduced in the liver of all tea treated rats while reduced glutathione (GSH) was markedly increased in the liver of the herbal tea treated rats. These changes resulted in a significant (P < 0.05) increase in the GSH/GSSG ratio by the unprocessed, processed rooibos and unprocessed honeybush teas. Green and black teas markedly to significantly decreased the oxygen radical absorbance capacity in liver homogenates, respectively. Modulation of phase II drug metabolizing enzymes and oxidative status in the liver may be important events in the protection against adverse effects related to mutagenesis and oxidative damage.

Animals↗

Antioxidant and pro-oxidant activities of aqueous extracts and crude polyphenolic fractions of rooibos (Aspalathus linearis).

Unfermented rooibos tea is known to contain higher levels of total polyphenols and flavonoids than its fermented counterpart, making it the obvious choice for the preparation of flavonoid-enriched fractions. Evaluation of aqueous extracts and crude polyphenolic fractions of unfermented and fermented rooibos showed anti- and/or pro-oxidant activities, using a linoleic acid-Tween-buffer emulsion for lipid peroxidation and the deoxyribose degradation assay, based on a Fenton reaction model system containing FeCl3-EDTA and H2O2 for the generation of hydroxyl radicals. Except for the ethyl acetate fraction, with the highest total polyphenol (TP) content and offering the least protection presumably due to pro-oxidant activity, the inhibition of lipid peroxidation by the samples correlated moderately with their TP content in a linear relationship (r = 0.896, P < 0.01). Using the deoxyribose degradation assay, the pro-oxidant activity of the aqueous extracts and their crude polymeric fractions (0.1 mg/mL in the reaction mixture) was linear with respect to their dihydrochalcone (aspalathin and nothofagin) (r = 0.977, P = 0.023) and flavonoid (r = 0.971, P = 0.029) content. Pro-oxidant activity was demonstrated for pure aspalathin. Using the same assay, but with ascorbate added to regenerate Fe3+ to Fe2+, the aqueous extract and crude polymeric fraction of fermented rooibos displayed hydroxyl radical scavenging activity. Fermentation (i.e., oxidation) of rooibos decreased the pro-oxidant activity of aqueous extracts, which was contributed to a decrease in their dihydrochalcone content. The in vitro pro-oxidant activity displayed by flavonoid-enriched fractions of rooibos demonstrates that one must be aware of the potential adverse biological properties of potent antioxidant extracts utilized as dietary supplements.

Antioxidants↗