Cytotoxicity and antihyperglycemic effect of minor constituents from Rhizoma Coptis in HepG2 cells

Generally, berberine, coptisine, palmatine, and jatrorrhizine were considered as the main bio-active compounds in Rhizoma Coptis (RC). Little attention was paid to investigate the pharmacological activity of minor constituents in RC. The present study was designed to separate the minor compounds, and the cytotoxicity and antihyperglycemic effect of these compounds in HepG2 cells were also studied. Palmatine (1), berberine (2), coptisine (3), epiberberine (4), columbamine (5), and jatrorrhizine (6) from RC ethanol extract were isolated by high speed counter current chromatography (HSCCC) in one run. The remaining fraction (about 50% of extract in HSCCC) was further isolated by traditional column chromatography methods to yield magnoflorine (7), ferulic acid (8), and choline (9). Another four alkaloids, namely groenlandicine (10), berberrubine (11), oxyberberine (12), 8-oxo-coptisine (13), also were obtained from CHCl₃ extracts. Especially, choline was first isolated from RC. Cell assay indicated that the minor fractions excluding compounds 1-6 showed obvious glucose lowering activity. In addition, the minor monomers also exhibited moderate glucose lowering activity. The combination of berberine and ferulic acid showed synergistic effect on antihyperglycemic. The combination of alkaloids 1-6 was same so. All compounds had different cytotoxicity in HepG2 cells within the test concentration. Of them, berberrubine showed the strongest cytotoxicity. The results suggested that combined action of variety constituents contributed to the antihyperglycemic effets and low cytotoxicity of RC extract in HepG2 cells.     

Should Anacardium humile St. Hil be used as an antiulcer agent? A scientific approach to the traditional knowledge

The crude methanolic extract (ME) obtained from the leaves of Anacardium humile was evaluated orally at doses of 250-500-1000 mg/kg on gastric lesion on ethanol and piroxicam induced gastric lesions in rodents. All the tested doses significantly inhibited gastric lesions by 56 to 100%. These results seems to support the traditional use of this species in the treatment of gastric diseases.     

Antihyperglycemic activity of the aqueous extract of Urtica dioica

When administered 30 min before glucose loading, the aqueous extract of Urtica dioica (nettle) (250 mg/kg) showed a strong glucose lowering effect. The decrease of glycemia has reached to 33+/-3.4% of the control value 1 h after glucose loading. This effect was persistent during 3 h. In contrast, nettle did not show hypoglycemic effect in alloxan-induced diabetic rats. The amount of glucose absorbed in a segment jejunum in situ was 8.05+/-0.68 mg in presence of nettle extract vs. 11.11+/-0.75 mg in control rats during 2 h (P<0.05). The results indicate that nettle has a significant antihyperglycemic effect in OGTT model. This effect may be caused in part by the reduction of intestinal glucose absorption. LD(50) is 3.5 g/kg (i.p.).     

Antidiabetic properties of aqueous barks extract of Parinari excelsa in alloxan-induced diabetic rats

The aqueous extract of the Parinari excelsa barks at doses of 100 and 300 mg/kg/day for 7 days has a significant antihyperglycemic effect on alloxan-induced diabetic rats. At the same dose the acute oral administration of aqueous extract of the P. excelsa barks (100 and 300 mg/kg) induced a significant decrease of blood glucose on glucose-loaded normoglycaemic rats. Our results seem to confirm the rational bases for its use in traditional medicine.     

Anti-diabetic effect of American ginseng may not be linked to antioxidant activity: Comparison between American ginseng and Scutellaria baicalensis using an ob/ob mice model

Antioxidants have been considered as a useful remedy in diabetes therapeutics, and thus, herbal medicines with antioxidant properties may play major role in treating diabetes. In this report, we performed a comparative study using American ginseng and Scutellaria baicalensis to test whether the anti-diabetic effect of American ginseng is associated with its antioxidant activity. We used a simple water extraction procedure to prepare American ginseng root extract (AGE) and S. baicalensis extract (SbE), and utilized these two antioxidant herbs to evaluate their anti-diabetic effect in obese diabetic ob/ob mice. HPLC analysis was used to identify major constituents in the AGE and SbE. After 12 days of daily intraperitoneal injection, AGE at 300 mg/kg showed significant effects on fasting blood glucose levels (P < 0.01) and glucose tolerance test (P < 0.01) compared to vehicle-treated mice. Animal body weights also reduced significantly after 12-day treatment (P < 0.01). However, SbE, a very strong antioxidant extract, administered at 5–50 mg/kg (based on our previous studies without adverse events) for 12 days did not show any significant effects on blood glucose and body weight changes. No effects were shown when baicalein, an effective antioxidant constituent in SbE, was administered at 1–5 mg/kg. It appears that the anti-diabetic effect of American ginseng may not be linked to its antioxidant actions. The mechanisms of American ginseng's effects on reducing high blood glucose levels and body weight remain to be investigated in future experiments.     

Relaxant effect of aqueous extract of Cistus ladaniferus on rodent intestinal contractions

The effects of the aqueous extract of Cistus ladaniferus leaves and stems were studied on the rodent isolated jejunum. The extract produced a reversible concentration dose-dependent (0.1-3 mg/ml) inhibition of the spontaneous motility of the rabbit jejunum. The inhibitory effects of the extract were not affected by pretreatment with the inhibitors of the alpha and beta adrenergic receptors yohimbine, prazosin or propranolol. The extract also inhibited K(+)-induced contractions in rabbit and rat jejunum at a similar concentration range. This result suggests that the antispasmodic action of the extract is mediated through calcium channel blockade. The results confirm the traditional use of C. ladaniferus in treating intestinal ache.     

Hypoglycemic effect of Mucuna pruriens seed extract on normal and streptozotocin-diabetic rats

The hypoglycemic effect of the aqueous extract of the seeds of Mucuna pruriens was investigated in normal, glucose load conditions and streptozotocin (STZ)-induced diabetic rats. In normal rats, the aqueous extract of the seeds of Mucuna pririens (100 and 200 mg/kg body weight) significantly (P<0.001) reduced the blood glucose levels after an oral glucose load from 127.5+/-3.2 to 75.6+/-4.8 mg% 2 h after oral administration of seed extract. It also significantly lowered the blood glucose in STZ diabetic rats from 240.5+/-7.2 to 90.6+/-5.6 mg% after 21 days of daily oral administration of the extract (P<0.001). Thus, this study shows that M. pruriens has an anti-hyperglycemic action and it could be a source of hypoglycemic compounds.     

Bioassay-guided isolation of an anti-ulcer chromene from Eupatorium aschenbornianum: Role of nitric oxide,prostaglandins and sulfydryls

Eupatorium aschenbornianum is considered useful in the treatment of gastric ulcer. In the current study the validity of this practice was tested by using the experimental model of an ethanol induced gastric ulcer in rats. The results show that E. aschenbornianum had gastroprotective activity, that the hexane extract had the highest protective activity (85.65 ± 4.76%), and that encecanescin isolated from this extract was the main active gastroprotective agent. The effect elicited by encecanescin was attenuated by N^G-nitro-l-arginine methyl ester, N-ethylmaleimide and indomethacin, which suggests that NO, prostaglandins and sulfydryl groups are involved in the mechanisms of gastroprotective action.     

Antidiabetic potential of Butea monosperma in rats

The antihyperglycemic activity of the ethanolic extract of Butea monosperma (BMEE) was studied in glucose-loaded and alloxan-induced diabetic rats. Single dose treatment of BMEE (200 mg/kg, p.o.) significantly improved glucose tolerance and caused reduction in blood glucose level in alloxan-induced diabetic rats. Repeated oral treatment with BMEE (200 mg/kg/day) for 2 weeks significantly reduced blood glucose, serum cholesterol and improved HDL-cholesterol and albumin as compared to diabetic control group.     

Anti-diabetic activity of flowers of Hibiscus rosasinensis

The ethanol extract of flowers of Hibiscus rosasinensis at doses of 250 mg/kg and 500 mg/kg significantly reduced the blood glucose level in both acute (1, 3, 5 h) and sub acute (1, 3, 5, 7 days) treatments.     

Hypoglycemic effect of Bauhinia cheilandra in rats

The extract of the methanolic leaves of Bauhinia cheilandra (BC) was tested on glucose loaded and alloxan-induced diabetic rats. In both tests, the methanolic extract at doses of 300, 600, and 900 mg/kg, has shown a statistically significant and considerable hypoglycemic activity.     

Compositional analysis and in vivo anti-diabetic activity of wild Algerian Marrubium vulgare L. infusion

Marrubium vulgare (Lamiaceae) is a plant traditionally used for the treatment of diabetes in Algeria. Compositional analysis of the aqueous infusion revealed the presence of fifteen metabolites, all belonging to the class of polyphenols. Particularly, seven flavonoids have been detected, together with 5-caffeoylquinic (chlorogenic) acid in small amounts; the extract is dominated by the presence of a series of complex molecules, characterized as verbascoside (acteoside) derivatives. Concerning the anti-diabetic effectiveness a series of in vivo experiments were carried out on albinos Wistar rats. Diabetes was induced in the animals by intra-peritoneal injection of alloxane; they were treated twice a day with aqueous extract from aerial part infusion (100, 200 and 300 mg/kg body weight) and glibenclamide (5mg/kg body weight) for 15 days. Oral administration of 200 and 300 mg/kg body weight of aqueous extract the Marrubium vulgare induced an significant effect antidiabetic and antihyperlipidemic (dose-dependent effect). A decrease in blood glucose by 50% for the dose 100 mg/kg and more than 60% for doses 200 and 300 mg/kg, as well as a significant lowering of total lipids, triglycerides, and total cholesterol levels in treated animals, compared with diabetic controls group (p<0.001), have been observed. Glibenclamide was used as reference and showed similar effects.     

Anti-hyperglycemic action of apigenin-6-C-β-fucopyranoside from Averrhoa carambola

A stimulatory effect of apigenin-6-C-β-fucopyranoside (1) on glucose uptake was observed when rat soleus muscle was incubated with 1, 10 and 100μM of this flavonoid glycoside. The presence of specific insulin signaling inhibitors, such as wortmannin, an inhibitor of phosphoinositide 3-kinase (PI3K), RO318220, an inhibitor of protein kinase C (PKC), PD98059, an inhibitor of mitogen-activated protein kinase (MEK), and HNMPA(AM)(3), an insulin receptor tyrosine kinase activity inhibitor showed that apigenin-6-C-β-fucopyranoside triggers different metabolic pathways in skeletal muscle. The oral administration of crude extract, fractions and isolated flavonoids (apigenin-6-C-β-fucopyranoside (1) and apigenin-6-C-(2″-O-α-rhamnopyranosyl)-β-fucopyranoside (2)) from Averrhoa carambola leaves exhibited a potential hypoglycemic activity in hyperglycemic normal rats. Additionally, both flavonoids significantly increased the muscle and liver glycogen content after an acute treatment. The results indicate that A. carambola can be regarded as a potent antihyperglycemic agent with insulin secretagogue and insulin mimetic properties.     

Type 2 antidiabetic activity of bergenin from the roots of Caesalpinia digyna Rottler

Bergenin, a major constituent of Caesalpinia digyna Rottler (Leguminosae) was isolated from its roots and was characterized by comparing its melting point and spectroscopic data (IR, (1)H, (13)C, Mass Spectra) with standard bergenin. Isolated bergenin was then evaluated for antidiabetic (Type 2) activity in streptozotocin (STZ)-nicotinamide induced diabetic rats. Bergenin was administered at doses of 2.5, 5, and 10 mg/kg; p.o. to normal rats which were subjected to oral glucose tolerance test (OGTT). Bergenin at same dose level was given to diabetic rats and fasting blood glucose level was estimated on 0th, 7th and 14th day of treatment while plasma lipids, antioxidant enzymes and liver glycogen level in diabetic rats were estimated on 14th day of treatment followed by histopathological studies of pancreas. Bergenin at 10mg/kg; p.o. was found to reduce blood glucose level significantly in OGTT (P<0.01) while it showed a significant reduction in fasting blood glucose level in diabetic rats at same dose level only on 14th day of treatment. Bergenin in all dose levels reversed plasma lipid (reduced elevated TC, LDL-C and increased HDL-C level) profile to normal values except TG. However, bergenin showed no significant effect on liver glycogen at all dose level. The decrease in lipid peroxides and increase in superoxide dismutase (SOD) and catalase (CAT) in liver illustrated the antioxidant potential of bergenin. Histopathological studies demonstrated the regenerative effect of bergenin on pancreatic β cells. Hence, bergenin isolated from C. digyna possesses significant antidiabetic, hypolipidemic and antioxidant activity in Type 2 diabetic rats.     

Stimulation of gastric acid secretion and intestinal motility by Vernonia amygdalina extract

Aqueous extract of Vernonia amygdalina infused intragastrically at a dose of 10 mg/ml to rats induced a significant increase in acid output which was reduced by, ranitidine (5 mg/kg b.w.) or atropine (1.2 microMol/kg b.w.). Moreover the extract evoked a dose-dependent contraction of the guinea pig ileum at a dose range of 0.6 mg/ml to 66 mg/ml which was inhibited by atropine (2.4 x 10(-8)-2.4 x 10(-6) M).     

Contractile effect of the aqueous extract of Psidium guajava leaves on aortic rings in rat

Aqueous leaves extract of Psidium guajava significantly and dose-dependently (0.25-2 mg/ml) contracted aorta rings. The effect was evaluated also in presence of nifedipine and phentolamine. The sensitivity of the aortic rings to cumulative doses of P. guajava was significantly enhanced in the presence of phentolamine suggesting that the effect of P. guajava was to a large extent mediated by activation of alpha-adrenoceptor and to a lesser extent by acting via calcium ion channel.     

Neuroprotective effect of methanolic extracts of Allium cepa on ischemia and reperfusion-induced cerebral injury

The present study is designed to investigate the effect of methanolic extract of outer scales and edible portions of Allium cepa bulb on ischemia and reperfusion-induced cerebral injury. Global cerebral ischemia was induced by bilateral carotid artery occlusion for 10 min followed by reperfusion for 24 h. Pretreatment with methanolic extract of outer scales (100 mg/kg and 200 mg/kg) and edible portions (100 mg/kg and 200 mg/kg) of A. cepa bulb markedly reduced cerebral infarct size and attenuated impairment in short-term memory and motor coordination. The protective effect of methanolic extract of outer scales and edible portions of A. cepa bulb was accompanied by a marked decrease in mitochondrial TBARS.     

Study on the antimicrobial activity of Hymatanthus sucuba

The antimicrobial activity of Hyamatantus sucuba roots methanol extract, fractions prepared from this extract (n-hexane, CHCl(3), EtOAc, and n-butanol) and some isolated compounds were evaluated against some Gram(+) and Gram(-) bacteria and yeasts.     

Four new neolignans from the leaves of Tripterygium wilfordii

Four new neolignans, wilfordiols A-D (1-4), together with five known compounds (5-9), were isolated from an aqueous extract of the dried leaves of Tripterygium wilfordii. Their structures were determined by spectroscopic methods, including 1D and 2D NMR, HRESIMS, and CD experiments. The anti-inflammation activities of compounds 1-9 were evaluated by the inhibitory effect on NO production, in vitro.     

Bioactive polar compounds from stem bark of Magnolia officinalis

Two new phenylethanoid glycosides magnoloside D (1) and E (2), together with nine known compounds, were isolated from the polar part of methanol extract of the stem bark of Magnolia officinalis. The structures of the new compounds were established on the basis of spectral analysis. Anti-spasmodic activity of four major constituents (3, 4, 9 and 11) was tested in isolated colon of rat, compounds 3, 4, and 9 showed inhibition against acetylcholine, with the effect similar to that of magnolol and honokiol. At the same time, antioxidant activity of the isolated compounds was investigated using a DPPH and an ORAC assay. All of the compounds, except compound 8 showed potent antioxidant capacity in the ORAC assay, while compounds 1-5 and 11 exhibited potent antioxidant activity in the DPPH assay.