Effect of herbal extract Eurycoma longifolia (Physta®) on female reproductive hormones and bone biochemical markers: an ovariectomised rat model study.

BACKGROUND: Each year 1.5 million women experience menopause when menstrual cycles cease resulting from the loss of ovarian function and oestrogen deprivation, a hormone that helps prevent bone loss. This study investigated the effects of Physta®, a standardized herbal extract of Eurycoma longifolia Jack (PEL), on hormonal balance and parameters associated with hormonal imbalance, namely body and uterus weight and bone biochemical markers relevant in menopausal symptoms. METHODS: Forty-eight Sprague Dawley rats were randomly divided into six groups of eight rats each: (A) Sham operated; control (B) Untreated (ovariectomised (OVX) with vehicle), (C) PEL 100 (OVX + 100 mg/kg body weight (bw)), (D) PEL 300 (OVX + 300 mg/kg bw), (E) PEL 500 (OVX + 500 mg/kg bw) and (F) Positive control, testosterone undecanoate (TU) (OVX+ 10 mg/kg bw). Group A and B received daily oral administrations of the vehicle, Group C-E received daily oral administration of PEL and Group F received testosterone undecanoate intramuscularly weekly. At the end of 8 weeks, serum calcium, phosphate, bone alkaline phosphatase (BALP), osteocalcin, follicle stimulating hormone (FSH), luteinising hormone (LH), oestrogen, progesterone and testosterone were measured, then the animals were sacrificed and uterus was isolated, while weight was recorded in all experimental groups. RESULTS: Treatment of OVX rats with PEL at a dose of 500 mg/kg showed decreased serum FSH (P < 0.001, 4.25 ± 0.22 mIU/ml) and LH (NS, 4.07 ± 0.12 mIU/ml), while there was a significant increase in progesterone (P < 0.05, 2.48 ± 0.08 ng/ml) and oestrogen (P < 0.05, 11.02 ± 0.13 pg/ml) levels when compared to untreated group. PEL treatment at doses of 100 mg/kg, 300 mg/kg and 500 mg/kg showed a non-significant but increasing trend in serum calcium, phosphate, bone alkaline phosphate and testosterone levels. Ovariectomy resulted in a significant reduction (P < 0.001, 238.81 ± 5.39 mg) in uterus weight in the ovariectomised rats, which was alleviated in all PEL treated ovariectomised rats with an increasing trend of uterine weight. CONCLUSION: The results suggest that PEL could be protective and beneficial for the management of reproductive hormone and bone markers. Therefore, it could be used to address hormonal imbalances and symptoms associated with menopause.

Momordica cymbalaria fruit extract attenuates high-fat diet-induced obesity and diabetes in C57BL/6 mice.

OBJECTIVES: The present study was aimed to evaluate the effect of methanolic fruit extract of Momordica cymbalaria (MeMC) against high-fat diet-induced obesity and diabetes in C57BL/6 mice. MATERIALS AND METHODS: In the present study, six weeks old male C57BL/6 mice were divided into four groups. G-1 and G-2 served as lean control and HFD control, G-3 and G-4 received MeMC 25 and 50 mg/kg, BW doses; all the treatments were given for a period of 11 weeks. The parameters such as body weight, fasting blood glucose, insulin, cholesterol, free fatty acid, and oral glucose tolerance tests were performed, further, at the end of the study fasting body weight, and weights of organs such as the liver, heart, and adipose tissue were measured and the liver tissue was subjected to histopathology evaluation, and insulin resistance was expressed as HOMA-IR index. RESULTS: The high-fat diet fed C57 mice showed significant elevation of body weight (P<0.01), blood glucose (P<0.01), insulin (P<0.01), cholesterol (P<0.01), free fatty acid (P<0.01), and HOMA-IR index (P<0.01) along with significant elevation of all organ weights and reduction in oral glucose tolerance (P<0.01) and brown adipose weight (P<0.01). The histopathology showed significant fatty infiltration and hypertrophy of hepatocytes. Interestingly, MeMC (50 mg/kg) alleviated all the HFD-induced perturbances significantly. Further, the HPLC analysis of MeMC revealed the presence of gallic acid and rutin as chief ingredients. CONCLUSION: MeMC possesses potent antidiabetic activity and ameliorates insulin resistance in HFD diet fed C57 mice.

Evaluation of anti-epileptic activity of leaf extracts of Punica granatum on experimental models of epilepsy in mice.

OBJECTIVES: This study was aimed to examine the anti-epileptic activity of leaf extracts of Punica granatum in experimental models of epilepsy in Swiss albino mice. MATERIALS AND METHODS: Petroleum ether leaf extract of P. granatum (PLPG), methanolic LPG (MLPG), and aqueous LPG (ALPG) extracts of P. granatum leaves was initially evaluated against 6-Hz-induced seizure model; the potent extract was further evaluated against maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions. Further, the potent extract was evaluated for its influence on Gamma amino butyric acid (GABA) levels in brain, to explore the possible mechanism of action. In addition, the potent extract was subjected to actophotometer test to assess its possible locomotor activity deficit inducing action. RESULTS: In 6-Hz seizure test, the MLPG has alleviated 6-Hz-induced seizures significantly and dose dependently at doses 50, 100, 200, and 400 mg/kg. In contrast, PLPG and ALPG did not show any protection, only high dose of ALPG (400 and 800 mg/kg, p.o.) showed very slight inhibition. Based on these observations, only MLPG was tested in MES and PTZ models. Interestingly, the MLPG (50, 100, 200 and 400 mg/kg) has offered significant and dose-dependent protection against MES (P < 0.01) and PTZ-induced (P < 0.01) seizures in mice. Further, MLPG showed a significant increase in brain GABA levels (P < 0.01) compared to control and showed insignificant change in locomotor activity in all tested doses (100, 200 and 400 mg/kg). Interestingly, higher dose of MLPG (400 mg/kg, p.o.) and Diazepam (5 mg/mg, p.o.) have completely abolished the convulsions in all the anticonvulsant tests. CONCLUSION: These findings suggest that MLPG possesses significant anticonvulsant property, and one of the possible mechanisms behind the anticonvulsant activity of MLPG may be through enhanced GABA levels in the brain.

Methanolic leaf extract of Gymnema sylvestre augments glucose uptake and ameliorates insulin resistance by upregulating glucose transporter-4, peroxisome proliferator-activated receptor-gamma, adiponectin, and leptin levels in vitro.

AIMS: The present study was undertaken to evaluate the effect of methanolic leaf extract of Gymnema sylvestre (MLGS) on glucose transport (GLUT) and insulin resistance in vitro. MATERIALS AND METHODS: Peroxisome proliferator-activated receptor-gamma (PPAR-γ) and GLUT-4 expression were assessed in L6 myotubes for concluding the GLUT activity, and adiponectin and leptin expression was studied in 3T3 L1 murine adipocyte cell line to determine the effect of MLGS (250-750 µg/ml) on insulin resistance. RESULTS: The findings of the experiments have demonstrated a significant and dose-dependent increase in glucose uptake in all the tested concentrations of MLGS, further the glucose uptake activity of MLGS (750 µg/ml) was at par with rosiglitazone (50 µg/ml). Concomitantly, MLGS has shown enhanced GLUT-4 and PPAR-γ gene expressions in L6 myotubes. Furthermore, cycloheximide (CHX) had completely abolished the glucose uptake activity of MLGS when co-incubated, which further confirmed that glucose uptake activity of MLGS was linked to enhanced expression of GLUT-4 and PPAR-γ. In addition, in another experimental set, MLGS showed enhanced expression of adiponectin and leptin, thus confirms the ameliorative effect of MLGS on insulin resistance. CONCLUSION: These findings suggest that MLGS has an enhanced glucose uptake activity in L6 myotubes, and ameliorate the insulin resistance in 3T3 L1 murine adipocyte cell line in vitro.

Methanolic extract of Momordica cymbalaria enhances glucose uptake in L6 myotubes in vitro by up-regulating PPAR-γ and GLUT-4.

The present study was undertaken to evaluate the influence of the methanolic fruit extract of Momordica cymbalaria (MFMC) on PPARγ (Peroxisome Proliferator Activated Receptor gamma) and GLUT-4 (Glucose transporter-4) with respect to glucose transport. Various concentrations of MFMC ranging from 62.5 to 500 µg·mL(-1) were evaluated for glucose uptake activity in vitro using L6 myotubes, rosiglitazone was used as a reference standard. The MFMC showed significant and dose-dependent increase in glucose uptake at the tested concentrations, further, the glucose uptake activity of MFMC (500 µg·mL(-1)) was comparable with rosigilitazone. Furthermore, MFMC has shown up-regulation of GLUT-4 and PPARγ gene expressions in L6 myotubes. In addition, the MFMC when incubated along with cycloheximide (CHX), which is a protein synthesis inhibitor, has shown complete blockade of glucose uptake. This indicates that new protein synthesis is required for increased GLUT-4 translocation. In conclusion, these findings suggest that MFMC is enhancing the glucose uptake significantly and dose dependently through the enhanced expression of PPARγ and GLUT-4 in vitro.

Investigation of the Antioxidant and Hepatoprotective Potential of Hypericum mysorense.

BACKGROUND: Hypericum is a well-known plant genus in herbal medicine. Hypericum mysorense (Family: Hypericaceae), a plant belonging to the same genus, is well known in folklore medicine for its varied therapeutic potential. OBJECTIVE: The aim of the present study was to investigate the different parts of the plant for antioxidant and hepatoprotective properties. MATERIALS AND METHODS: The methanol extracts of Hypericum mysorense prepared from various parts of the plant were tested in vitro for their free radical scavenging activity against ABTS(•) (diammonium salt), DPPH(•) (1,1-diphenyl-2-picrylhydrazyl), NO(•), O2(•-) and (•)OH radicals, using standard systems of assays. The total antioxidant capacity, total phenolic and total flavonoid content of the extracts were analyzed. Further, the leaf and flowering top extracts were tested for their in vivo antioxidant and hepatoprotective activities on Wistar rats using a carbon tetrachloride-induced hepatic injury model. RESULTS: The leaf and flowering top extract showed potent antioxidant activity and also possessed highest total phenolic and flavonoid content. The antioxidant activity and the total phenolic and flavonoid content present in these extracts showed a good correlation. The leaf and flowering top extracts at 200 mg/kg restored aspartate amino transferase (ASAT), alanine amino transferase (ALAT), alkaline phosphatase (ALP), total bilirubin and protein levels significantly in CCl4-intoxicated rats. The tested extracts also showed a significant (p < 0.001) reduction in 2-thiobarbituric acid reactive substance (TBARS) levels with an increase in SOD and CAT levels. The histopathology of liver did not show any toxicity after the treatment with the extracts. The active extracts were standardized using two marker compounds, hyperoside and rutin, which were isolated from the plant by HPLC. HPLC studies revealed that the maximum concentration of hyperoside and rutin is present in the flowering top extract.

Evaluation of antioxidant, in vitro cytotoxicity of micropropagated and naturally grown plants of Leptadenia reticulata (Retz.) Wight & Arn.-an endangered medicinal plant

OBJECTIVE@#To evaluate the antioxidant and anti proliferative potential of different solvent extract of micropropagated and naturally grown plants of Leptadenia reticulata against various cancer cell lines.@*METHODS@#In this study different extract were tested for cytotoxicity against human breast adenocarcinoma cell line MCF-7, human colon adenocarcinoma grade II cell line HT-29 and non cancer skeletal muscle cell line L6 through 3-(4, 5-dimethyl thiazol-2-yl)-5-diphenyl tetrazolium bromide assay. The total antioxidant potential was estimated by three different antioxidant model diphenylpicrylhydrazyl free radical scavenging activity, H2O2 scavenging activity and FeCl3 reducing activity.@*RESULTS@#The ethyl acetate extract of both naturally grown plant and tissue cultured plant exhibited significant cytotoxicity with IC50 values of 21 µg/mL, 26 µg/mL and 22 µg/mL; 20 µg/mL, 30 µg/mL and 18 µg/mL respectively against three cell lines. The diphenylpicrylhydrazyl free radical scavenging activity was found to be highest with IC50 value of 267.13 µg/mL in ethyl acetate extract. The methanolic extract exhibited moderate antioxidant activity with IC50 value of 510.15 µg/mL. A highly positive correlation was observed between the antioxidant potential and cytotoxic activity of the plant.@*CONCLUSIONS@#The strong cytotoxicity of ethyl acetate extract revealed anti carcinogenic potential of the plant which supports its traditional use as medicine. The present investigation is new to literature till date and will provide better scientific basis for future pharmacological, in vivo studies and novel source of pure bioactive compounds having anti cancer properties in this plant.

Evaluation of antioxidant, in vitro cytotoxicity of micropropagated and naturally grown plants of Leptadenia reticulata (Retz.) Wight & Arn.-an endangered medicinal plant

Objective: To evaluate the antioxidant and anti proliferative potential of different solvent extract of micropropagated and naturally grown plants of Leptadenia reticulata against various cancer cell lines. Methods: In this study different extract were tested for cytotoxicity against human breast adenocarcinoma cell line MCF-7, human colon adenocarcinoma grade II cell line HT-29 and non cancer skeletal muscle cell line L6 through 3-(4, 5-dimethyl thiazol-2-yl)-5-diphenyl tetrazolium bromide assay. The total antioxidant potential was estimated by three different antioxidant model diphenylpicrylhydrazyl free radical scavenging activity, H