Assessment of preclinical effect of (+)-catechin hydrate on sexual function: An in silico and in vivo study.

Considering dopamine-enhancing effect of (+)-catechin, the present study was designed to evaluate dopamine-2 (D2) receptor agonistic and phosphodiesterase-5 (PDE5) enzyme inhibitory effects in in silico and effect on male sexual function of Sprague Dawley rats in vivo. (+)-Catechin and standard (sildenafil and bromocriptine) were docked using Autodock Vina 1.1.2 and visualised by UCSF Chimera 1.14. Significant interactions in terms of binding energies were observed for catechin with both proteins. In in vivo study, the rats were dosed orally for 54 days with (+)-catechin hydrate (50 mg/kg), sildenafil citrate (standard, 4 mg/kg) and carboxymethylcellulose (vehicle, 0.25% w/v). The aphrodisiac effects were evaluated on the day 14, 28, 42 and 54 using the behavioural parameters of mounting and intromission. After the study, animals were sacrificed and testes and spermatozoa were assessed for safety profile. Results showed a significant increase in mount and intromission frequencies and a significant reduction in mount and intromission latencies in the catechin group on all tested days when compared to vehicle control. (+)-Catechin was found to be safe on histology of testes, sperm count, sperm motility and sperm morphology parameters. In conclusion, catechin demonstrated an enhancement in sexual behaviour without eliciting toxicity on the male reproductive system in rats.

Evaluation of the aphrodisiac potential of a chemically characterized aqueous extract of Tamarindus indica pulp.

ETHNOPHARMACOLOGICAL RELEVANCE: Tamarindus indica is an ingredient in the traditional aphrodisiac formulations in Africa and India. It is also a widely used food ingredient in other tropical countries. AIM OF THE STUDY: The present study was aimed to evaluate the aphrodisiac potential and reproductive safety profile of aqueous extract of Tamarindus indica in male Wistar rats. MATERIALS AND METHODS: The aqueous extract was prepared by maceration of pulp followed by reduction of volume in rotavapor under heat followed by freeze drying. The prepared extract was characterized for contents of total phenol, flavonoid, and saponin. It was also subjected to phytoconstituent analysis using GCMS. Further, the extract was evaluated for acute toxicity study. The aphrodisiac and reproductive toxicity potential were evaluated in animals after grouping them in four with six animals each namely, normal control, standard (Sildenafil citrate, 4mg/kg p.o.) and extract of Tamarindus indica treated groups at two dose levels, 125 and 250mg/kg p.o. The study was conducted for 54 days with daily once dosing of extract and standard. Equal number of females was grouped without treatment for evaluation of parameters of sexual desire (mount frequency and intromission frequency) and parameters of sexual arousal (mount latency and intromission latency). These parameters were evaluated on day 14, 28, 42 and 54. Animals were sacrificed on day 54, testes were removed and studied for histopathological changes. RESULTS: The extract showed 6.6mg gallic acid equivalent/g of total phenol, 2.3mg catechin equivalent/g of flavonoid and 11.6% saponin. Forty chemical constituents were identified by GCMS analysis. In acute toxicity study, the extract was found to be safe till 2000mg/kg p.o. Efficacy study showed significant (p<0.05) improvement in parameters of sexual desire (mount frequency and intromission frequency) and parameters of sexual arousal on all observed days except mount frequency for 125mg/kg on 42nd day and intromission frequency for both doses of tamarind compared to normal control. Improvements in these parameters were comparable to the standard drug. Histopathology study and sperm count suggested an increase in sperm production without any sign of toxicity in testis. Sperm motility significantly (p<0.05) increased in the treatment groups that received extract at 250mg/kg compared to normal control. CONCLUSION: Aqueous extract of Tamarindus indica possessed aphrodisiac activity together with spermatogenic potential.

Anti-osteoporotic activity of the petroleum ether extract of Cissus quadrangularis Linn. in ovariectomized Wistar rats.

BACKGROUND: The plant Cissus quadrangularis (CQ) is used as an osteoprotective agent in Ayurveda, the Indian system of alternative medicine. The present study was done to validate the anti-osteoporotic role of the petroleum ether extract of CQ on ovariectomy-induced osteoporosis in rats. METHODS: Female wistar rats were divided into five groups of six rats each; (1) The Normal control (NC) group (n=6) received no surgery and no treatment, (2). The Sham control (SHAM) group (n=6) received sham surgery but no treatment, (3) the Ovariectomized (OVX) group (n=6) received an ovariectomy and normal saline treatment for 90 days, (4) the Ovariectomized+raloxifene (OVX+RAL) group (n=6) received an ovariectomy and treatment with raloxifene, a known anti-osteoporotic agent for 90 days commencing from 22nd post ovariectomy day and (5) the Ovariectomy+Cissus quadrangularis (OVX+CQ) group (n=6) received an ovariectomy, and treatmentwith the petroleum ether extract of CQ 500 mg/kg body weight daily for 90 days commencing from 22nd post ovariectomy day. At the end of the treatment period, rats in all groups were sacrificed and the right femur was used for biomechanical analysis, and the left femur for histomorphometrical analysis. RESULTS: CQ significantly increased the force required to break the femur (p<0.001) and significantly increased the thickness of both cortical (p<0.001) and trabecular bone (p<0.001). This action of CQ was comparable to the action of raloxifene. CONCLUSIONS: The petroleum ether extract of CQ stem seems to possess anti-osteoporotic activity in rats.

Petroleum ether extract of Cissus quadrangularis (Linn.) enhances bone marrow mesenchymal stem cell proliferation and facilitates osteoblastogenesis.

OBJECTIVE: To evaluate the effects of the petroleum ether extract of Cissus quadrangularis on the proliferation rate of bone marrow mesenchymal stem cells, the differentiation of marrow mesenchymal stem cells into osteoblasts (osteoblastogenesis) and extracellular matrix calcification. This study also aimed to determine the additive effect of osteogenic media and Cissus quadrangularis on proliferation, differentiation and calcification. METHODS: MSCs were cultured in media with or without Cissus quadrangularis for 4 weeks and were then stained for alkaline phosphatase. Extracellular matrix calcification was confirmed by Von Kossa staining. marrow mesenchymal stem cells cultures in control media and osteogenic media supplemented with Cissus quadrangularis extract (100, 200, 300 microg/mL) were also subjected to a cell proliferation assay (MTT). RESULTS: Treatment with 100, 200 or 300 microg/mL petroleum ether extract of Cissus quadrangularis enhanced the differentiation of marrow mesenchymal stem cells into ALP-positive osteoblasts and increased extracellular matrix calcification. Treatment with 300 microg/mL petroleum ether extract of Cissus quadrangularis also enhanced the proliferation rate of the marrow mesenchymal stem cells. Cells grown in osteogenic media containing Cissus quadrangularis exhibited higher proliferation, differentiation and calcification rates than did control cells. CONCLUSION: The results suggest that Cissus quadrangularis stimulates osteoblastogenesis and can be used as preventive/ alternative natural medicine for bone diseases such as osteoporosis.

Petroleum ether extract of Cissus quadrangularis (Linn. ) enhances bone marrow mesenchymal stem cell proliferation and facilitates osteoblastogenesis

OBJECTIVE: To evaluate the effects of the petroleum ether extract of Cissus quadrangularis on the proliferation rate of bone marrow mesenchymal stem cells, the differentiation of marrow mesenchymal stem cells into osteoblasts (osteoblastogenesis) and extracellular matrix calcification. This study also aimed to determine the additive effect of osteogenic media and Cissus quadrangularis on proliferation, differentiation and calcification. METHODS: MSCs were cultured in media with or without Cissus quadrangularis for 4 weeks and were then stained for alkaline phosphatase. Extracellular matrix calcification was confirmed by Von Kossa staining. marrow mesenchymal stem cells cultures in control media and osteogenic media supplemented with Cissus quadrangularis extract (100, 200, 300 µg/mL) were also subjected to a cell proliferation assay (MTT). RESULTS: Treatment with 100, 200 or 300 µg/mL petroleum ether extract of Cissus quadrangularis enhanced the differentiation of marrow mesenchymal stem cells into ALP-positive osteoblasts and increased extracellular matrix calcification. Treatment with 300 µg/mL petroleum ether extract of Cissus quadrangularis also enhanced the proliferation rate of the marrow mesenchymal stem cells. Cells grown in osteogenic media containing Cissus quadrangularis exhibited higher proliferation, differentiation and calcification rates than did control cells. CONCLUSION: The results suggest that Cissus quadrangularis stimulates osteoblastogenesis and can be used as preventive/alternative natural medicine for bone diseases such as osteoporosis.

Petroleum ether extract of Cissus quadrangularis (LINN) stimulates the growth of fetal bone during intra uterine developmental period: a morphometric analysis.

OBJECTIVE: The aim of the present study was to analyze the effect Cissus quadrangularis plant petroleum ether extract on the development of long bones during the intra-uterine developmental stage in rats. METHODS: Pregnant rats (n=12) were randomly assigned into either a control group (n=6) or a Cissus quadrangularis treatment (n=6) group. Pregnant rats in the Cissus quadrangularis group were treated with Cissus quadrangularis petroleum ether extract at a dose of 500 mg/kg body weight from gestation day 9 until delivery. The animals in the control group received an equal volume of saline. Newborn pups were collected from both groups for alizarin red S - alcian blue staining to differentiate ossified and unossified cartilage. The ossified cartilage (bone) was morphometrically analyzed using Scion image software. RESULTS: Morphometric analysis revealed that the percentage of the total length of ossified cartilage (bone) in pups born to treated dams was significantly higher (P<0.001- -0.0001) than that of the control group. CONCLUSION: The results of the present study suggest that maternal administration of Cissus quadrangularis petroleum ether extract during pregnancy can stimulate the development of fetal bone growth during the intra-uterine developmental period.

Assessment of hypolipidaemic activity of three thiazolidin-4-ones in mice given high-fat diet and fructose.

Three 4-thiazolidinones, two with nicotinamide (NAT1 and NAT2) and one with 4-chlorophenoxyacetamide (PAT1) side chains were evaluated for their hypolipidaemic, hypoglycaemic activity in Swiss albino mice fed a high-fat diet along with fructose administered in drinking water. NAT1 and PAT caused reduction of elevated triglycerides, cholesterol and glucose; NAT2 was effective only against triglycerides. Nicotinamide side chain might have contributed to the lipid lowering effect of both NAT1 and NAT2, but the bulky group of the latter could have affected proper binding to the receptor sites, making it ineffective against elevated cholesterol. On the other hand, the 4-chlorophenoxyacetamide side chain of PAT might have exerted powerful hypolipidaemic activity, despite the bulky substitution at C2. As antioxidants, NAT2 and PAT1 showed superior activity, compared to NAT1. The thiazolidinone ring might be responsible for the lipid lowering effect, which is however, modified by the type of substitutions at C2 and N of the ring. Detailed study is warranted to explain the mechanism of action of these compounds as also to make more potent ones.

Petroleum ether extract of Cissus quadrangularis (LINN) stimulates the growth of fetal bone during intra uterine developmental period: a morphometric analysis

OBJECTIVE: The aim of the present study was to analyze the effect Cissus quadrangularis plant petroleum ether extract on the development of long bones during the intra-uterine developmental stage in rats. METHODS: Pregnant rats (n=12) were randomly assigned into either a control group (n=6) or a Cissus quadrangularis treatment (n=6) group. Pregnant rats in the Cissus quadrangularis group were treated with Cissus quadrangularis petroleum ether extract at a dose of 500 mg/kg body weight from gestation day 9 until delivery. The animals in the control group received an equal volume of saline. Newborn pups were collected from both groups for alizarin red S - alcian blue staining to differentiate ossified and unossified cartilage. The ossified cartilage (bone) was morphometrically analyzed using Scion image software. RESULTS: Morphometric analysis revealed that the percentage of the total length of ossified cartilage (bone) in pups born to treated dams was significantly higher (P<0.001- -0.0001) than that of the control group. CONCLUSION: The results of the present study suggest that maternal administration of Cissus quadrangularis petroleum ether extract during pregnancy can stimulate the development of fetal bone growth during the intra-uterine developmental period.