Inhibitory effects of aqueous extract of Hibiscus sabdariffa on contractility of the rat bladder and uterus

We examined an aqueous extract of Hibiscus sabdariffa calyces extracts (HSE) by close-arterial injection on micturition thresholds (MTs) and on uterine contractions (rate and amplitude). Five doses of HSE were examined (1, 5, 10, 50, and 100 mg/kg) in 3 groups of rats: controls, after bladder inflammation, and after bilateral hypogastric neurectomy. In some rats, uterine contractions were induced by injection of oxytocin (OT) and the effect of HSE was compared with that of nifedipine. HSE increased MTs in a dose-dependent manner in all groups. Neither atropine (0.1 mg/kg) nor propranolol (0.4 mg/kg) had significant effects on cystometric parameters. They also did not affect the responses obtained by HSE on cystometric parameters. As with bladder response, HSE inhibited both the rate and amplitude of uterine contractions in all groups in a dose-dependent manner. The uterine response to HSE was not affected by administration of either atropine or propranolol. A slight, but significant, reduction of contraction amplitude by HSE in the OT precontracted uteri was only noted at a dose of 500 mg/kg. Nifedipine was more potent than HSE in reducing uterine contraction amplitude. The present work documents inhibition by HSE of the rat bladder and uterine contractility in a dose-dependent manner via a mechanism unrelated to local or remote autonomic receptors or calcium channels. However, further investigation is needed to establish the exact mechanism of action.

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The effect of deer antler from East Kalimantan to increase trabecular bone density and calcium levels in serum on osteoporotic mice

Journal of Basic and Clinical Physiology and Pharmacology ◽

10.1515/jbcpp-2020-0140 ◽

2021 ◽

Vol 0 (0) ◽

Author(s):

Retno Widyowati ◽

Suciati Suciati ◽

Dewi Melani Haryadi ◽

Hsin-I Chang ◽

IPG Ngurah Suryawan ◽

...

Keyword(s):

Bone Density ◽

Trabecular Bone ◽

Aqueous Extract ◽

Dependent Manner ◽

Aqueous Extracts ◽

Trabecular Bone Density ◽

Male Mice ◽

Deer Antler ◽

East Kalimantan ◽

Dose Dependent

Abstract Objectives Glucocorticoid-induced osteoporosis (dexamethasone) is a primary cause of secondary osteoporosis by the decreasing formation and increasing resorption activities. Previously, the in vitro study showed that 70% ethanol and aqueous extract of deer antler have increased alkaline phosphatase in osteoblast cell that known as marker of bone formation. The mind of this study is to analyze the effect of deer antlers in increasing the bone trabecular density of osteoporosis-induced male mice. Methods This study used a post-test control group design. A total of 54 healthy male mice were randomly divided to nine groups, i.e., healthy control, osteoporotic, positive control, 70% ethanol (4, 8, and 12 mg/kg BW), and aqueous extracts (4, 8, and 12 mg/kg BW) of deer antler groups. All of the interventions were given 1 mL of test sample for 4 weeks orally. The bone densities were determined using histomorphometry by Image J and Adobe Photoshop. The statistical data were performed using SPSS 23 and statistical significance was set at p<0.05. Results The results showed that alendronate group, 70% ethanol, and aqueous extract groups increased bone density and calcium levels in serum (p<0.05) compared to osteoporotic group in dose dependent manner. It indicated that 70% ethanol and aqueous extract of deer antler stimulating bone turnover and aqueous extract showed the highest. Conclusions Dexamethasone induction for 4 weeks caused osteoporotic mice and the administration of 70% ethanol and aqueous extracts of deer antler from East Kalimantan increased trabecular bone density and calcium levels in dose dependent manner.

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HEPATOPROTECTIVE EVALUATION OF EPALTES DIVARICATA (L.) CASS. WHOLE PLANT EXTRACTS AGAINST PARACETAMOL-INDUCED HEPATOTOXICITY IN RATS

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2016v8i12.14951 ◽

2016 ◽

Vol 8 (12) ◽

pp. 231 ◽

Cited By ~ 1

Author(s):

K. Amala ◽

R. Ilavarasan ◽

R. Arunadevi ◽

S. Amerjothy

Keyword(s):

Aqueous Extract ◽

Histopathological Examination ◽

Hepatoprotective Activity ◽

Hepatoprotective Effect ◽

Dependent Manner ◽

Traditional Use ◽

Whole Plant ◽

Medicinal Use ◽

Histopathological Studies ◽

Dose Dependent

Objective: The plant of Epaltes divaricata (L.) Cass. Traditionally used for jaundice. The present work aimed to investigate the hepatoprotective activity of alcohol and aqueous extract of the whole plant against paracetamol-induced hepatotoxicity in rats to substantiate its traditional use.Methods: The alcohol and aqueous (200 and 400 mg/kg) extract of Epaltes divaricata prepared by cold maceration were administered orally to the animals with hepatotoxicity induced by paracetamol (1000 mg/kg). Silymarine (40 mg/k) was given as reference standard. Hepatoprotective activity was assessed by estimating marker enzymes and by histopathological studies.Results: Both alcohol and aqueous (200 and 400 mg/kg) extract treatment significantly restored the paracetamol-induced elevations in levels of serum enzymes aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphate (ALP) and total bilirubin in a dose-dependent manner. Histopathological examination revealed that the treatment attenuated the paracetamol-induced damage to the liver. The hepatoprotective effect of both extracts was comparable to that of the standard hepatoprotective agent, silymarin.Conclusion: The alcohol and aqueous extract of E. divaricata exhibited hepatoprotective effect against paracetamol-induced liver damage in rats. This study also validated their traditional medicinal use in jaundice.

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Activation of Phosphatidylinositol-Linked Novel D1 Dopamine Receptors Inhibits High-Voltage-Activated Ca2+ Currents in Primary Cultured Striatal Neurons

Journal of Neurophysiology ◽

10.1152/jn.90345.2008 ◽

2009 ◽

Vol 101 (5) ◽

pp. 2230-2238 ◽

Cited By ~ 8

Author(s):

Li-Qun Ma ◽

Chao Liu ◽

Fang Wang ◽

Na Xie ◽

Jun Gu ◽

...

Keyword(s):

Dopamine Receptor ◽

High Voltage ◽

Dependent Manner ◽

Striatal Neurons ◽

Inhibitory Effects ◽

Patch Clamp Technique ◽

Whole Cell Patch Clamp ◽

Intracellular Ca ◽

Dose Dependent

Recent evidences indicate the existence of a putative novel phosphatidylinositol (PI)-linked D1 dopamine receptor that mediates excellent anti-Parkinsonian but less severe dyskinesia action. To further understand the basic physiological function of this receptor in brain, the effects of a PI-linked D1 dopamine receptor-selective agonist 6-chloro-7,8-dihydroxy-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine (SKF83959) on high-voltage activated (HVA) Ca2+ currents in primary cultured striatal neurons were investigated by whole cell patch-clamp technique. The results indicated that stimulation by SKF83959 induced an inhibition of HVA Ca2+ currents in a dose-dependent manner in substance-P (SP)-immunoreactive striatal neurons. Application of D1 receptor, but not D2, α1 adrenergic, 5-HT receptor, or cholinoceptor antagonist prevented SKF83959-induced reduction, indicating that a D1 receptor-mediated event assumed via PI-linked D1 receptor. SKF83959-induced inhibitory modulation was mediated by activation of phospholipase C (PLC), mobilization of intracellular Ca2+ stores and activation of calcineurin. Furthermore, the inhibitory effects were attenuated significantly by the L-type calcium channel antagonist nifedipine, suggesting that L-type calcium channels involved in the regulation induced by SKF83959. These findings may help to further understand the functional role of the PI-linked dopamine receptor in brain.

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The Effects of Salacia reticulata on Anti-Cellular Oxidants and Melanogenesis Inhibition in α-MSH-stimulated and UV Irradiated B16 Melanoma Cells

Natural Product Communications ◽

10.1177/1934578x1400900433 ◽

2014 ◽

Vol 9 (4) ◽

pp. 1934578X1400900

Author(s):

Prasit Sirwannalert ◽

Ryusho Kariya ◽

Ikuko Suzu ◽

Seiji Okada

Keyword(s):

Melanoma Cells ◽

Pharmaceutical Products ◽

B16 Melanoma ◽

Tyrosinase Activity ◽

Root Extract ◽

Dependent Manner ◽

Inhibitory Effects ◽

B16 Melanoma Cells ◽

Dose Dependent ◽

Salacia Reticulata

The purposes of this study were to investigate the inhibitory effects of Salacia reticulata Tul. root extract on cellular oxidants and melanogenesis in B16 melanoma cells. Cells treated with non-toxic doses of S. reticulata root extract were investigated for their effects on melanogenesis, cellular tyrosinase activity and cellular oxidant scavenging activity. The results indicated that S. reticulata extract inhibited melanin synthesis and tyrosinase activity in α-MSH-induced or UV-irradiated B16 melanoma cells in a dose dependent manner. Additionally, the extract also exhibited anti-cellular oxidants in UV-induced radical melanoma cells. Altogether, these results suggested that S. reticulata root extract has roles in suppression of melanogenesis and oxidant inhibition. S. reticulata root extract may be a potential source for the development of pharmaceutical products for treatment of skin hyperpigmentation disorders.

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Interaction between perchlorate and nifedipine on insulin secretion from mouse pancreastic islets

Bioscience Reports ◽

10.1007/bf01145963 ◽

1993 ◽

Vol 13 (2) ◽

pp. 107-117 ◽

Cited By ~ 6

Author(s):

Gerd Larsson-Nyrén ◽

Janove Sehlin

Keyword(s):

Insulin Secretion ◽

Insulin Release ◽

Specific Effect ◽

Maximum Effect ◽

Dependent Manner ◽

Inhibitory Effects ◽

Maximum Inhibition ◽

Second Phases ◽

Dose Dependent ◽

Higher Sensitivity

In order to elucidate the mechanisms responsible for the stimulatory effect of perchlorate (ClO4−) on insulin secretion, we have investigated the interaction between this chaotropic anion and the organic calcium antagonist nifedipine. This drug, known as a blocker of L-type calcium channels, was chosen as a tool to test the idea that ClO4− acts on insulin secretion by stimulating the gating of voltage-controlled Ca2+ channels. ClO4− amplified the stimulatory effect of D-glucose on insulin release from perfused pancreas (first and second phases) as well as from isolated islets incubated in static incubations for 60 min. This indicates that ClO4− amplifies physiologically regulated insulin secretion. Nifedipine reduced D-glucose-induced (20 mM) insulin release in a dose-dependent manner with half-maximum effect at about 0.8 μM and apparent maximum effect at 5 μM nifedipine. In the presence of 20 mM D-glucose, the inhibitory effects of 0.5, 1 or 5 μM nifedipine were only slightly, if at all, counteracted by perchlorate. When 12 mM ClO4− and 20 mM D-glucose were combined, calculation of the specific effect of ClO4− revealed that nifedipine produced almost maximum inhibition already at 0.05 μM. Thus, the perchlorate-induced amplification of D-glucose-stimulated insulin release shows higher sensitivity to nifedipine than the D-glucose-effect as such. This supports the hypothesis that perchlorate primarily affects the voltage-sensitive L-type calcium channel in the β-cell.

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Towards Al3+-Induced Manganese-Containing Superoxide Dismutase Inactivation and Conformational Changes: An Integrating Study with Docking Simulations

Enzyme Research ◽

10.4061/2011/307464 ◽

2011 ◽

Vol 2011 ◽

pp. 1-7

Author(s):

Jiang-Liu Yang ◽

Shang-Jun Yin ◽

Yue-Xiu Si ◽

Zhi-Rong Lü ◽

Xiangrong Shao ◽

...

Keyword(s):

Superoxide Dismutase ◽

Conformational Changes ◽

Tertiary Structure ◽

Kinetic Studies ◽

Computational Prediction ◽

Enzyme Inactivation ◽

Dependent Manner ◽

Inhibitory Effects ◽

Docking Simulations ◽

Dose Dependent

Superoxide dismutase (SOD, EC 1.15.1.1) plays an important antioxidant defense role in skins exposed to oxygen. We studied the inhibitory effects of Al3+ on the activity and conformation of manganese-containing SOD (Mn-SOD). Mn-SOD was significantly inactivated by Al3+ in a dose-dependent manner. The kinetic studies showed that Al3+ inactivated Mn-SOD follows the first-order reaction. Al3+ increased the degree of secondary structure of Mn-SOD and also disrupted the tertiary structure of Mn-SOD, which directly resulted in enzyme inactivation. We further simulated the docking between Mn-SOD and Al3+ (binding energy for Dock 6.3: −14.07 kcal/mol) and suggested that ASP152 and GLU157 residues were predicted to interact with Al3+, which are not located in the Mn-contained active site. Our results provide insight into the inactivation of Mn-SOD during unfolding in the presence of Al3+ and allow us to describe a ligand binding via inhibition kinetics combined with the computational prediction.

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Kinetics of Mushroom Tyrosinase and Melanogenesis Inhibition byN-Acetyl-pentapeptides

The Scientific World JOURNAL ◽

10.1155/2014/409783 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 6

Author(s):

Ching-Yi Lien ◽

Ching-Yu Chen ◽

Shih-Ting Lai ◽

Chin-Feng Chan

Keyword(s):

Kojic Acid ◽

Lag Time ◽

Melanoma Cells ◽

Dependent Manner ◽

Mushroom Tyrosinase ◽

Inhibitory Effects ◽

B16f10 Melanoma ◽

B16f10 Melanoma Cells ◽

Kinetics Of ◽

Dose Dependent

We investigated the kinetics of 4N-acetyl-pentapeptides, Ac-P1, Ac-P2, Ac-P3, and Ac-P4, regarding inhibition of mushroom tyrosinase activity. The peptides sequences of Ac-P1, Ac-P2, Ac-P3, and Ac-P4 were Ac-RSRFK, Ac-KSRFR, Ac-KSSFR, and Ac-RSRFS, respectively. The 4N-acetyl-pentapeptides were able to reduce the oxidation ofL-DOPA by tyrosinase in a dose-dependent manner. Of the 4N-acetyl-pentapeptides, only Ac-P4 exhibited lag time (80 s) at a concentration of 0.5 mg/mL. The tyrosinase inhibitory effects of Ac-P4 (IC500.29 mg/mL) were more effective than those of Ac-P1, Ac-P2, and Ac-P3, in which IC50s were 0.75 mg/mL, 0.78 mg/mL, and 0.81 mg/mL, respectively. Kinetic analysis demonstrated that all 4N-acetyl-pentapeptides were mixed-type tyrosinase inhibitors. Furthermore, 0.1 mg/mL of Ac-P4 exhibited significant melanogenesis inhibition on B16F10 melanoma cells and was more effective than kojic acid. The melanogenesis inhibition of Ac-P4 was dose-dependent and did not induce any cytotoxicity on B16F10 melanoma cells.

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Possible Antioxidant and Haematinic Properties of the Stem Bark of Theobroma cacao L. in Wistar Rats

International Journal of Biochemistry Research & Review ◽

10.9734/ijbcrr/2021/v30i330256 ◽

2021 ◽

pp. 18-26

Author(s):

B. O. Oluwatayo ◽

T. A. Kolawole ◽

C. C. Wali ◽

O. A. Olayanju ◽

A. E. J. Okwori

Keyword(s):

Aqueous Extract ◽

Theobroma Cacao ◽

Wistar Rats ◽

Antioxidant Activities ◽

Research Work ◽

Stem Bark ◽

Dependent Manner ◽

Group 2 ◽

Dose Dependent ◽

Theobroma Cacao L

Background: This study investigated the potential antioxidant effects of aqueous extract of the stem bark of Theobroma cacao L. in Wistar rats. Methods: Twenty Wistar rats weighing between 126 g – 224 g were grouped randomly into 4groups of 5 rats each. Group 1 served as control and received water while groups 2, 3 and 4 rats were given 1000mg/kg, 3000mg/kg and 5000mg/kg b.wt of the extract respectively for 28days. On the 29th day, the rats were anaesthetized and blood samples were collected for analysis of some haematological parameters, enzymatic and non- enzymatic antioxidant activities. Results: The results obtained showed that there was significant increase (p<0.001) in SOD, Catalase activities and MDA levels in a dose dependent manner. The results also showed significant increase (p<0.001) in RBC Group 2, 3 and 4 rats when compared to the Group1. Significant increase was also observed in Hemoglobin (Hb) and Hematocrit (Hct) level in group 2 and 3 rats (p<0.001). Mean corpuscular volume was significantly increased in group 2 rats (p<0.001). Conclusion: The findings from this study showed the antioxidant and hematinic potentials of the stem bark of Theobroma cacao L.The aqueous extract of the stem bark of Theobroma cacao L. has a potential antioxidative and hematinic effects in Wistar rats. This is largely due to its rich phytochemical and nutritive contents. Further research work will be needed to see the possible application of these properties in humans.

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Acetate Suppresses Lipopolysaccharide-stimulated Nitric Oxide Production in Primary Rat Microglia but not in BV-2 Microglia Cells

Current Molecular Pharmacology ◽

10.2174/1874467213666200420101048 ◽

2020 ◽

Vol 14 (2) ◽

pp. 253-260

Author(s):

Mitsuaki Moriyama ◽

Yasunori Nishimura ◽

Ryosuke Kurebayashi ◽

Tomoki Minamihata ◽

Kenji Kawabe ◽

...

Keyword(s):

Nitric Oxide ◽

Ethics Committees ◽

No Production ◽

Dependent Manner ◽

Intraventricular Administration ◽

Ros Production ◽

Primary Microglia ◽

Inhibitory Effects ◽

Intracellular Ros ◽

Dose Dependent

Aims: To show that acetate attenuates neuroinflammatory responses in activated microglia. Background: Dietary acetate supplementation alleviates neuroglial activation in a rat model of neuroinflammation induced by intraventricular administration of lipopolysaccharide (LPS). However, the precise mechanism(s) underlying the anti-inflammatory effect of acetate is not fully understood. Objective: To determine whether acetate has inhibitory effects on LPS-induced neuroinflammatory responses in microglia. Methods: We examined LPS-stimulated nitric oxide (NO) production in primary rat microglia and BV-2 cells. Protein expression of inducible NO synthase (iNOS) was determined by western blot analysis. The intracellular generation of reactive oxygen species (ROS) and glutathione (GSH) were also evaluated. Results: In primary microglia, acetate decreased LPS-stimulated NO production in a dose-dependent manner, reaching significance at greater than 10 mM, and cell viability was not affected. Acetate suppressed LPS-induced expression of iNOS protein concomitantly with the decrease in NO. The LPS-induced increase in intracellular ROS production was attenuated by acetate. In addition, acetate prevented LPSinduced reduction of GSH. Notably, such suppressive effects of acetate on NO and ROS production were not observed in BV-2 cells. Conclusion: These findings suggest that acetate may alleviate neuroinflammatory responses by attenuating NO and ROS production in primary microglia but not in BV-2 cells. Other: All animals received humane care and the animal protocols used in this study were approved by the Ethics Committees for Animal Experimentation.

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Effects of removing heat and phlegm prescription on the proliferation and autoantigens expression of esophageal carcinoma cell.

Journal of Clinical Oncology ◽

10.1200/jco.2020.38.15_suppl.e16510 ◽

2020 ◽

Vol 38 (15_suppl) ◽

pp. e16510-e16510

Author(s):

Fuchun Si

Keyword(s):

Esophageal Carcinoma ◽

G1 Phase ◽

Dependent Manner ◽

Inhibitory Effects ◽

Ethanol Extraction ◽

Phase Arrest ◽

G1 Phase Arrest ◽

M Phase ◽

Ic50 Values ◽

Dose Dependent

e16510 Background: o explore the effects of removing heat and phlegm prescription (RHPP) on the proliferation and autoantigens expression of esophageal carcinoma(EC) cell, so as to provide basis for the molecular pathogenesis and clinical medication of EC. Methods: RHPP was developed by us for treating EC, EC autoantigens CK13, CK16, CaD, ACTG2 were identified in our previous studies. The effects of RHPP and and its ethanol extraction on the proliferation, cell cycle and autoantigen protein expression of Eca109 cell, EC9706 cell and TE-1 cell were investigated by MTT assay, flow cytometry and western blot analysis. Results: RHPP and its removing heat (RH) and removing phlegm (RP) separated prescriptions all have inhibitory effects on the proliferation of EC9706, EC109 and TE-1 cells in dose-dependent and time-dependent manner, changed morphology of four esophageal carcinoma cells, which appeared as round with rough edges, karyopyknosis, and karyorrhexis. Ic50 values of RHPP for Ec9706, Eca109 and TE1 cell were 33.31 ug·ml−1, 20.70 ug·ml−1, 21.93 ug·ml−1 respectively, while Ic50 values of RHPP’s ethanol extraction for Ec9706, Eca109, TE1 were 0.653 ug·ml−1, 0.082 ug·ml−1, 0.172 ug·ml−1 respectively. RHPP and RP induced G2/M phase arrest in EC109 and TE-1 cells, while RH induced G0/G1 phase arrest in EC109 and TE-1 cells; RHPP and RP induced G0/G1 phase arrest in EC9706 cells, while RH induced S phase arrest in EC9706 cells. RHPP and its two separated prescription could downregulate CK16, CaD, ACTG2 expression and upregulate CK13 expression. Conclusions: Autoantigens CK13, CK16, CaD and ACTG2 were expressed in EC cell, RHPP could regulate these four autoantigens expression. This study provides new basis for the EC mlecular mechanism and development of anti-esophageal carcinoma drugs in traditional Chinese medicine.

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