scholarly journals Evaluation of Analgesic, Antidiarrheal and Anti-hyperglycemic Activities of Dactyloctenium australe (Poaceae)

2019 ◽  
Vol 22 (1) ◽  
pp. 85-91
Author(s):  
Md Enamul Hoque ◽  
Md Akbar Hossain ◽  
Md Sohel Rana
Keyword(s):  
Methanol Extract ◽  
Pharmaceutical Journal ◽  
Tolerance Test ◽  
Oral Glucose ◽  
Dependent Manner ◽  
Writhing Test ◽  
Aerial Parts ◽  
The Family ◽  
Dose Dependent

Dactyloctenium australe belongs to the family of Poaceae. It is also called gramineae or true grasses. Poaceae is the fifth largest family of flowering plants. The current study was conducted on methanol extract of the aerial parts of D. australe (MEDA) to evaluate its in vivo analgesic activity by acetic acidinduced writhing method in mice. The plant extract was also evaluated for antidiarrheal and antihyperglycemic activities using castor oil-induced diarrhea and oral glucose tolerance test, respectively. In acetic acid-induced writhing test, the extract showed 52.18 % and 62.40 % inhibition of writhing at the doses of 200-400mg/kg body weight, respectively while standard aspirin at the dose of 50 mg/kg bw showed 58.12 % writhing inhibition. In anti-hyperglycemic test, the extract revealed its activity in a dose dependent manner. In antidiarrheal activity test, the extract exhibited 48.54 % and 72.92 % inhibition of defecation at the doses of 250-500mg/kg bw, respectively whereas the standard loperamide (3 mg/kg bw) displayed 70.24 % inhibition of defecation. Bangladesh Pharmaceutical Journal 22(1): 85-91, 2019

scholarly journals In Vivo Efficacy of HD0471953: A Novel GPR119 Agonist for the Treatment of Type 2 Diabetes Mellitus

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
So Ra Kim ◽  
Dae-Hoon Kim ◽  
Soo Hyun Park ◽  
Young Seok Kim ◽  
Chun Hwa Kim ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Type 2 Diabetes ◽  
Type 2 Diabetes Mellitus ◽  
Tolerance Test ◽  
Oral Glucose ◽  
Dependent Manner ◽  
Gpr119 Agonist ◽  
Dose Dependent

G-protein coupled receptor 119 (GPR119) has emerged as a promising new target for the treatment of type 2 diabetes mellitus. The expression of GPR119 on the pancreatic B cells and intestinal L cells provides a unique opportunity for a single drug to promote insulin and GLP-1 secretion. In this study, we identified a novel small molecule GPR119 agonist, HD0471953, from our large library of synthetic compounds based on its ability to anti-hyperglycemic effects on T2DM murine models. We have tested the acute efficacy of HD0471953 by the oral glucose tolerance test (OGTT) with normal C57BL/6J mice. Then, chronic administrations of HD0471953 were performed to evaluate the efficacy on various diabetic rodent models. Single administration of HD0471953 showed improved glycemic control with a dose-dependent manner in OGTT with normal mice, and the insulin and GLP-1 were also increased. To identify chronic efficacy, we have observed a decline of blood glucose and fasting insulin in a dose-dependent manner of 10, 20, and 50 mpk indb/dbmice. The results suggest that HD0471953 may be a potentially promising anti-hyperglycemic agent for the treatment of patients with type 2 diabetes mellitus.

Incretin release from gut is acutely enhanced by sugar but not by sweeteners in vivo

2009 ◽  
Vol 296 (3) ◽  
pp. E473-E479 ◽  
Author(s):  
Yukihiro Fujita ◽  
Rhonda D. Wideman ◽  
Madeleine Speck ◽  
Ali Asadi ◽  
David S. King ◽  
...  
Keyword(s):  
Blood Glucose ◽  
Sweet Taste ◽  
Tolerance Test ◽  
Oral Glucose ◽  
Dependent Manner ◽  
Glucose Levels ◽  
Zucker Diabetic Fatty Rats ◽  
Glucagon Like Peptide 1

Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) are released during meals from endocrine cells located in the gut mucosa and stimulate insulin secretion from pancreatic β-cells in a glucose-dependent manner. Although the gut epithelium senses luminal sugars, the mechanism of sugar sensing and its downstream events coupled to the release of the incretin hormones are not clearly elucidated. Recently, it was reported that sucralose, a sweetener that activates the sweet receptors of taste buds, triggers incretin release from a murine enteroendocrine cell line in vitro. We confirmed that immunoreactivity of α-gustducin, a key G-coupled protein involved in taste sensing, is sometimes colocalized with GIP in rat duodenum. We investigated whether secretion of incretins in response to carbohydrates is mediated via taste receptors by feeding rats the sweet-tasting compounds saccharin, acesulfame potassium, d-tryptophan, sucralose, or stevia. Oral gavage of these sweeteners did not reduce the blood glucose excursion to a subsequent intraperitoneal glucose tolerance test. Neither oral sucralose nor oral stevia reduced blood glucose levels in Zucker diabetic fatty rats. Finally, whereas oral glucose increased plasma GIP levels ∼4-fold and GLP-1 levels ∼2.5-fold postadministration, none of the sweeteners tested significantly increased levels of these incretins. Collectively, our findings do not support the concept that release of incretins from enteroendocrine cells is triggered by carbohydrates via a pathway identical to the sensation of “sweet taste” in the tongue.

scholarly journals Analgesic, Antidiarrheal and CNS-depressant Activities of Flemingia macrophylla (Willd.)

2020 ◽  
Vol 23 (2) ◽  
pp. 141-145
Author(s):  
Asheka Rahman ◽  
Mohammad Mahmudul Hasan ◽  
Mohammad Abdullah Taher ◽  
Tanvir Muslim
Keyword(s):  
Methanol Extract ◽  
Pharmaceutical Journal ◽  
Developed Countries ◽  
Dependent Manner ◽  
Flemingia Macrophylla ◽  
Cns Depressant ◽  
Time Test ◽  
Analgesic Activities ◽  
Dose Dependent ◽  
Developing And Developed Countries

Plants are the priceless sources of bioactive natural compounds. Medicinal plants have been used since time immemorial in both developing and developed countries. Flemingia macrophylla (Willd.) is widely used as a hereditary medicines. The current study was designed to observe the analgesic, antidiarrheal and CNS depressant activities of methanol extract of the leaves of F. macrophylla (MEFM) and its petroleum ether (PEFM), dichloromethane (DFM), chloroform (CFM) and aqueous (AFM) fractions. The analgesic activities was assessed by acetic acid induced writhing method at doses 200- and 400- mg/kg body weight. The CNS-depressant effect was assayed by phenobarbitone sodium-induced sleeping time test. The anti-diarrheal activity of the extract was evaluated using castor oil-induced diarrhea in mice. The crude extract displayed significant peripheral analgesic activity at both test doses with 56.72- to 59.70-% inhibition of writhing responses, respectively. In CNS-depressant test, the extract revealed its activity in a dose dependent manner. In screening for antidiarrheal activity, the extract exhibited 20.83 and 41.67 % inhibition of defecation at 200- and 400-mg/kg bw, respectively whereas the standard loperamide (50 mg/kg bw) displayed 70.83 % inhibition of defecation. Bangladesh Pharmaceutical Journal 23(2): 141-145, 2020

scholarly journals Peripheral Analgesic and Anti-diarrheal Activities of Leaf of Syzygium cumini (L.) Skeel

2019 ◽  
Vol 22 (1) ◽  
pp. 13-17
Author(s):  
Md Shahidulla Kayser ◽  
Rubel Nath ◽  
Halima Khatun ◽  
Mohammad A Rashid
Keyword(s):  
Acetic Acid ◽  
Methanol Extract ◽  
Folk Medicine ◽  
Pharmaceutical Journal ◽  
Dependent Manner ◽  
Syzygium Cumini ◽  
Mice Model ◽  
Medicinal Value ◽  
First Time ◽  
Dose Dependent

Syzygium cumini has been used in folk medicine to treat many diseases. To establish the potential medicinal value of leaves of S. cumini, the current study was carried out to assess the peripheral analgesic and anti-diarrheal activities in mice model. The crude methanol extract and its petroleum ether and chloroform soluble fraction were administered to the experimental mice at a dose of 200- and 400- mg/kg b.w. (denoted as CME1, CME2, PESF1, PESF2, CLSF1 and CLSF2 respectively) using acetic acid induced writhing method and castrol oil induced anti-diarrheal assay protocol. The extract and its Kupchan fractions exhibited significant (p < 0.001) reduction of writhing response in a dose dependent manner. In the acetic acid-induced writhing test, the activity decreased in the order diclofenac (75.33%) > PESF2 (70.33%) > CME2 (67.00%) > PESF1 (64.00%) > CLSF2 (61.33%) > CME1 (56.67%) >CLSF1 (48.67%). All the fractions significantly (p < 0.001) attenuated anti-diarrheal effect in a dose dependent manner with the highest activity observed by CME2 (47.73%) as compared to standard lopeiramide (54.55%). The results of our study, being reported for the first time, provide reasonable indication that the methanol extract of S. cumini leaf and its different fractions possess peripheral analgesic and antidiarrheal activities. Bangladesh Pharmaceutical Journal 22(1): 13-17, 2019

scholarly journals In vivo Anti-diarrheal and CNS Depressant Activities of Hemigraphis hirta (Vahl) T. Anders.

2019 ◽  
Vol 22 (2) ◽  
pp. 176-180
Author(s):  
Md Shahidulla Kayser ◽  
Moazzema Binta Bashar ◽  
Tufael Ahmed ◽  
DA Anwar Al Aman
Keyword(s):  
Pharmaceutical Journal ◽  
Dependent Manner ◽  
Mice Model ◽  
Pharmacological Activities ◽  
Reference Drug ◽  
Preliminary Screening ◽  
Cns Depressant ◽  
First Time ◽  
Dose Dependent

Hemigraphis hirta has been used by folk practitioners to alleviate symptoms of several diseases, although the pharmacological activities of this plant have not been thoroughly explored. The current study was designed to assess the anti-diarrheal and CNS depressant activities of H. hirta in mice model. For both assays, the experimental mice received the methanolic crude extract and its petroleum ether soluble fraction at dose of 200 and 400 mg/kg body weight which are denoted as CME 200, CME 400, PESF 200 and PESF 400, respectively. Both fractions remarkably attenuated castor oil-induced diarrheal effect in a dose-dependent manner and the results were comparable to standard loperamide (89.47%). Among all, PESF 400 exhibited statistically significant (p < 0.01) anti-diarrheal activity as demonstrated by 78.95% inhibition of defacetion. Compared to reference drug diazepam, all the tested samples considerably shortened the time for onset of sleep and prolonged the duration of phenobarbitoneinduced sleep in mice. The results of our present study, being reported for the first time, demonstrate that the methanol extract of leaves of H. hirta and its organic soluble partionates possesses significant anti-diarrheal and CNS depressant properties. However, this preliminary screening requires further detailed investigation to confirm these findings as well as to isolate and characterize the bioactive compounds. Bangladesh Pharmaceutical Journal 22(2): 176-180, 2019

The Evaluation of Antianaphylactic Effect of Oryza sativa L. in Rats

1999 ◽  
Vol 27 (01) ◽  
pp. 63-71 ◽  
Author(s):  
Hyung Min Kim ◽  
Dong-Kue Yi ◽  
Hye Young Shin
Keyword(s):  
Oryza Sativa ◽  
Mast Cells ◽  
Histamine Release ◽  
Methanol Extract ◽  
Oryza Sativa L ◽  
Dependent Manner ◽  
Peritoneal Mast Cells ◽  
Dose Dependent

This study was carried out to examine the effect of methanol extract of Oryza sativa L. (Dong-Jin in Korean, abbreviate as Os-DJ hereafter) on anaphylaxis. Os-DJ (10-5 to 1 g/kg) dose-dependently inhibited systemic anaphylaxis induced by compound 48/80 in rats. When Os-DJ was pretreated at concentration ranging from 10-5 to 1 g/kg, the serum histamine levels were reduced in a dose-dependent manner. Os-DJ (1 g/kg) also significantly inhibited local anaphylaxis activated by anti-dinitrophenyl (DNP) IgE. Moreover, Os-DJ dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. These results indicate that Os-DJ possess anti anaphylactic activity by inhibition of histamine release from mast cells in vivo and in vitro.

Effects of NO-Donors on Thrombus Formation and Microcirculation in Cerebral Vessels of the Rat

1996 ◽  
Vol 76 (01) ◽  
pp. 111-117 ◽  
Author(s):  
Yasuto Sasaki ◽  
Junji Seki ◽  
John C Giddings ◽  
Junichiro Yamamoto
Keyword(s):  
Blood Flow ◽  
Thrombus Formation ◽  
Dependent Manner ◽  
Red Cell ◽  
Cell Velocity ◽  
Red Cell Velocity ◽  
The Mean ◽  
Wall Shear ◽  
Dose Dependent

SummarySodium nitroprusside (SNP) and 3-morpholinosydnonimine (SIN-1), are known to liberate nitric oxide (NO). In this study the effects of SNP and SIN-1 on thrombus formation in rat cerebral arterioles and venules in vivo were assessed using a helium-neon (He-Ne) laser. SNP infused at doses from 10 Μg/kg/h significantly inhibited thrombus formation in a dose dependent manner. This inhibition of thrombus formation was suppressed by methylene blue. SIN-1 at a dose of 100 Μg/kg/h also demonstrated a significant antithrombotic effect. Moreover, treatment with SNP increased vessel diameter in a dose dependent manner and enhanced the mean red cell velocity measured with a fiber-optic laser-Doppler anemometer microscope (FLDAM). Blood flow, calculated from the mean red cell velocity and vessel diameters was increased significantly during infusion. In contrast, mean wall shear rates in the arterioles and venules were not changed by SNP infusion. The results indicated that SNP and SIN-1 possessed potent antithrombotic activities, whilst SNP increased cerebral blood flow without changing wall shear rate. The findings suggest that the NO released by SNP and SIN-1 may be beneficial for the treatment and protection of cerebral infarction

Ecological and physiological as well as biochemical properties of representatives of the Genus sedum L.

2014 ◽  
Vol 25 (3-4) ◽  
pp. 24-33
Author(s):  
O. I. Dzjuba ◽  
M. V. Yatsenko
Keyword(s):  
Nitric Oxide ◽  
Cell Line ◽  
Methanol Extract ◽  
Hepatoma Cell ◽  
Ethanol Extract ◽  
Biochemical Properties ◽  
Biologically Active ◽  
Hepatoma Cell Line ◽  
Dependent Manner ◽  
Dose Dependent

The article deals with the history of the study and the current state of research of physiological and biochemical properties of the plant genus Sedum that are useful for human and has been used in folk medicine for many years. It was noticed that antioxidant properties of extracts from plants S. sarmentosum, S. sempervivoides, S. takesimense were caused by the presence of phenolic compounds. Methanol extract of plants S. takesimense exhibited strong scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals as well as significant inhibitory effects on lipid peroxidation and low density lipoprotein (LDL) oxidation induced by a metal ion Cu2+. Various immunomodulatory activities of various fractions of plants extracts (S. dendroideum, S. kamtschaticum, S. sarmentosum, S. telephium) are observed. It was shown that the ethanol extract of S. sarmentosum and it’s fractions suppressed specific antibody and cellular responses to ovalbumin in mice. The methanol extract of plants S. sarmentosum reduced the levels of anti-inflammatory markers, such as volume of exudates, number of polymorphonuclear leukocytes, suppressed nitric oxide synthesis in activated macrophages via suppressed induction of inducible nitric oxide synthase (iNOS). Polysaccharides fractions from plants S. telephium inducing productions of tumor necrosis factor alpha (TNF-α), increasing the intensity of phagocytosis in vitro and in vivo. Methanol extract from the whole part of S. kamtschaticum strongly inhibit PGE2 production from lipopolysaccharide-induced RAW 264.7 cells, a mouse macrophage cell line via modulating activity in gene expression of the enzyme cyclooxygenase-2 (COX-2). The methanol extract of plants S. sarmentosum and the major kaempferol glycosides from S. dendroideum have antinociceptive activity. It was noticed that anti-adipogenic activity of extracts from plants S. kamtschaticum were caused by inhibition of peroxisome-proliferator-activated receptor γ (PPARγ) expression and it’s dependent target genes, such as genes encoding adipocyte protein 2 (аР2), lipoprotein lipase (LPL), adiponectin and CD36. Polysaccharides fractions from S. telephium cause inhibition of cell adhesion of human fibroblast (MRC5) to laminin and fibronectin via interfere with integrin-mediated cell behaviour and they contributed to the role of polysaccharides in cell-matrix interaction. The methanol extract of plants S. sarmentosum exhibited a significant inhibitory activity in the chick embryo chorioallantoic membrane angiogenesis in a dose-dependent manner. The crude alkaloid fraction of S. sarmentosum caused a dose-dependent inhibition of cell proliferation on murine hepatoma cell line BNL CL.2 and human hepatoma cell line HepG2 without necrosis or apoptosis. Alkaloids from plants S. sarmentosum may improve survival of hepatoma patients via the inhibition of excessive growth of tumor cells. Plant’s juices have antiviral activity (S. sarmentosum, S. spurium, S. stahlii). Crude ethanol extract S. praealtum have spermicidal activity of the in mice and a relevant inhibitory effect of aqueous extract on human spermatozoa motility as well as an anti-fertilizing activity in rats. Hepatoprotective triterpenes, e.g., δ-amyrone, 3-epi-δ-amyrin, δ-amyrin and sarmentolin were isolated from S. sarmentosum. 2- and 2,6-substituted piperidine alkaloids (e.g., norsedamine, allosedridine, sedamine, allosedamine) are observed in plants S. acre, which in the presence of data on the use of pyridine and piperidine derivatives for treating neurodegenerative diseases (e.g., Alzheimer's disease), points on the promising research in this area. Taking into account that biologically active compounds are accumulated in the aboveground vegetative organs of plants of Sedum, the prospects of further study of the use of Sedum for the purposes of biotechnology and in the pharmaceutical industry becomes apparent. This work extends the existing views regarding the use of plants Sedum.

scholarly journals Anti-tumor activity of a novel proteasome inhibitor D395 against multiple myeloma and its lower cardiotoxicity compared with carfilzomib

2021 ◽  
Vol 12 (5) ◽  
Author(s):  
Xuxing Shen ◽  
Chao Wu ◽  
Meng Lei ◽  
Qing Yan ◽  
Haoyang Zhang ◽  
...  
Keyword(s):  
Multiple Myeloma ◽  
Proteasome Inhibitor ◽  
Osteoclast Differentiation ◽  
Dependent Manner ◽  
Serum Enzyme ◽  
Herg Channels ◽  
Anti Tumor Activity ◽  
Dose Dependent

AbstractCarfilzomib, a second-generation proteasome inhibitor, has significantly improved the survival rate of multiple myeloma (MM) patients, but its clinical application is still restricted by drug resistance and cardiotoxicity. Here, we identified a novel proteasome inhibitor, D395, and assessed its efficacy in treating MM as well as its cardiotoxicity at the preclinical level. The activities of purified and intracellular proteasomes were measured to determine the effect of D395 on the proteasome. CCK-8 and flow cytometry experiments were designed to evaluate the effects of D395 on cell growth and apoptosis. The effects of D395 and carfilzomib on serum enzyme activity, echocardiography features, cardiomyocyte morphology, and hERG channels were also compared. In our study, D395 was highly cytotoxic to MM cell lines and primary MM cells but not normal cells, and it was well tolerated in vivo. Similar to carfilzomib, D395 inhibited osteoclast differentiation in a dose-dependent manner. In particular, D395 exhibited lower cardiotoxicity than carfilzomib in all experiments. In conclusion, D395 is a novel irreversible proteasome inhibitor that has remarkable anti-MM activity and mild cardiotoxicity in vitro and in vivo.

scholarly journals Effect of Synchronous Versus Sequential Regimens on the Pharmacokinetics and Biodistribution of Regorafenib with Irradiation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 386
Author(s):  
Tung-Hu Tsai ◽  
Yu-Jen Chen ◽  
Li-Ying Wang ◽  
Chen-Hsi Hsieh
Keyword(s):  
Stereotactic Body Radiation Therapy ◽  
In Vivo Studies ◽  
Control Group ◽  
High Dose ◽  
Dependent Manner ◽  
Hep G2 ◽  
Time Curve ◽  
Dose Dependent

This study was performed to evaluate the interaction between conventional or high-dose radiotherapy (RT) and the pharmacokinetics (PK) of regorafenib in concurrent or sequential regimens for the treatment of hepatocellular carcinoma. Concurrent and sequential in vitro and in vivo studies of irradiation and regorafenib were designed. The interactions of RT and regorafenib in vitro were examined in the human hepatoma Huh-7, HA22T and Hep G2 cell lines. The RT–PK phenomenon and biodistribution of regorafenib under RT were confirmed in a free-moving rat model. Regorafenib inhibited the viability of Huh-7 cells in a dose-dependent manner. Apoptosis in Huh-7 cells was enhanced by RT followed by regorafenib treatment. In the concurrent regimen, RT decreased the area under the concentration versus time curve (AUC)regorafenib by 74% (p = 0.001) in the RT2 Gy × 3 fraction (f’x) group and by 69% (p = 0.001) in the RT9 Gy × 3 f’x group. The AUCregorafenib was increased by 182.8% (p = 0.011) in the sequential RT2Gy × 1 f’x group and by 213.2% (p = 0.016) in the sequential RT9Gy × 1 f’x group. Both concurrent regimens, RT2Gy × 3 f’x and RT9Gy × 3 f’x, clearly decreased the biodistribution of regorafenib in the heart, liver, lung, spleen and kidneys, compared to the control (regorafenib × 3 d) group. The concurrent regimens, both RT2Gy × 3 f’x and RT9Gy × 3 f’x, significantly decreased the biodistribution of regorafenib, compared with the control group. The PK of regorafenib can be modulated both by off-target irradiation and stereotactic body radiation therapy (SBRT).

Sign in / Sign up

Export Citation Format

Share Document