scholarly journals Biological Evaluation ofPupalia lappaceafor Antidiabetic, Antiadipogenic, and Hypolipidemic Activity BothIn VitroandIn Vivo

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Vivek Kumar ◽  
Parag Jain ◽  
Kalpana Rathore ◽  
Zabeer Ahmed
Keyword(s):  
Cell Line ◽  
Reference Group ◽  
Lipid Level ◽  
Biological Evaluation ◽  
Diabetic Rats ◽  
Hypolipidemic Activity ◽  
Albino Rats ◽  
Reference Drug

Objective. The present study assesses the effect ofPupalia lappacea(L.) Juss. (Amaranthaceae) (PL) leaves ethanolic extract on adipocytes, blood glucose level, and lipid level in streptozotocin (STZ) induced diabetic rats.Materials and Methods. Male Albino rats were rendered diabetic by a single moderately sized dose of STZ (45 mg/kg, intraperitoneally) at once before starting the treatment. Animals were divided into five groups: normoglycemic control, diabetic control, reference group (glibenclamide, 5.0 mg/kg), AS001 (250 mg/kg extract), and AS002 (500 mg/kg extract) each containing six animals forin vivostudy. Antidiabetic and hypolipidemic activity of extract were determined byin vivomethod on STZ induced diabetic rats. Antiadipogenic activity was determined byin vitromethod on 3T3-L1 cell line in comparison to simvastatin as reference drug.Result. The extract showed significant fall in fasting serum glucose (FSG), that is, 234.68 and 211.61 mg/dL, in STZ induced diabetic animals for dose groups AS001 and AS002, respectively. ThePLextract also exhibited noteworthy antiadipogenic activity on 3T3-L1 cell line. The value of inhibitory concentration (IC50) ofPLextract to reduce adipocyte cells was found to be 662.14 μg/mL.Conclusion. ThePLextract exhibited significant antiadipogenic, antidiabetic, and hypolipidemic activities.

scholarly journals IN VITRO ANTIOXIDANT AND IN VIVO ANTIDIABETIC ACTIVITY OF TWO POTENTIAL PROBIOTIC ENTEROCOCCUS SPP. ON ALLOXAN-INDUCED DIABETIC RATS

2021 ◽  
pp. 94-98
Author(s):  
KAMNI RAJPUT ◽  
RAMESH CHANDRA DUBEY
Keyword(s):  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Control Group ◽  
Albino Rats ◽  
Bacterial Cells ◽  
Bacterial Strains ◽  
Animal Group ◽  
Enterococcus Spp

Objective: In vitro antioxidant activity, in vivo antidiabetic property and intestinal attachment by two potential probiotic bacterial strains, namely, Enterococcus faecium and Enterococcus hirae were studied using albino rats. Methods: Antioxidant the activity was assessed using 2,2-Diphenyl-1-picrylhydrazyl radicals scavenging assay. Alloxan was administered intraperitoneally to induce diabetic conditions in experimental rats. Animals were treated with oral administration of Enterococcus spp., such as E. faecium, and E. hirae isolated from goat and sheep milk. The control animal group received normal saline for the same days. Glibenclamide drug was used as a positive control against probiotic bacterial cells. Results: However, administration of probiotic bacterial strains E. faecium and E. hirae, in albino rats significantly (p<0.05) at varying doses lowered blood glucose levels in diabetic rats as compared to the diabetic control group. Both the species of Enterococcus increased the bodyweight of experimental rats. However, E. faecium was the best antidiabetic strain having the antioxidant activities also in comparison to E. hirae. The attachment of probiotic bacterial cells E. faecium on the rat’s intestine wall against pathogens was examined. Furthermore, E. faecium showed its aggregation with pathogens by attachment of the intestines of albino rats. This showed that both the bacterial strains exhibited in vivo antidiabetic effect. Conclusion: The results of this study showed that probiotic bacteria possess antioxidant, antidiabetic activities, and attachment of intestine.

scholarly journals Design, synthesis and biological evaluation of a series of CNS penetrant HDAC inhibitors structurally derived from amyloid-β probes

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Myeong A Choi ◽  
Sun You Park ◽  
Hye Yun Chae ◽  
Yoojin Song ◽  
Chiranjeev Sharma ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Hdac Inhibitors ◽  
Amyloid Β ◽  
Biological Evaluation ◽  
Pharmacokinetic Studies ◽  
Dependent Manner ◽  
Reference Drug ◽  
Novel Scaffold

Abstract To develop novel CNS penetrant HDAC inhibitors, a new series of HDAC inhibitors having benzoheterocycle were designed, synthesized, and biologically evaluated. Among the synthesized compounds, benzothiazole derivative 9b exhibited a remarkable anti-proliferative activity (GI50 = 2.01 μM) against SH-SY5Y cancer cell line in a dose and time-dependent manner, better than the reference drug SAHA (GI50 = 2.90 μM). Moreover, compound 9b effectively promoted the accumulation of acetylated Histone H3 and α-tubulin through inhibition of HDAC1 and HDAC6 enzymes, respectively. HDAC enzyme assay also confirmed that compound 9b efficiently inhibited HDAC1 and HDAC6 isoforms with IC50 values of 84.9 nM and 95.9 nM. Furthermore, compound 9b inhibited colony formation capacity of SH-SY5Y cells, which is considered a hallmark of cell carcinogenesis and metastatic potential. The theoretical prediction, in vitro PAMPA-BBB assay, and in vivo brain pharmacokinetic studies confirmed that compound 9b had much higher BBB permeability than SAHA. In silico docking study demonstrated that compound 9b fitted in the substrate binding pocket of HDAC1 and HDAC6. Taken together, compound 9b provided a novel scaffold for developing CNS penetrant HDAC inhibitors and therapeutic potential for CNS-related diseases.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

scholarly journals Persea americana Leaf Ethyl Acetate Extract Phytochemical, In-vitro Antioxidant and In-vivo Potentials to Mitigate Oxidative Stress in Alloxan-induced Hyperglycaemic Rats

2019 ◽  
pp. 1-11
Author(s):  
J. A. Mashi ◽  
A. M. Sa’id ◽  
R. I. Idris ◽  
I. Aminu ◽  
A. A. Muhammad ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Body Weight ◽  
Ethyl Acetate ◽  
Ethyl Acetate Extract ◽  
Diabetic Rats ◽  
Persea Americana ◽  
Albino Rats ◽  
Standard Drug

The purpose of this study was to investigate the in-vivo and in-vitro potentials of ethyl acetate extract of P. americana leaf in alloxan-induced diabetic rats. Quantitative phytochemicals analyzed includes; flavonoids, saponins, tannins, alkaloids and phenolics. Measurement of antioxidant activity using 1,1-Diphenyl-2-picrylhydrazyl, total antioxidant capacity, hydroxyl radical, hydrogen peroxide, superoxide radical and ferric reducing activity of the extract was carried out. Hyperglycemia was induced by intraperitoneal injection of alloxan monohydrate to albino rats. In-vivo anti-oxidant potentials of the extract were evaluated by measuring liver homogenate activity of superoxide dismutase, catalase, glutathione reductase, glutathione peroxidase and malondyaldehyde in alloxan-induced diabetic rats administered with the extract.  A total of 30 Albino rats were used for this experiment and they were divided into six groups of 5 rats each. Group A; normal control, Group B; diabetic control, Groups C-E; experimental groups administered with different doses (100, 200 and 400 mg/kg body weight respectively); of the extract and Group F; glucophage (84 mg/kg body weight, standard drug) for 4 weeks. This study was conducted in the Department of Biochemistry, Bayero University, Kano, in August, 2018. Data was analyzed using one-way ANOVA with P=.05 value considered as significant. Results of the quantitative phytochemical investigation shows that the extract is rich in phenolics (184.1±0.6), flavonoids (115.8±2.1), alkaloids (41.5±1.8), with least concentration of tannis (21.2±0.8) and saponins (15.2±2.3). The extract exhibited high radical scavenging activity against synthetic free radicals (DPPH), reactive oxygen species (peroxide, superoxide and hydroxyl acid) and high ability to reduce Fe3+ to Fe2+ (FRAP). The activities of antioxidant enzymes of the treated rats were increased significantly (P=.05) while the level malondyaldehyde was significantly decreased (P=.05) in the treated groups. Ethyl acetate leaf extract of Persea americana contains phytochemical substances which improved antioxidant status and can be use as herbal therapy for the management of oxidative stress induced by diabetes mellitus and associated complications.

scholarly journals In vivo and in vitro antidiabetic properties of alkaloids extract from Salvia chudaei

2021 ◽  
pp. 45-53
Author(s):  
Mohammed Tlili ◽  
Roukia Hammoudi ◽  
Mahfoud Hadj-Mahammed
Keyword(s):  
Blood Glucose ◽  
Lipid Profile ◽  
Kidney Function ◽  
Inhibitory Effect ◽  
Diabetic Rats ◽  
Albino Rats ◽  
Liver And Kidney ◽  
Mean Blood Glucose

The aim of this study was to evaluate, for the first time, the antidiabetic effect of the alkaloids extract of Salvia chudaei Batt. & Trab. (Lamiaceae) on alloxan-induced diabetic rats. The alkaloids extract was prepared, and the in vitro inhibitory effect of key digesting enzymes related to postprandial hyperglycemia were determined. After acute toxicity test, the Swiss albino rats were induced with alloxan to get experimental diabetes animals. The fasting mean blood glucose, lipid profile, different liver and kidney function biomarkers and antioxidant biomarkers levels, after treatment for 30 days, diabetic untreated and diabetic rats treated with alkaloids extract were estimated. The alkaloids displayed remarkable in inhibiting ?-glucosidase (IC50 = 248.25?2.61 ?g/ml) than ?-amylase (IC50 = 262.96?9.64 ?g/ml) activities. In vivo, the results proved that alkaloids extract at dose of 500 mg/kg bw decreased significantly the blood glucose, lipid profile levels and improved the liver and kidney function biomarkers and increased the activities of antioxidant enzymes (superoxide dismutase and gluthatione reductase). This study demonstrates, that alkaloids are effective in inhibiting hyperglycemia and oxidative stress caused by diabetes.

scholarly journals Synthesis and Biological Evaluation of Thiazolyl-Ethylidene Hydrazino-Thiazole Derivatives: A Novel Heterocyclic System

2021 ◽  
Vol 11 (19) ◽  
pp. 8908
Author(s):  
Laila A. Al-Mutabagani ◽  
Fathy M. Abdelrazek ◽  
Sobhi M. Gomha ◽  
Ali S. Hebishy ◽  
Mohamed S. Abdelfattah ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Evaluation ◽  
Liver Carcinoma ◽  
Cytotoxic Activities ◽  
Thiazole Derivatives ◽  
Reference Drug ◽  
Anticancer Properties ◽  
Breast Carcinoma Cell Lines

The reaction of 2-(1-(2-(2-(4-methoxybenzylidene)hydrazinyl)-4-methylthiazol-5-yl)ethylidene)hydrazinecarbothioamide with a range of hydrazonoyl chlorides and α-halo-compounds yielded three new series of thiazole derivatives. Chemical and physical techniques were used to analyze all newly prepared derivatives (1H-NMR, 13C-NMR, FT-IR and mass spectrometry). The potential antimicrobial and anticancer properties of the synthesized derivatives were investigated using various in vitro biological experiments. Most of the thiazole compounds tested were effective against Gram-positive and Gram-negative bacteria. In addition, a minimum inhibition concentration was determined for the antibiotic properties of the most active produced substances. The cytotoxic activities were tested on HepG-2 (liver carcinoma), HCT-116 (colorectal carcinoma) and MDA-MB-231 (breast carcinoma) cell lines in comparison with cisplatin reference drug and using colorimetric MTT assay. The results detected that compound 10c was the most potent against the three tested cell lines. Interestingly, when the tested compounds were evaluated for their toxicity against normal (MRC-5) cells, they exhibited low toxic effects indicating the safe use of most of them that may require further in vivo and pharmacological studies.

A Novel Triazole Derivative Drug Presenting In Vitro and In Vivo Anticancer Properties

2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Hepatic Function ◽  
Anticancer Properties ◽  
Mcf 7

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.

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