tanmoy guria | Adamas University (original) (raw)

Papers by tanmoy guria

Research paper thumbnail of Synthesis, Characterization and Evaluation of Anticancer Activity of Some New Schiff Bases of 1, 3, 4-THIADIAZOLE Derivatives

International Journal of Pharmacy and Pharmaceutical Sciences, 2015

Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticance... more Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticancer activity. Methods: In the present study five new derivatives of N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine (Schiff bases containing 1, 3, 4-thiadiazole) were synthesized according to the literature methods and were characterized by FT-IR, 1 H NMR spectroscopy and C, H, N analysis. Anticancer activity was evaluated in Male Swiss albino mice using Ehrlich’s Ascites carcinoma cells. Compounds were administered at a dose of 25 mg/kg, body weight intraperitoneally. Results: The compounds were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition, non-viable cell count and increase in life span (%ILS). All the compounds exhibited significant (P< 0.01) anticancer activity compared to control and the compound 2d & 4d was found to be most potent. Conclusion: It is concluded that synthesized Schiff bases of 2-amino-5-...

Research paper thumbnail of Rise of Covid 19 Pandemic: Management Strategies and Effect on Human Health and Wealth

International research journal of pharmacy, 2020

The world is currently witnessing a pandemic crisis caused by SARS CoV-2 having its origin in Wuh... more The world is currently witnessing a pandemic crisis caused by SARS CoV-2 having its origin in Wuhan, China Transformation from epidemic to pandemic within a very short time-gap resulting in massive global mortality has created a sudden global deadlock affecting both human health and wealth Clinical symptoms expressed by affected patients include dry cough, dyspnea, fever, bilateral lung infiltration and ultimately severe acute respiratory distress in advanced stages The disease is spread over 150 countries and termed as COVID-19 by the World Health Organization (W H O) As per W H O report on 2nd May 2020 there are over 3000000 infected cases distributed throughout the globe claiming more than 200000 lives Mortality rate is accelerating at high speed and presently crossing 6% The entire global healthcare system is exposed and found to be inadequate to mitigate the deadly virus At present there is no medicine or vaccine available or clinically proven for COVID-19 management However, t...

Research paper thumbnail of SYNTHESIS, CHARACTERIZATION AND EVALUATION OF ANTICANCER ACTIVITY OF SOME NEW SCHIFF BASES OF 1, 3, 4-THIADIAZOLE DERIVATIVES Original Article

Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticance... more Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticancer activity. Methods: In the present study five new derivatives of N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine (Schiff bases containing 1, 3, 4thiadiazole) were synthesized according to the literature methods and were characterized by FT-IR, 1 Results: The compounds were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition, non-viable cell count and increase in life span (%ILS). All the compounds exhibited significant (P< 0.01) anticancer activity compared to control and the compound 2d & 4d was found to be most potent. H NMR spectroscopy and C, H, N analysis. Anticancer activity was evaluated in Male Swiss albino mice using Ehrlich’s Ascites carcinoma cells. Compounds were administered at a dose of 25 mg/kg, body weight intraperitoneally. Conclusion: It is concluded that synthesized Schiff bases of 2-amino-5-a...

Research paper thumbnail of Isolation and Characterization of Phytoconstituents of Roots of Amaranthus spinosus Linn. (Fam. Amaranthaceae)

Research paper thumbnail of A Novel Tetraenoic Fatty Acid Isolated from Amaranthus spinosus Inhibits Proliferation and Induces Apoptosis of Human Liver Cancer Cells

Amaranthus spinosus Linn. (Family: Amaranthaceae) has been shown to be useful in preventing and m... more Amaranthus spinosus Linn. (Family: Amaranthaceae) has been shown to be useful in preventing and mitigating adverse pathophysiological conditions and complex diseases. However, only limited information is available on the anticancer potential of this plant. In this study, we examined the antiproliferative and pro-apoptotic effects of a novel fatty acid isolated from A. spinosus-(14E,18E,22E,26E)-methyl nonacosa-14,18,22,26 tetraenoate-against HepG2 human liver cancer cells. We used 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to determine cell viability, flow cytometry assay for cell cycle analysis, and Western blot analysis to measure protein expression of Cdc2), cyclin B1, Bcl-2-associated X protein (Bax), and B-cell lymphoma 2 (Bcl-2). The MTT assay showed that the fatty acid markedly inhibited the proliferation of HepG2 cells in a dosage-dependent fashion, with a half maximal inhibitory concentration (IC 50) value of 25.52 µmol/L. This antiproliferative result was superior to that of another known fatty acid, linoleic acid (IC 50 38.65 µmol/L), but comparable to that of standard anticancer drug doxorubicin (IC 50 24.68 µmol/L). The novel fatty acid also induced apoptosis mediated by downregulation of cyclin B1, upregulation of Bax, and downregulation of Bcl-2, resulting in the G 2 /M transition arrest. Our results provide the first experimental evidence that a novel fatty acid isolated from A. spinosus exhibits significant antiproliferative activity mediated through the induction of apoptosis in HepG2 cells. These encouraging results may facilitate the development of A. spinosus fatty acid for the prevention and intervention of hepatocellular carcinoma.

Research paper thumbnail of Synthesis, Pharmacological Evaluation and Ligand-Protein Interaction Study of Hybrid Urea and Thiourea Derivatives as Antihyperglycemic Agents

International Research Journal Of Pharmacy

A series of hybrid urea/thiourea derivatives (5a-5f) with chalcone moiety were synthesized and ph... more A series of hybrid urea/thiourea derivatives (5a-5f) with chalcone moiety were synthesized and pharmacological activity was evaluated using invitro αglucosidase inhibition assay and invivo antidiabetic activity in streptozotocin (STZ) induced diabetic rat model. Among the synthesized molecules, compound 5d (1-[4′-N-(N′-p-chlorophenylurenyl) phenyl]-3-(4-methoxyphenyl)-2-propen-1-one) is more potent with IC50 value 12.88 µM when compared to the standard drug Acarbose (IC50 16.54 µM) in invitro study. Invivo study demonstrated that compound 5d was more effective than other synthesized molecules by estimation of different biochemical parameters. For the understanding of ligand-protein interaction, molecular docking studies of the synthesized compounds were also performed. Overall, synthesized hybrid urea/thiourea derivatives might be potential a new class of compound for the treatment of type-II diabetes.

Research paper thumbnail of Evaluation of Analgesic and Anti-Inflammatory Activity of Chloroform and Methanol Extracts of Centella asiatica Linn

International Scholarly Research Notices, Nov 21, 2013

Research paper thumbnail of A new ester of fatty acid from methanol extract of the whole plant of Amaranthus spinosus and its α-glucosidase inhibitory activity

Pharmaceutical Biology, 2014

Abstract Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as &amp;amp;amp;a... more Abstract Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as &amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;quot;spiny pigweed&amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;quot;, is used both in the Indian traditional system and in folk medicine to treat diabetes. The present study evaluates the scientific basis of antidiabetic activity of chloroform fraction of methanol extract of A. spinosus and of an isolated constituent of A. spinosus. HPLC analysis was performed to determine the purity and the amount of the constituent present in the plant extract. The yeast α-glucosidase inhibition technique was used to determine the antidiabetic activity of A. spinosus. Acarbose was used as a standard. An appropriate therapeutic approach for preventing diabetes mellitus and obesity is to retard the absorption of glucose by inhibition of α-glucosidase. One novel fatty acid with strong α-glucosidase inhibitory activity - (14E, 18E, 22E, 26E) - methyl nonacosa-14, 18, 22, 26 tetraenoate [1] (IC50 value 6.52 µM/mL) and β-sitosterol [2] were purified. Compound 1 was found to be more potent than the methanol extract. HPLC quantative analysis revealed that 0.15% of compound 1 and 0.06% of compound 2 were present in the plant extract. This novel fatty acid can potentially be developed as a novel natural nutraceutical for the management of diabetes.

Research paper thumbnail of Pharmacological Actions and Phytoconstituents of Amaranthus spinosus Linn: A Review

International Journal of Pharmacognosy and Phytochemical Research

This work presents a brief overview of the morphological, phytochemical and pharmacological prope... more This work presents a brief overview of the morphological, phytochemical and pharmacological properties of Amaranthus spinosus Linn. The available information on the ethnopharmacological uses in traditional medicine, phytochemistry, pharmacology and clinical practice of Amaranthus spinosuswere collected via a library and electronic search (PubMed, ScienceDirect, Google Scholar and Spingerlink). Phytochemical investigation of this plant h as resulted in the identification of more than 20 active chemical constituents, among which betalains, hydroxycinnamates, saponins, steroids and flavonoids are the predominant ones. The plant has desirable effects like cooling, digestible, alexiteric, laxa tive, diuretic, stomachic, antipyretic, improves the appetite, useful in kapha and biliousness, blood disease, burning sensation, hallucination, leprosy, bronchitis, rat bite, piles and leucorrhoea. This article enumerates an overview of phytochemical and pharmacological aspects that is useful to researchers for further exploration necessary for the development of this potential herb.

Research paper thumbnail of Evaluation of Analgesic and Anti-Inflammatory Activity of Chloroform and Methanol Extracts of Centella asiatica Linn

ISRN pharmacology, 2013

A variety of active constituents with wide range of pharmacological actions have been reported wi... more A variety of active constituents with wide range of pharmacological actions have been reported with Centella asiatica. The present study was undertaken to assess analgesic and anti-inflammatory properties of its leaf extracts. Dried leaves were defatted with petroleum ether and extracted with chloroform and methanol. Both chloroform and methanol extracts were evaluated for analgesic activity through tail clip, tail flick, tail immersion, and writhing assay tests at doses of 50, 100, and 200 mg/kg using Swiss albino mice. On the other hand, anti-inflammatory assay was performed by carrageenan induced paw edema of methanol extract at 100 and 200 mg doses in Wistar albino rat. Dextropropoxyphene and indomethacin were employed as a standard for analgesic and anti-inflammatory studies, respectively. Our present study demonstrated that Centella asiatica bears significant analgesic and anti-inflammatory activities in those models.

Research paper thumbnail of A new ester of fatty acid from a methanol extract of the whole plant of Amaranthus spinosus and its α-glucosidase inhibitory activity

Pharmaceutical biology, 2015

Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as "spiny pigweed", ... more Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as "spiny pigweed", is used both in the Indian traditional system and in folk medicine to treat diabetes. The present study evaluates the scientific basis of antidiabetic activity of chloroform fraction of methanol extract of A. spinosus and of an isolated constituent of A. spinosus. HPLC analysis was performed to determine the purity and the amount of the constituent present in the plant extract. The yeast α-glucosidase inhibition technique was used to determine the antidiabetic activity of A. spinosus. Acarbose was used as a standard. An appropriate therapeutic approach for preventing diabetes mellitus and obesity is to retard the absorption of glucose by inhibition of α-glucosidase. One novel fatty acid with strong α-glucosidase inhibitory activity - (14E, 18E, 22E, 26E) - methyl nonacosa-14, 18, 22, 26 tetraenoate [1] (IC50 value 6.52 µM/mL) and β-sitosterol [2] were purified. Compound 1 was found to be...

Research paper thumbnail of Synthesis and anticancer evaluation of 5-benzyl-1,3,4-thiadiazol-2-amine derivatives on Ehrlich ascites carcinoma bearing mice

5-benzyl-1,3,4-thiadiazol-2-amine derivatives (2-12) were synthesized by reaction of 5-benzyl-1,3... more 5-benzyl-1,3,4-thiadiazol-2-amine derivatives (2-12) were synthesized by reaction of 5-benzyl-1,3,4-thiadiazol-2- amine with different substituted phenyl isocyanates or phenyl isothiocyanates. Structures of all compounds were established on the basis of FT-IR, 1HNMR, and LC-MS spectral data. The effects of all compounds on in-vivo tumor growth inhibition were evaluated by studying the parameters such as tumor volume, tumor cell count (viable and non-viable), haematological values, and mean survival time of carcinoma cells bearing mice. Among the tested compounds, compound 2 (54.63%), 3 (60.8%), and 11 (51.54%) showed significant tumor growth inhibition and compared favourably with the standard anticancer drug 5-fluorouracil

Research paper thumbnail of Synthesis, Characterization and Evaluation of Anticancer Activity of Some New Schiff Bases of 1, 3, 4-THIADIAZOLE Derivatives

International Journal of Pharmacy and Pharmaceutical Sciences, 2015

Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticance... more Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticancer activity. Methods: In the present study five new derivatives of N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine (Schiff bases containing 1, 3, 4-thiadiazole) were synthesized according to the literature methods and were characterized by FT-IR, 1 H NMR spectroscopy and C, H, N analysis. Anticancer activity was evaluated in Male Swiss albino mice using Ehrlich’s Ascites carcinoma cells. Compounds were administered at a dose of 25 mg/kg, body weight intraperitoneally. Results: The compounds were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition, non-viable cell count and increase in life span (%ILS). All the compounds exhibited significant (P< 0.01) anticancer activity compared to control and the compound 2d & 4d was found to be most potent. Conclusion: It is concluded that synthesized Schiff bases of 2-amino-5-...

Research paper thumbnail of Rise of Covid 19 Pandemic: Management Strategies and Effect on Human Health and Wealth

International research journal of pharmacy, 2020

The world is currently witnessing a pandemic crisis caused by SARS CoV-2 having its origin in Wuh... more The world is currently witnessing a pandemic crisis caused by SARS CoV-2 having its origin in Wuhan, China Transformation from epidemic to pandemic within a very short time-gap resulting in massive global mortality has created a sudden global deadlock affecting both human health and wealth Clinical symptoms expressed by affected patients include dry cough, dyspnea, fever, bilateral lung infiltration and ultimately severe acute respiratory distress in advanced stages The disease is spread over 150 countries and termed as COVID-19 by the World Health Organization (W H O) As per W H O report on 2nd May 2020 there are over 3000000 infected cases distributed throughout the globe claiming more than 200000 lives Mortality rate is accelerating at high speed and presently crossing 6% The entire global healthcare system is exposed and found to be inadequate to mitigate the deadly virus At present there is no medicine or vaccine available or clinically proven for COVID-19 management However, t...

Research paper thumbnail of SYNTHESIS, CHARACTERIZATION AND EVALUATION OF ANTICANCER ACTIVITY OF SOME NEW SCHIFF BASES OF 1, 3, 4-THIADIAZOLE DERIVATIVES Original Article

Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticance... more Objective: N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine derivatives: Synthesis and anticancer activity. Methods: In the present study five new derivatives of N-benzylidene-5-phenyl-1, 3, 4-thiadiazol-2-amine (Schiff bases containing 1, 3, 4thiadiazole) were synthesized according to the literature methods and were characterized by FT-IR, 1 Results: The compounds were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition, non-viable cell count and increase in life span (%ILS). All the compounds exhibited significant (P< 0.01) anticancer activity compared to control and the compound 2d & 4d was found to be most potent. H NMR spectroscopy and C, H, N analysis. Anticancer activity was evaluated in Male Swiss albino mice using Ehrlich’s Ascites carcinoma cells. Compounds were administered at a dose of 25 mg/kg, body weight intraperitoneally. Conclusion: It is concluded that synthesized Schiff bases of 2-amino-5-a...

Research paper thumbnail of Isolation and Characterization of Phytoconstituents of Roots of Amaranthus spinosus Linn. (Fam. Amaranthaceae)

Research paper thumbnail of A Novel Tetraenoic Fatty Acid Isolated from Amaranthus spinosus Inhibits Proliferation and Induces Apoptosis of Human Liver Cancer Cells

Amaranthus spinosus Linn. (Family: Amaranthaceae) has been shown to be useful in preventing and m... more Amaranthus spinosus Linn. (Family: Amaranthaceae) has been shown to be useful in preventing and mitigating adverse pathophysiological conditions and complex diseases. However, only limited information is available on the anticancer potential of this plant. In this study, we examined the antiproliferative and pro-apoptotic effects of a novel fatty acid isolated from A. spinosus-(14E,18E,22E,26E)-methyl nonacosa-14,18,22,26 tetraenoate-against HepG2 human liver cancer cells. We used 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to determine cell viability, flow cytometry assay for cell cycle analysis, and Western blot analysis to measure protein expression of Cdc2), cyclin B1, Bcl-2-associated X protein (Bax), and B-cell lymphoma 2 (Bcl-2). The MTT assay showed that the fatty acid markedly inhibited the proliferation of HepG2 cells in a dosage-dependent fashion, with a half maximal inhibitory concentration (IC 50) value of 25.52 µmol/L. This antiproliferative result was superior to that of another known fatty acid, linoleic acid (IC 50 38.65 µmol/L), but comparable to that of standard anticancer drug doxorubicin (IC 50 24.68 µmol/L). The novel fatty acid also induced apoptosis mediated by downregulation of cyclin B1, upregulation of Bax, and downregulation of Bcl-2, resulting in the G 2 /M transition arrest. Our results provide the first experimental evidence that a novel fatty acid isolated from A. spinosus exhibits significant antiproliferative activity mediated through the induction of apoptosis in HepG2 cells. These encouraging results may facilitate the development of A. spinosus fatty acid for the prevention and intervention of hepatocellular carcinoma.

Research paper thumbnail of Synthesis, Pharmacological Evaluation and Ligand-Protein Interaction Study of Hybrid Urea and Thiourea Derivatives as Antihyperglycemic Agents

International Research Journal Of Pharmacy

A series of hybrid urea/thiourea derivatives (5a-5f) with chalcone moiety were synthesized and ph... more A series of hybrid urea/thiourea derivatives (5a-5f) with chalcone moiety were synthesized and pharmacological activity was evaluated using invitro αglucosidase inhibition assay and invivo antidiabetic activity in streptozotocin (STZ) induced diabetic rat model. Among the synthesized molecules, compound 5d (1-[4′-N-(N′-p-chlorophenylurenyl) phenyl]-3-(4-methoxyphenyl)-2-propen-1-one) is more potent with IC50 value 12.88 µM when compared to the standard drug Acarbose (IC50 16.54 µM) in invitro study. Invivo study demonstrated that compound 5d was more effective than other synthesized molecules by estimation of different biochemical parameters. For the understanding of ligand-protein interaction, molecular docking studies of the synthesized compounds were also performed. Overall, synthesized hybrid urea/thiourea derivatives might be potential a new class of compound for the treatment of type-II diabetes.

Research paper thumbnail of Evaluation of Analgesic and Anti-Inflammatory Activity of Chloroform and Methanol Extracts of Centella asiatica Linn

International Scholarly Research Notices, Nov 21, 2013

Research paper thumbnail of A new ester of fatty acid from methanol extract of the whole plant of Amaranthus spinosus and its α-glucosidase inhibitory activity

Pharmaceutical Biology, 2014

Abstract Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as &amp;amp;amp;a... more Abstract Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as &amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;quot;spiny pigweed&amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;amp;quot;, is used both in the Indian traditional system and in folk medicine to treat diabetes. The present study evaluates the scientific basis of antidiabetic activity of chloroform fraction of methanol extract of A. spinosus and of an isolated constituent of A. spinosus. HPLC analysis was performed to determine the purity and the amount of the constituent present in the plant extract. The yeast α-glucosidase inhibition technique was used to determine the antidiabetic activity of A. spinosus. Acarbose was used as a standard. An appropriate therapeutic approach for preventing diabetes mellitus and obesity is to retard the absorption of glucose by inhibition of α-glucosidase. One novel fatty acid with strong α-glucosidase inhibitory activity - (14E, 18E, 22E, 26E) - methyl nonacosa-14, 18, 22, 26 tetraenoate [1] (IC50 value 6.52 µM/mL) and β-sitosterol [2] were purified. Compound 1 was found to be more potent than the methanol extract. HPLC quantative analysis revealed that 0.15% of compound 1 and 0.06% of compound 2 were present in the plant extract. This novel fatty acid can potentially be developed as a novel natural nutraceutical for the management of diabetes.

Research paper thumbnail of Pharmacological Actions and Phytoconstituents of Amaranthus spinosus Linn: A Review

International Journal of Pharmacognosy and Phytochemical Research

This work presents a brief overview of the morphological, phytochemical and pharmacological prope... more This work presents a brief overview of the morphological, phytochemical and pharmacological properties of Amaranthus spinosus Linn. The available information on the ethnopharmacological uses in traditional medicine, phytochemistry, pharmacology and clinical practice of Amaranthus spinosuswere collected via a library and electronic search (PubMed, ScienceDirect, Google Scholar and Spingerlink). Phytochemical investigation of this plant h as resulted in the identification of more than 20 active chemical constituents, among which betalains, hydroxycinnamates, saponins, steroids and flavonoids are the predominant ones. The plant has desirable effects like cooling, digestible, alexiteric, laxa tive, diuretic, stomachic, antipyretic, improves the appetite, useful in kapha and biliousness, blood disease, burning sensation, hallucination, leprosy, bronchitis, rat bite, piles and leucorrhoea. This article enumerates an overview of phytochemical and pharmacological aspects that is useful to researchers for further exploration necessary for the development of this potential herb.

Research paper thumbnail of Evaluation of Analgesic and Anti-Inflammatory Activity of Chloroform and Methanol Extracts of Centella asiatica Linn

ISRN pharmacology, 2013

A variety of active constituents with wide range of pharmacological actions have been reported wi... more A variety of active constituents with wide range of pharmacological actions have been reported with Centella asiatica. The present study was undertaken to assess analgesic and anti-inflammatory properties of its leaf extracts. Dried leaves were defatted with petroleum ether and extracted with chloroform and methanol. Both chloroform and methanol extracts were evaluated for analgesic activity through tail clip, tail flick, tail immersion, and writhing assay tests at doses of 50, 100, and 200 mg/kg using Swiss albino mice. On the other hand, anti-inflammatory assay was performed by carrageenan induced paw edema of methanol extract at 100 and 200 mg doses in Wistar albino rat. Dextropropoxyphene and indomethacin were employed as a standard for analgesic and anti-inflammatory studies, respectively. Our present study demonstrated that Centella asiatica bears significant analgesic and anti-inflammatory activities in those models.

Research paper thumbnail of A new ester of fatty acid from a methanol extract of the whole plant of Amaranthus spinosus and its α-glucosidase inhibitory activity

Pharmaceutical biology, 2015

Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as "spiny pigweed", ... more Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as "spiny pigweed", is used both in the Indian traditional system and in folk medicine to treat diabetes. The present study evaluates the scientific basis of antidiabetic activity of chloroform fraction of methanol extract of A. spinosus and of an isolated constituent of A. spinosus. HPLC analysis was performed to determine the purity and the amount of the constituent present in the plant extract. The yeast α-glucosidase inhibition technique was used to determine the antidiabetic activity of A. spinosus. Acarbose was used as a standard. An appropriate therapeutic approach for preventing diabetes mellitus and obesity is to retard the absorption of glucose by inhibition of α-glucosidase. One novel fatty acid with strong α-glucosidase inhibitory activity - (14E, 18E, 22E, 26E) - methyl nonacosa-14, 18, 22, 26 tetraenoate [1] (IC50 value 6.52 µM/mL) and β-sitosterol [2] were purified. Compound 1 was found to be...

Research paper thumbnail of Synthesis and anticancer evaluation of 5-benzyl-1,3,4-thiadiazol-2-amine derivatives on Ehrlich ascites carcinoma bearing mice

5-benzyl-1,3,4-thiadiazol-2-amine derivatives (2-12) were synthesized by reaction of 5-benzyl-1,3... more 5-benzyl-1,3,4-thiadiazol-2-amine derivatives (2-12) were synthesized by reaction of 5-benzyl-1,3,4-thiadiazol-2- amine with different substituted phenyl isocyanates or phenyl isothiocyanates. Structures of all compounds were established on the basis of FT-IR, 1HNMR, and LC-MS spectral data. The effects of all compounds on in-vivo tumor growth inhibition were evaluated by studying the parameters such as tumor volume, tumor cell count (viable and non-viable), haematological values, and mean survival time of carcinoma cells bearing mice. Among the tested compounds, compound 2 (54.63%), 3 (60.8%), and 11 (51.54%) showed significant tumor growth inhibition and compared favourably with the standard anticancer drug 5-fluorouracil