Pub Date : 2022-03-30DOI: 10.25004/ijpsdr.2022.140111
B. Fegade, S. Jadhav
The Claisen-Schmidt condensation of 4-(aryl)-aminobenzaldehyde and 2-hydroxyacetophenone resulted in a new series of heterocyclic chalcone (4a-4g) derivatives. Nucleophilic aromatic substitution (SNAr) of 4-fluorobenzaldehyde with heterocycle amines by ultrasonication in the presence of a base and polar aprotic solvent yielde 4-(aryl)-aminobenzaldehydes. Spectral investigations were used to establish the structures of synthesized compounds. The in vitro anti-cancer activity of the synthesized derivative was evaluated against MCF-7 (breast cancer) cells by SRB assay. Compounds 4c, 4b, and 4c have a high affinity for the ER receptor binding site, whereas compounds 4c and 4g have a moderate affinity for the VEGER-2 receptor. The GI50 value of 4c ((E)-1-(2-hydroxyphenyl)-3-(4-(4-methylpiperazin-1-yl)-phenyl) prop-2-en-1-one) was 44.6 uM, while the GI50 value of all other derivatives was greater than 80 uM. These findings lay the groundwork for additional research into the combination's potential uses in cancer therapy.
{"title":"Design, Synthesis and Molecular Docking Study of N-Heterocyclic Chalcone Derivatives as an Anti-cancer Agents","authors":"B. Fegade, S. Jadhav","doi":"10.25004/ijpsdr.2022.140111","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140111","url":null,"abstract":"The Claisen-Schmidt condensation of 4-(aryl)-aminobenzaldehyde and 2-hydroxyacetophenone resulted in a new series of heterocyclic chalcone (4a-4g) derivatives. Nucleophilic aromatic substitution (SNAr) of 4-fluorobenzaldehyde with heterocycle amines by ultrasonication in the presence of a base and polar aprotic solvent yielde 4-(aryl)-aminobenzaldehydes. Spectral investigations were used to establish the structures of synthesized compounds. The in vitro anti-cancer activity of the synthesized derivative was evaluated against MCF-7 (breast cancer) cells by SRB assay. Compounds 4c, 4b, and 4c have a high affinity for the ER receptor binding site, whereas compounds 4c and 4g have a moderate affinity for the VEGER-2 receptor. The GI50 value of 4c ((E)-1-(2-hydroxyphenyl)-3-(4-(4-methylpiperazin-1-yl)-phenyl) prop-2-en-1-one) was 44.6 uM, while the GI50 value of all other derivatives was greater than 80 uM. These findings lay the groundwork for additional research into the combination's potential uses in cancer therapy.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90806874","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-30DOI: 10.25004/ijpsdr.2022.140110
Vijay K. Sharma, Anuka Sharma, Parag R Ghorpade, M. Nandanwar, A. Kansagara, S. Tripathi
A debilitating complication of diabetes mellitus is diabetic ulcers, which leads to increased overall morbidity in patients. The high growth factor content in Platelet Rich Plasma (PRP) makes it a widely used intervention for the treatment of diabetic foot ulcers. The topical application of Stromal Vascular Fraction (SVF) could possibly enhance wound healing. This study aims at evaluating the efficacy of combining SVF and PRP on wound healing in diabetic rabbit model. Diabetes was induced in New Zealand white rabbits by intravenous injection of 125 mg/Kg Alloxan. After two weeks of alloxan, three 6 mm diameter, full thickness excision wounds were made, on inner side of the right ear pinna. The animals after induction were allocated into 4 groups with [8 Diabetic (treated with SVF+PRP), 4 Diabetic (treated with 10% Povidone Iodine (PI)), 1 non-diabetic (treated with SVF+PRP), 1 non diabetic (treated with 10% PI)]. The effect of combined therapy was evaluated by assessing wound margin closure rate, histo-pathological evaluation, and inflammatory cell infiltration, epithelization of ulcerative region, neo-vascularization, and fibrosis. We observed that the rate of wound closure is enhanced in wounds treated with SVF+PRP as compared to the PI solution. Wound closure and healthy healing were demonstrated by histo-pathological analysis. The analysis clearly indicates that the healing process of PI treated animals is slower than that of SVF + PRP treated animals. In conclusion, based on wound healing assessment and histo-pathological examination, the diabetic rabbits treated with SVF + PRP exhibited early development of granulation tissue and early signs of wound closure as compared to diabetic animals with normal PI dressing
{"title":"Evaluation of Healing Effect of Stromal Vascular Fraction and Platelet Rich Plasma Application on Ulcerative Ear Wound in Diabetic Rabbit","authors":"Vijay K. Sharma, Anuka Sharma, Parag R Ghorpade, M. Nandanwar, A. Kansagara, S. Tripathi","doi":"10.25004/ijpsdr.2022.140110","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140110","url":null,"abstract":"A debilitating complication of diabetes mellitus is diabetic ulcers, which leads to increased overall morbidity in patients. The high growth factor content in Platelet Rich Plasma (PRP) makes it a widely used intervention for the treatment of diabetic foot ulcers. The topical application of Stromal Vascular Fraction (SVF) could possibly enhance wound healing. This study aims at evaluating the efficacy of combining SVF and PRP on wound healing in diabetic rabbit model. Diabetes was induced in New Zealand white rabbits by intravenous injection of 125 mg/Kg Alloxan. After two weeks of alloxan, three 6 mm diameter, full thickness excision wounds were made, on inner side of the right ear pinna. The animals after induction were allocated into 4 groups with [8 Diabetic (treated with SVF+PRP), 4 Diabetic (treated with 10% Povidone Iodine (PI)), 1 non-diabetic (treated with SVF+PRP), 1 non diabetic (treated with 10% PI)]. The effect of combined therapy was evaluated by assessing wound margin closure rate, histo-pathological evaluation, and inflammatory cell infiltration, epithelization of ulcerative region, neo-vascularization, and fibrosis. We observed that the rate of wound closure is enhanced in wounds treated with SVF+PRP as compared to the PI solution. Wound closure and healthy healing were demonstrated by histo-pathological analysis. The analysis clearly indicates that the healing process of PI treated animals is slower than that of SVF + PRP treated animals. In conclusion, based on wound healing assessment and histo-pathological examination, the diabetic rabbits treated with SVF + PRP exhibited early development of granulation tissue and early signs of wound closure as compared to diabetic animals with normal PI dressing","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78955268","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-30DOI: 10.25004/ijpsdr.2022.140116
S. Swarnakar, A. Manna, Tapasi Roy, Tanusree Das, S. Bandyopadhyay
Plants provide natural molecules as an effective agent for phytomedicine. Anticancer properties of natural products are well described. Several studies on hydroxychavicol (HCH), and plumbagin (PLB), which are found in Piper betle leaf and Plumbago sp. respectively, are evidenced as anti-carcinogenic effect on chronic myeloid leukemic (CML) cells through increased reactive oxygen species (ROS). An attempt was taken to determine the efficacy of a new combination of HCH and PLB on CML cells (K562) and the mechanism of apoptosis thereon. 3-{4,5-Dimethylthiazol-2-yl}-2,5-diphenyltetrazolium bromide (MTT) assay was performed to determine the dose for individual and combination treatments of HCH and PLB against leukemic cells, (K562). Apoptotic activity was assessed through flow cytometric analysis with annexin V-FITC/propidium iodide staining. Immunoblots were also performed on cell extracts before and after the treatments. Levels of ROS and nitric oxide (NO) in K562 cells were measured by DCF-DA and DAF-FM staining, respectively. In addition, P38 and JNK siRNA transfection were performed to assess the roles of mitogen-activated protein kinase (MAPK) pathways on apoptosis. Combination treatments of HCH (16 µM) and PLB (0.5 µM) showed synergistic effects on reducing viability and increased cellular apoptosis of K562 cells. Combined treatments showed elevated reactive oxygen species (ROS) and NO levels than individual treatments of HCH and PLB. Moreover, decreasing the ROS generations by antioxidants/ catalase reversed cell deaths and increased viability. Immunoblotting of MAPK pathways components showed reduction of pERK levels, while upregulation pJNK and pP38 levels upon HCH+PLB treatments. Furthermore, silencing of JNK and/or P38 rescued the K562 cells from deaths. The present study indicates combination treatments of HCH and PLB act as a better therapeutic against CML by promoting MAPK-mediated apoptosis via increased oxidative and nitrosative stress. This in vitro approach is the first report describing the mechanism of action of HCH/PLB to fight against Leukemia via interaction with phosphorylated P38.
{"title":"Potency of Phytocompounds as Hydroxychavicol and Plumbagin in Combination to Fight Against Leukemia via Activation of MAPKMediated Apoptotic Pathway: An In vitro Approach","authors":"S. Swarnakar, A. Manna, Tapasi Roy, Tanusree Das, S. Bandyopadhyay","doi":"10.25004/ijpsdr.2022.140116","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140116","url":null,"abstract":"Plants provide natural molecules as an effective agent for phytomedicine. Anticancer properties of natural\u0000products are well described. Several studies on hydroxychavicol (HCH), and plumbagin (PLB), which are found\u0000in Piper betle leaf and Plumbago sp. respectively, are evidenced as anti-carcinogenic effect on chronic myeloid\u0000leukemic (CML) cells through increased reactive oxygen species (ROS). An attempt was taken to determine the\u0000efficacy of a new combination of HCH and PLB on CML cells (K562) and the mechanism of apoptosis thereon.\u00003-{4,5-Dimethylthiazol-2-yl}-2,5-diphenyltetrazolium bromide (MTT) assay was performed to determine the dose\u0000for individual and combination treatments of HCH and PLB against leukemic cells, (K562). Apoptotic activity was\u0000assessed through flow cytometric analysis with annexin V-FITC/propidium iodide staining. Immunoblots were\u0000also performed on cell extracts before and after the treatments. Levels of ROS and nitric oxide (NO) in K562 cells\u0000were measured by DCF-DA and DAF-FM staining, respectively. In addition, P38 and JNK siRNA transfection were\u0000performed to assess the roles of mitogen-activated protein kinase (MAPK) pathways on apoptosis. Combination\u0000treatments of HCH (16 µM) and PLB (0.5 µM) showed synergistic effects on reducing viability and increased\u0000cellular apoptosis of K562 cells. Combined treatments showed elevated reactive oxygen species (ROS) and NO\u0000levels than individual treatments of HCH and PLB. Moreover, decreasing the ROS generations by antioxidants/\u0000catalase reversed cell deaths and increased viability. Immunoblotting of MAPK pathways components showed\u0000reduction of pERK levels, while upregulation pJNK and pP38 levels upon HCH+PLB treatments. Furthermore,\u0000silencing of JNK and/or P38 rescued the K562 cells from deaths. The present study indicates combination\u0000treatments of HCH and PLB act as a better therapeutic against CML by promoting MAPK-mediated apoptosis via\u0000increased oxidative and nitrosative stress. This in vitro approach is the first report describing the mechanism of\u0000action of HCH/PLB to fight against Leukemia via interaction with phosphorylated P38.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77196388","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-30DOI: 10.25004/ijpsdr.2022.140118
Atul Desai, K. Desai, Hem Desai, R. Desai, Chirag V Desai
The world has seen various variants of coronavirus and attempting all the feasible options to combat this pandemic situation. By far, vaccination is the most remarkable approach in controlling the Pandemic. India is fighting against the delta variant of the second wave COVID-19. Meanwhile, World Health Organization has already warned about the initial stages of the third wave in all countries. Therefore, on considering the variants of coronavirus, no standard option of care is available to date. In this article, we present a case study on the clinical outcome of the integrated treatment approach in COVID-19 patients suffering from critical conditions. The patient with a history of coronavirus was advised of strict home quarantine and standard treatment of care for 14 days. She was brought to the COVID-19 healthcare center in an unconscious state by her family. On examination, she had a 79% oxygen saturation, heart rate 88 beats/minute and her laboratory findings: CRP 37.3(mg/dL), ESR 84(mm/hour), D-dimer 793(ng/mL), and RBS 158 mg/d. After receiving consent from her family members, we initiated the integrated treatment approach. It includes T-AYU-HM Premium 600mg, is a herbo-mineral formulation, and Acupen 600 mg thrice a day with modern medicines. By adhering to the treatment, she recovered completely within a one-month duration. Her HRCT report showed a significant reduction in lung involvement with ill-defined low-density ground-glass opacities and atelectatic bands in both lungs. The patient's vitals and laboratory parameters presented striking improvement. This case study provides information about the effect of the integrated treatment approach in critical COVID-19 cases.
{"title":"Case Report Study of an Integrated Treatment Approach in Critical Case of COVID-19 Patient","authors":"Atul Desai, K. Desai, Hem Desai, R. Desai, Chirag V Desai","doi":"10.25004/ijpsdr.2022.140118","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140118","url":null,"abstract":"The world has seen various variants of coronavirus and attempting all the feasible options to combat this\u0000pandemic situation. By far, vaccination is the most remarkable approach in controlling the Pandemic. India\u0000is fighting against the delta variant of the second wave COVID-19. Meanwhile, World Health Organization\u0000has already warned about the initial stages of the third wave in all countries. Therefore, on considering the\u0000variants of coronavirus, no standard option of care is available to date. In this article, we present a case study\u0000on the clinical outcome of the integrated treatment approach in COVID-19 patients suffering from critical\u0000conditions. The patient with a history of coronavirus was advised of strict home quarantine and standard\u0000treatment of care for 14 days. She was brought to the COVID-19 healthcare center in an unconscious state\u0000by her family. On examination, she had a 79% oxygen saturation, heart rate 88 beats/minute and her\u0000laboratory findings: CRP 37.3(mg/dL), ESR 84(mm/hour), D-dimer 793(ng/mL), and RBS 158 mg/d. After\u0000receiving consent from her family members, we initiated the integrated treatment approach. It includes\u0000T-AYU-HM Premium 600mg, is a herbo-mineral formulation, and Acupen 600 mg thrice a day with modern\u0000medicines. By adhering to the treatment, she recovered completely within a one-month duration. Her\u0000HRCT report showed a significant reduction in lung involvement with ill-defined low-density ground-glass\u0000opacities and atelectatic bands in both lungs. The patient's vitals and laboratory parameters presented\u0000striking improvement. This case study provides information about the effect of the integrated treatment\u0000approach in critical COVID-19 cases.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72966586","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-30DOI: 10.25004/ijpsdr.2022.140119
Kiran Dudhat, H. Patel
Drug particles less than 5 µm have the greatest probability of deposition in the lung, whereas those less than 2 µm tend to be concentrated in the alveoli. A large proportion of particles within the 2-5 μm range are present in the dose released from the inhaled drug, providing a relatively even distribution across the lungs. The efficient need for inhaled therapy highly depends on the essence of the method of drug delivery and the patient's ability to correctly use the system. A large range of inhaler products, each with positive and negative aspects, are on the market. It facilitates the administration of a lower dose; there is a quicker onset of action and less severe side effects. The deposition of the inhaled drug in the lung is dependent on particle size, inhalation technique and the type of inhaler device. Importance of particle size distribution and Particle aerodynamic diameter, Influence of environmental humidity on particle size Particle deposition in the airways, Methods to identify drug deposition in lungs, Physiological factors which affect the therapeutic efficacy of pulmonary delivery drugs. The nano and micro size particles is a mainstay of treatment for a variety of pulmonary diseases because they provide a platform to deliver drugs directly reliably and inexpensively to the disease site, thus allowing for a minimum amount of drug to be used and minimize side effects.
{"title":"Influence of Particle Size and Particle Deposition of Inhaled Medication in Lung Disease: A Comrehensive Review","authors":"Kiran Dudhat, H. Patel","doi":"10.25004/ijpsdr.2022.140119","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140119","url":null,"abstract":"Drug particles less than 5 µm have the greatest probability of deposition in the lung, whereas those less than 2 µm tend to be concentrated in the alveoli. A large proportion of particles within the 2-5 μm range are present in the dose released from the inhaled drug, providing a relatively even distribution across the lungs. The efficient need for inhaled therapy highly depends on the essence of the method of drug delivery and the patient's ability to correctly use the system. A large range of inhaler products, each with positive and negative aspects, are on the market. It facilitates the administration of a lower dose; there is a quicker onset of action and less severe side effects. The deposition of the inhaled drug in the lung is dependent on particle size, inhalation technique and the type of inhaler device. Importance of particle size distribution and Particle aerodynamic diameter, Influence of environmental humidity on particle size Particle deposition in the airways, Methods to identify drug deposition in lungs, Physiological factors which affect the therapeutic efficacy of pulmonary delivery drugs. The nano and micro size particles is a mainstay of treatment for a variety of pulmonary diseases because they provide a platform to deliver drugs directly reliably and inexpensively to the disease site, thus allowing for a minimum amount of drug to be used and minimize side effects.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84690122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-29DOI: 10.25004/ijpsdr.2022.140107
Veluru Hari, D. Jothieswari, K. S. Maheswaramma
Polyphenolics such as tannins and flavonoids are proved as powerful antioxidants to resolve cellular stress, sustain homeostasis in the body and prevent stress-associated disorders. Plant-based medicine gained importance due to its safety margin and multiple benefits. Regular intake of antioxidants is an alternative to avoid serious illness. The current investigation is aimed to measure the phenolic, flavonoid content, the antioxidant activity of Justicia tranquebariensis L.f. and Cycas beddomei leaves. The selected plants are used by tribes and traditional medicine to cure various diseases. Total phenolic content was estimated using the Folin–Ciocalteu colorimetric method, taking gallic acid as standard. At the same time, total flavonoid content was determined by aluminum chloride colorimetric assay using Rutin as standard.The absorbance was measured at 760 nm and 510 nm, respectively. Antioxidant activity was measured by two In vitro methods (DPPH and NO free radical scavenging assay) using standard protocols, where Ascorbic acid served as a reference standard. Results disclosed that the total phenolic content for the methanolic extracts of C. beddomei (36.14 ± 1.72) and J. tranquebariensis (28.57 ± 0.91) was found to be higher than petroleum ether extracts. Similarly, C. beddomei (28.13 ± 2.48) is richer in flavonoids than Jtranquebariensis (20.32 ± 1.24). In DPPH assay, methanolic extract C. beddomei (78.21%) is more effective to inhibit the free radicals than J. tranquebariensis (73.05%) with IC50 values 41.55µg/ml and 59.52 µg/ml respectively at higher doses that are comparable to standard ascorbic acid (84.34%, IC50 =63.27 µg/ml). Similarly, in NO free radical scavenging assay, methanolic extract of C. beddomei (72.54%) stood best among all to scavenge the free radicals with IC50 values 50.06 µg/ml, whereas ascorbic acid is found to inhibit 83.26% with IC50 values 39.75µg/ml. The presence of various secondary metabolites such as alkaloids, carbohydrates, phenols, steroids, terpenoids, glycosides, saponins, especially tannins and flavonoids, either alone or in combination, may be responsible for the observed scavenging property. The quantity of the phenolic compounds and flavonoids can be directly correlated to the exhibited activity.
{"title":"Total Phenolic, Flavonoid Content, and Antioxidant Activity of Justicia tranquebariensis LF and Cycas Beddomei Dyer. Leaves","authors":"Veluru Hari, D. Jothieswari, K. S. Maheswaramma","doi":"10.25004/ijpsdr.2022.140107","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140107","url":null,"abstract":"Polyphenolics such as tannins and flavonoids are proved as powerful antioxidants to resolve cellular stress, sustain homeostasis in the body and prevent stress-associated disorders. Plant-based medicine gained importance due to its safety margin and multiple benefits. Regular intake of antioxidants is an alternative to avoid serious illness. The current investigation is aimed to measure the phenolic, flavonoid content, the antioxidant activity of Justicia tranquebariensis L.f. and Cycas beddomei leaves. The selected plants are used by tribes and traditional medicine to cure various diseases. Total phenolic content was estimated using the Folin–Ciocalteu colorimetric method, taking gallic acid as standard. At the same time, total flavonoid content was determined by aluminum chloride colorimetric assay using Rutin as standard.The absorbance was measured at 760 nm and 510 nm, respectively. Antioxidant activity was measured by two In vitro methods (DPPH and NO free radical scavenging assay) using standard protocols, where Ascorbic acid served as a reference standard. Results disclosed that the total phenolic content for the methanolic extracts of C. beddomei (36.14 ± 1.72) and J. tranquebariensis (28.57 ± 0.91) was found to be higher than petroleum ether extracts. Similarly, C. beddomei (28.13 ± 2.48) is richer in flavonoids than Jtranquebariensis (20.32 ± 1.24). In DPPH assay, methanolic extract C. beddomei (78.21%) is more effective to inhibit the free radicals than J. tranquebariensis (73.05%) with IC50 values 41.55µg/ml and 59.52 µg/ml respectively at higher doses that are comparable to standard ascorbic acid (84.34%, IC50 =63.27 µg/ml). Similarly, in NO free radical scavenging assay, methanolic extract of C. beddomei (72.54%) stood best among all to scavenge the free radicals with IC50 values 50.06 µg/ml, whereas ascorbic acid is found to inhibit 83.26% with IC50 values 39.75µg/ml. The presence of various secondary metabolites such as alkaloids, carbohydrates, phenols, steroids, terpenoids, glycosides, saponins, especially tannins and flavonoids, either alone or in combination, may be responsible for the observed scavenging property. The quantity of the phenolic compounds and flavonoids can be directly correlated to the exhibited activity.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80784487","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-29DOI: 10.25004/ijpsdr.2022.140105
Arunchandra Singh, Roushan Kumari, S. Bharti
Diabetes mellitus is a metabolic disorder that causes chronic hyperglycemia. Diabetes and its crippling complications are a significant cause of morbidity and mortality. This study evaluates the comparative antihyperglycemic and hepatoprotective effects of alcoholic extracts of rhizome of Zinger officinale plant and seed extract of Cuminum cyminum plant on alloxan-induced diabetic mice. Mice were divided into four groups (one normal control, one diabetic control and two diabetic groups treated with the two extracts). Mice were induced diabetes by intraperitoneal administration of alloxan. Normal control and diabetic control mice received normal saline water during the treatment period while diabetic mice were administrated with ethanolic extracts of ginger rhizome @100mg/kg/BW and cumin seeds extract @80mg/kg/BW for 16 weeks. At the end of the experiment, animals were sacrificed, and biochemical as well as histopathological examinations were carried out. Hyperglycaemia with increased SGPT and bilirubin have been observed in diabetic mice. However, normoglycemic conditions along with restored liver marker enzymes have been observed in diabetic rats treated with extracts. Histopathological examination showed that alloxan administration causes damage to hepatic cells. Conversely, in ginger and cumin-treated diabetic groups, a significant improvement in the architecture of hepatic cells has been observed, which showed the ability of the extracts to repair the damaged tissue. Thus, this study safely submitted that ginger and cumin significantly reduce the blood glucose level, with ginger having greater potential as a hepatoprotective agent than cumin.
{"title":"Comparative Phyto-Remedial Effect of Zingiber officinale and Cuminum cyminum on Hepatocytes of Alloxan Induced Diabetic Mus musculus","authors":"Arunchandra Singh, Roushan Kumari, S. Bharti","doi":"10.25004/ijpsdr.2022.140105","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140105","url":null,"abstract":"Diabetes mellitus is a metabolic disorder that causes chronic hyperglycemia. Diabetes and its crippling complications are a significant cause of morbidity and mortality. This study evaluates the comparative antihyperglycemic and hepatoprotective effects of alcoholic extracts of rhizome of Zinger officinale plant and seed extract of Cuminum cyminum plant on alloxan-induced diabetic mice. Mice were divided into four groups (one normal control, one diabetic control and two diabetic groups treated with the two extracts). Mice were induced diabetes by intraperitoneal administration of alloxan. Normal control and diabetic control mice received normal saline water during the treatment period while diabetic mice were administrated with ethanolic extracts of ginger rhizome @100mg/kg/BW and cumin seeds extract @80mg/kg/BW for 16 weeks. At the end of the experiment, animals were sacrificed, and biochemical as well as histopathological examinations were carried out. Hyperglycaemia with increased SGPT and bilirubin have been observed in diabetic mice. However, normoglycemic conditions along with restored\u0000liver marker enzymes have been observed in diabetic rats treated with extracts. Histopathological\u0000examination showed that alloxan administration causes damage to hepatic cells. Conversely, in ginger\u0000and cumin-treated diabetic groups, a significant improvement in the architecture of hepatic cells has been observed, which showed the ability of the extracts to repair the damaged tissue. Thus, this study safely submitted that ginger and cumin significantly reduce the blood glucose level, with ginger having greater potential as a hepatoprotective agent than cumin.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79814147","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-28DOI: 10.25004/ijpsdr.2022.140106
V. Sumitha, I. Mini, Laija. S. Nair
Medicinal plants occupy a key position in maintaining the health of the human population. Hyptis capitataJacq. is an exotic ethnomedicinal plant of Lamiaceae possessing immense potential. The present study was carried out to assess the in vitro hepatoprotective activity of methanolic leaf extract of H. capitata against H2O2 induced oxidative stress in HepG2 cell lines. Total antioxidant capacity and Superoxide radical scavenging activity of the extract were also performed. The extract displayed considerable free radical scavenging activity (P IS LESS THAN 0.01). MTT assay was used to assess the in vitro hepatoprotective activity in HepG2 cell lines. The extract displayed concentration-dependent cell viability with maximum protection (63.97 ± 1.23%) in H2O2 induced HepG2 cell lines at 100 μgml-1. H. capitata is a promising herb with significant antioxidant and hepatoprotective potential.
{"title":"Assessment of Hepatoprotective Activity of Hyptis capitata Jacq. Against Oxidative Stress Induced by H2O2","authors":"V. Sumitha, I. Mini, Laija. S. Nair","doi":"10.25004/ijpsdr.2022.140106","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140106","url":null,"abstract":"Medicinal plants occupy a key position in maintaining the health of the human population. Hyptis capitataJacq. is an exotic ethnomedicinal plant of Lamiaceae possessing immense potential. The present study was carried out to assess the in vitro hepatoprotective activity of methanolic leaf extract of H. capitata against H2O2 induced oxidative stress in HepG2 cell lines. Total antioxidant capacity and Superoxide radical scavenging activity of the extract were also performed. The extract displayed considerable free radical scavenging activity (P IS LESS THAN 0.01). MTT assay was used to assess the in vitro hepatoprotective activity in HepG2 cell lines. The extract displayed concentration-dependent cell viability with maximum protection (63.97 ± 1.23%) in H2O2 induced HepG2 cell lines at 100 μgml-1. H. capitata is a promising herb with significant antioxidant and hepatoprotective potential.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74663874","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-11DOI: 10.25004/ijpsdr.2022.140104
R. Salfi, Fatima Shireen, M. Ajitha
The current study aimed to formulate an elementary osmotic pump (EOP) and push-pull osmotic pump (PPOP) based drug delivery system for controlled release of an anti-diabetic agent, repaglinide is expected to provide sustained release. EOP and PPOP method prepared repaglinide tablets by wet granulation technique. EOP designed 15 formulations F1-F15 and 14 formulations were done by PPOP method. All the formulations were evaluated for various physicochemical parameters and in-vitro dissolution studies. The release data was fitted into mathematical kinetic modeling studies to check the release mechanism. Further, the optimized formulations from both methods were characterized by FTIR and stability studies. EOP and PPOP methods successfully prepared repaglinide osmotic tablets. All the formulations exhibitedb satisfactory results for all evaluated parameters. The highest drug release was exhibited from F15 prepared by EOP method with 99.76% and FF14 with 15% coating prepared by PPOP method with drug release of 99.73%. Based on the in vitro dissolution profile, formulation F15 and FF14 exhibited zero-order with Korsmeyer-Peppas kinetics with Fickian diffusion-controlled release mechanism with high drug release in 24 hours and hence were selected as optimized formulations. The drug-excipient compatibility study by FTIR indicated no significant interactions between drugs and excipients. The formulations were stable after 3 months of accelerated stability studies. EOP and PPOP were designed to effectively administrate repaglinide drugs for a prolonged period of time.
{"title":"Optimization of Repaglinide Osmotic Drug Delivery System Using Two Different Techniques","authors":"R. Salfi, Fatima Shireen, M. Ajitha","doi":"10.25004/ijpsdr.2022.140104","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140104","url":null,"abstract":"The current study aimed to formulate an elementary osmotic pump (EOP) and push-pull osmotic pump (PPOP) based drug delivery system for controlled release of an anti-diabetic agent, repaglinide is expected to provide sustained release. EOP and PPOP method prepared repaglinide tablets by wet granulation technique. EOP designed 15 formulations F1-F15 and 14 formulations were done by PPOP method. All the formulations were evaluated for various physicochemical parameters and in-vitro dissolution studies. The release data was fitted into mathematical kinetic modeling studies to check the release mechanism. Further, the optimized formulations from both methods were characterized by FTIR and stability studies. EOP and PPOP methods successfully prepared repaglinide osmotic tablets. All the formulations exhibitedb satisfactory results for all evaluated parameters. The highest drug release was exhibited from F15 prepared by EOP method with 99.76% and FF14 with 15% coating prepared by PPOP method with drug release of 99.73%. Based on the in vitro dissolution profile, formulation F15 and FF14 exhibited zero-order with Korsmeyer-Peppas kinetics with Fickian diffusion-controlled release mechanism with high drug release in 24 hours and hence were selected as optimized formulations. The drug-excipient compatibility study by FTIR indicated no significant interactions between drugs and excipients. The formulations were stable after 3 months of accelerated stability studies. EOP and PPOP were designed to effectively administrate repaglinide drugs for a prolonged period of time.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89373239","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-01-31DOI: 10.25004/ijpsdr.2022.140102
T. R. R. Naik, G. Mahanthesha, T. Suresh
A novel series of (4-Fluorophenyl (1-(5-phenyl-1,3,4-oxadiazol-2-yl)indolizin-3-yl)methanone derivatives 9(a-n) were synthesized by the coupling reaction of 3-(4-fluorobenzoyl)indolizine-1-carboxylic acid and substituted benzohydrazide followed by intramolecular cyclization. The structures of the compounds were characterized by 1 H NMR, 13C NMR, LCMS, FT-IR, and elemental analyses. The compounds 9(a-n) anti-cancer activity was evaluated against the MCF-7 cell line (HTB-22, Homo sapiens, Breast carcinoma). Compound 9j (IC50 = 21.57 µM), and 9n (IC50 = 8.52 µM) exhibited the most potent cytotoxicity activity compared with standard drug doxorubicin (IC50= 25.71). The antibacterial activity was evaluated against Staphylococcus aureus ATCC 6538 and Escherichia coli ATCC 8739. The compounds ZOI=16mm) and 9i (ZOI=18 mm) exhibited moderate antibacterial activity compared with standard drug ciprofloxacin. The antifungal activity was evaluated against Candida albicans ATCC 10231. Most compounds exhibited moderate antifungal activity compared with the standard drug Itraconazole.
{"title":"Synthesis and Biological Evaluation of (4-Fluorophenyl)(1-(5-phenyl-1,3,4-oxadiazol-2-yl)indolizin-3-yl)methanone Derivatives as Anti-cancer and Antimicrobial Agents","authors":"T. R. R. Naik, G. Mahanthesha, T. Suresh","doi":"10.25004/ijpsdr.2022.140102","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140102","url":null,"abstract":"A novel series of (4-Fluorophenyl (1-(5-phenyl-1,3,4-oxadiazol-2-yl)indolizin-3-yl)methanone derivatives\u00009(a-n) were synthesized by the coupling reaction of 3-(4-fluorobenzoyl)indolizine-1-carboxylic acid and\u0000substituted benzohydrazide followed by intramolecular cyclization. The structures of the compounds\u0000were characterized by 1 H NMR, 13C NMR, LCMS, FT-IR, and elemental analyses. The compounds 9(a-n)\u0000anti-cancer activity was evaluated against the MCF-7 cell line (HTB-22, Homo sapiens, Breast carcinoma).\u0000Compound 9j (IC50 = 21.57 µM), and 9n (IC50 = 8.52 µM) exhibited the most potent cytotoxicity activity\u0000compared with standard drug doxorubicin (IC50= 25.71). The antibacterial activity was evaluated against\u0000Staphylococcus aureus ATCC 6538 and Escherichia coli ATCC 8739. The compounds ZOI=16mm) and 9i\u0000(ZOI=18 mm) exhibited moderate antibacterial activity compared with standard drug ciprofloxacin.\u0000The antifungal activity was evaluated against Candida albicans ATCC 10231. Most compounds exhibited\u0000moderate antifungal activity compared with the standard drug Itraconazole.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88183460","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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