Pub Date : 2021-08-01DOI: 10.13189/app.2021.090302
N. Ali
Various medicinal plants are found in the dense forest of Albaha region, southwest of Saudi Arabia. These plant species are natively utilized for the prevention and treatment of various diseases. This study was designed to analyze the chemical composition of ethanolic, petroleum ether, chloroform, and methanolic extracts of Rosmarinus officinalis (rosemary) collected from Albaha region and evaluate the antimicrobial and cytotoxic activities of these extracts. Fresh aerial parts of R. officinalis (stem and leaves) were used for extraction. Then the crude extracts were investigated by using gas chromatography- mass spectrometry (GC-MS) technique to determine their chemical constituents. Antimicrobial assays were performed using Bacillus subtilis and Staphylococcus aureus (Gram-positive bacteria), Escherichia coli (Gram-negative bacteria), and Candida albicans (fungus) to determine the antimicrobial activities. MTT assay was applied to MCF-7 (human breast cancer cell line) as well as on HCT-116 (human colon cancer cell line) to calculate the IC50 of different plant extracts. The GC-MS analysis showed that only petroleum ether extract has an abundance of cyclohexane compounds including 46.5% methyl-cyclohexane. Significant antibacterial and antifungal actions against the tested strains were shown by the petroleum ether and chloroform extracts in antimicrobial assay. Antibacterial activity against S. aureus (SA) and E. coli (EC) was exhibited by methanolic extract, whereas no effect was observed on B. subtilis (BS) and C. albicans (CA). In MTT assay, the petroleum ether extract showed the greatest cytotoxic activity against MCF-7 (3.77 μg/mL) and HCT-116 (3.09 μg/mL) cells. The extract of chloroform also displayed significant cytotoxic effect but only against MCF-7 with IC50 values of 12.7 µg/mL. The present study showed that the R. officinalis petroleum ether extract contains significant antimicrobial and cytotoxic activities which can be accredited to the plentiful manifestation of methyl-cyclohexane, methylbenzene and other cyclohexane derivatives, and it may be used to develop new antimicrobial and anticancer drugs.
{"title":"Phytochemical Screening and in Vitro Antimicrobial and Anticancer Activities of Different Extracts of Rosmarinus officinalis (Rosemary): A Comparative Study","authors":"N. Ali","doi":"10.13189/app.2021.090302","DOIUrl":"https://doi.org/10.13189/app.2021.090302","url":null,"abstract":"Various medicinal plants are found in the dense forest of Albaha region, southwest of Saudi Arabia. These plant species are natively utilized for the prevention and treatment of various diseases. This study was designed to analyze the chemical composition of ethanolic, petroleum ether, chloroform, and methanolic extracts of Rosmarinus officinalis (rosemary) collected from Albaha region and evaluate the antimicrobial and cytotoxic activities of these extracts. Fresh aerial parts of R. officinalis (stem and leaves) were used for extraction. Then the crude extracts were investigated by using gas chromatography- mass spectrometry (GC-MS) technique to determine their chemical constituents. Antimicrobial assays were performed using Bacillus subtilis and Staphylococcus aureus (Gram-positive bacteria), Escherichia coli (Gram-negative bacteria), and Candida albicans (fungus) to determine the antimicrobial activities. MTT assay was applied to MCF-7 (human breast cancer cell line) as well as on HCT-116 (human colon cancer cell line) to calculate the IC50 of different plant extracts. The GC-MS analysis showed that only petroleum ether extract has an abundance of cyclohexane compounds including 46.5% methyl-cyclohexane. Significant antibacterial and antifungal actions against the tested strains were shown by the petroleum ether and chloroform extracts in antimicrobial assay. Antibacterial activity against S. aureus (SA) and E. coli (EC) was exhibited by methanolic extract, whereas no effect was observed on B. subtilis (BS) and C. albicans (CA). In MTT assay, the petroleum ether extract showed the greatest cytotoxic activity against MCF-7 (3.77 μg/mL) and HCT-116 (3.09 μg/mL) cells. The extract of chloroform also displayed significant cytotoxic effect but only against MCF-7 with IC50 values of 12.7 µg/mL. The present study showed that the R. officinalis petroleum ether extract contains significant antimicrobial and cytotoxic activities which can be accredited to the plentiful manifestation of methyl-cyclohexane, methylbenzene and other cyclohexane derivatives, and it may be used to develop new antimicrobial and anticancer drugs.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"38 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2021-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81100870","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 : 2021-08-01DOI: 10.13189/app.2021.090303
A. Yousofi, Kawsar Alami, Sayed Yousof Mousavi
The purpose of this study is to evaluate the effect of Afghan Ferula assa-foetida L. and Crocus Sativus L. aqueous extracts either alone or in combination on morphine withdrawal signs. For this purpose, rats were randomly divided into 13 groups (1 Normal, 1 Morphine, 4 Ferula assa-foetida-treated groups, 4 Crocus sativus-treated groups, and 3 combination groups). Morphine dependency was rendered by subcutaneous injection of morphine hydrochloride for 4 days (10, 20 and 40 mg/kg doses twice daily for 3 days and a single dose of 60 mg/kg on 4th day). Various doses of extracts were injected into extract groups simultaneously with morphine. After two hours of last morphine administration, withdrawal signs were induced by naloxone (3 mg/kg) and noted for 30 minutes. According to the results, different doses of Ferula assa-foetida and Crocus sativus extracts and their combination (in low dose) could significantly decrease the number of morphine withdrawal signs (P<0.05). However, the combination of Ferula assa-foetida and Crocus sativus extracts in high doses showed toxic effects. In conclusion, Ferula assa-foetida and Crocus sativus extract combination in low dose can decrease the morphine withdrawal signs, but without any synergic effects.
{"title":"Effect of Afghan Ferula assa-foetida L. and Crocus Sativus L. Aqueous Extracts Combination on Withdrawal Signs in Morphine-Dependent Rats","authors":"A. Yousofi, Kawsar Alami, Sayed Yousof Mousavi","doi":"10.13189/app.2021.090303","DOIUrl":"https://doi.org/10.13189/app.2021.090303","url":null,"abstract":"The purpose of this study is to evaluate the effect of Afghan Ferula assa-foetida L. and Crocus Sativus L. aqueous extracts either alone or in combination on morphine withdrawal signs. For this purpose, rats were randomly divided into 13 groups (1 Normal, 1 Morphine, 4 Ferula assa-foetida-treated groups, 4 Crocus sativus-treated groups, and 3 combination groups). Morphine dependency was rendered by subcutaneous injection of morphine hydrochloride for 4 days (10, 20 and 40 mg/kg doses twice daily for 3 days and a single dose of 60 mg/kg on 4th day). Various doses of extracts were injected into extract groups simultaneously with morphine. After two hours of last morphine administration, withdrawal signs were induced by naloxone (3 mg/kg) and noted for 30 minutes. According to the results, different doses of Ferula assa-foetida and Crocus sativus extracts and their combination (in low dose) could significantly decrease the number of morphine withdrawal signs (P<0.05). However, the combination of Ferula assa-foetida and Crocus sativus extracts in high doses showed toxic effects. In conclusion, Ferula assa-foetida and Crocus sativus extract combination in low dose can decrease the morphine withdrawal signs, but without any synergic effects.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"17 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2021-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78788513","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 : 2021-08-01DOI: 10.13189/app.2021.090304
J. B., Kavya Yadav P G, Murali M., A. K N
Various reactive species which are either radicals or non radicals formed during normal metabolic processes. Oxidative stress has been identified as a major causative factor in the development and progression of several life threatening diseases, including neurodegenerative and cardiovascular disease, Antioxidants play a vital role in preventing or delaying oxidation and scavenging free radicals. Plants have been used as exogenous antioxidants from several years. In this contest, the rhizome extracts of two important medicinal plants Curcuma amada Roxb and Zingiber officinale Rosc were investigated for antioxidant properties and phytochemical constituents. Antioxidant capacity of different solvent extracts of these plants was estimated by scavenging diphenyl picryl hydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide. The petroleum ether and alcohol extracts of Curcuma amada showed stronger antioxidant activity with IC50 values of 26-30µg/ml and 25-29µg/ml, respectively in all the methods while methanol extract showed moderate activity, while petroleum ether and ethanol extracts Zingiber officinale reported good scavenging activity in all the three methods with IC50 ranging from 25-30µg/ml except hydroxyl radical scavenging method. Petroleum ether extracts of both the test plants exhibited good inhibition of free radicals generated by DPPH, hydrogen peroxide and nitric oxide when compared to standard ascorbic acid. The phenolic substances are commonly present in all the studied extracts. Among the two medicinal plants tested, Zingiber officinale has better scavenging activity in all the performed methods followed by Curcuma amada. In the present study, potent antioxidant activity of Zingiber officinale and Curcuma amada extracts leads to scientific validation of these plants. A natural substance which is a part of daily diet and nutritional supplement with antioxidant property constitutes a new source of herbal drug.
{"title":"Antioxidant and Phytochemical Studies of the Rhizome Extracts of Curcuma amada Roxb and Zingiber officinale Rosc","authors":"J. B., Kavya Yadav P G, Murali M., A. K N","doi":"10.13189/app.2021.090304","DOIUrl":"https://doi.org/10.13189/app.2021.090304","url":null,"abstract":"Various reactive species which are either radicals or non radicals formed during normal metabolic processes. Oxidative stress has been identified as a major causative factor in the development and progression of several life threatening diseases, including neurodegenerative and cardiovascular disease, Antioxidants play a vital role in preventing or delaying oxidation and scavenging free radicals. Plants have been used as exogenous antioxidants from several years. In this contest, the rhizome extracts of two important medicinal plants Curcuma amada Roxb and Zingiber officinale Rosc were investigated for antioxidant properties and phytochemical constituents. Antioxidant capacity of different solvent extracts of these plants was estimated by scavenging diphenyl picryl hydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide. The petroleum ether and alcohol extracts of Curcuma amada showed stronger antioxidant activity with IC50 values of 26-30µg/ml and 25-29µg/ml, respectively in all the methods while methanol extract showed moderate activity, while petroleum ether and ethanol extracts Zingiber officinale reported good scavenging activity in all the three methods with IC50 ranging from 25-30µg/ml except hydroxyl radical scavenging method. Petroleum ether extracts of both the test plants exhibited good inhibition of free radicals generated by DPPH, hydrogen peroxide and nitric oxide when compared to standard ascorbic acid. The phenolic substances are commonly present in all the studied extracts. Among the two medicinal plants tested, Zingiber officinale has better scavenging activity in all the performed methods followed by Curcuma amada. In the present study, potent antioxidant activity of Zingiber officinale and Curcuma amada extracts leads to scientific validation of these plants. A natural substance which is a part of daily diet and nutritional supplement with antioxidant property constitutes a new source of herbal drug.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"50 Suppl 1 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2021-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90995258","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 : 2021-08-01DOI: 10.13189/app.2021.090301
I. Syed, C. Patro, A. Alshanberi, S. Ansari
The present study involves the formulation and characterization of valsartan (VT) oral disintegrating tablets by using crospovidone (CP) and Hibiscus rosasinensis (HRS) mucilage as complexing agent. Valsartan (VT), anti-hypertensive drug (class II) is an orally active non-peptide triazole-derived antagonist of angiotensin II. The direct compression method was used to obtain 13 such formulations, and the tablets obtained were evaluated for drug content, hardness, friability (FT), disintegration time (DT) and dissolution rate. A significant increase in the dissolution rate of VT was obtained. FTIR and DSC studies showed no interaction between the drug and excipients. The amount of CP (X1) and amount to HRS mucilage (X2) is selected for 32 factorial designs. The DT (Y1), FT (Y2) and % drug released at 25 min (Y3) interval were taken as the response variables. X1 and X2 represents the result of changing the variable at a time from low level to high level. The interaction terms (X1X2, X12, X22, X12X2 and X1X22) exhibited that Y1, Y2 and Y3 had changed simultaneously (as analyzed by Design expert software 8 version). The contour and 3D plots revealed that there is an effect of X1 and X2 with the interaction on Y1, Y2 and Y3. F2 formulation exhibited minimum errors with CP and HRS in response to dependable variables which is concluded as best formulation.
{"title":"Statistical Designing and Characterization of Valsartan Oral Disintegrating Tablet","authors":"I. Syed, C. Patro, A. Alshanberi, S. Ansari","doi":"10.13189/app.2021.090301","DOIUrl":"https://doi.org/10.13189/app.2021.090301","url":null,"abstract":"The present study involves the formulation and characterization of valsartan (VT) oral disintegrating tablets by using crospovidone (CP) and Hibiscus rosasinensis (HRS) mucilage as complexing agent. Valsartan (VT), anti-hypertensive drug (class II) is an orally active non-peptide triazole-derived antagonist of angiotensin II. The direct compression method was used to obtain 13 such formulations, and the tablets obtained were evaluated for drug content, hardness, friability (FT), disintegration time (DT) and dissolution rate. A significant increase in the dissolution rate of VT was obtained. FTIR and DSC studies showed no interaction between the drug and excipients. The amount of CP (X1) and amount to HRS mucilage (X2) is selected for 32 factorial designs. The DT (Y1), FT (Y2) and % drug released at 25 min (Y3) interval were taken as the response variables. X1 and X2 represents the result of changing the variable at a time from low level to high level. The interaction terms (X1X2, X12, X22, X12X2 and X1X22) exhibited that Y1, Y2 and Y3 had changed simultaneously (as analyzed by Design expert software 8 version). The contour and 3D plots revealed that there is an effect of X1 and X2 with the interaction on Y1, Y2 and Y3. F2 formulation exhibited minimum errors with CP and HRS in response to dependable variables which is concluded as best formulation.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2021-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76454604","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}
Flunitrazepam (Rohypnol) is a benzodiazepine drug medically proscribed in United States whereas it’s legally prescribed in over sixty nations where the drug is administered as pre-anesthetic drug and in the treatment of insomnia but not without the loss of cerebral cortex functions which inspired this investigation to establish its neurotoxicity on the cerebral cortex of adult wistar rat. Sixteen adult female wistar rats were randomly divided into four groups with four rats in each group (A, B, C and D). Group A, the control group received distilled water. Groups B, C and D received 1mg/kg, 2mg/kg and 3mg/kg of Flunitrazepam (Rohypnol) respectively. The animals were sacrificed after three weeks of administration and the cerebral cortexes were harvested and fixed in 10% formal saline for histological processing and studies. The anthropometric investigation presented an insignificant increase in the relative body weight of the test groups when compared to the control group and also presented a significant increase in the relative organ weight in the entire test groups when compared to the control group. The cerebral cortex of experimental animals showed; severe lymphocytic infiltration, focal areas of liquefactive necrosis, intracerebral hemorrhage, vacuolation and various degrees of damages to the tissue layers and neuronal cells of the cerebral cortex. This scientific investigation indicates that consumption of Flunitrazepam (Rohypnol) across various graded doses causes changes in the cerebral cortex histoarchitecture which explains the rationale behind the loss of cerebral cortex function in drug addicts and patients placed on prolonged Flunitrazepam (Rohypnol) therapy.
{"title":"A Study on the Neurotoxicity of Flunitrazepam (Rohypnol) Administration on the Cerebral Cortex of Adult Wistar Rats","authors":"Udodi Princewill Sopuluchukwu, Ezejindu Damian Nnabuihe","doi":"10.13189/APP.2021.090202","DOIUrl":"https://doi.org/10.13189/APP.2021.090202","url":null,"abstract":"Flunitrazepam (Rohypnol) is a benzodiazepine drug medically proscribed in United States whereas it’s legally prescribed in over sixty nations where the drug is administered as pre-anesthetic drug and in the treatment of insomnia but not without the loss of cerebral cortex functions which inspired this investigation to establish its neurotoxicity on the cerebral cortex of adult wistar rat. Sixteen adult female wistar rats were randomly divided into four groups with four rats in each group (A, B, C and D). Group A, the control group received distilled water. Groups B, C and D received 1mg/kg, 2mg/kg and 3mg/kg of Flunitrazepam (Rohypnol) respectively. The animals were sacrificed after three weeks of administration and the cerebral cortexes were harvested and fixed in 10% formal saline for histological processing and studies. The anthropometric investigation presented an insignificant increase in the relative body weight of the test groups when compared to the control group and also presented a significant increase in the relative organ weight in the entire test groups when compared to the control group. The cerebral cortex of experimental animals showed; severe lymphocytic infiltration, focal areas of liquefactive necrosis, intracerebral hemorrhage, vacuolation and various degrees of damages to the tissue layers and neuronal cells of the cerebral cortex. This scientific investigation indicates that consumption of Flunitrazepam (Rohypnol) across various graded doses causes changes in the cerebral cortex histoarchitecture which explains the rationale behind the loss of cerebral cortex function in drug addicts and patients placed on prolonged Flunitrazepam (Rohypnol) therapy.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"45 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2021-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84667358","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 : 2021-02-01DOI: 10.13189/APP.2021.090101
R. Haleshappa, Sharangouda J. Patil, K. Murthy
Traditional Indian medicinal plant Simarouba glauca is a highly sacred plant known as “Paradise Tree or Lakshmi Taru” which is recognized for its pharmacological and pharmaceutical properties. The present study was envisaged to know the in vitro phytochemical, antioxidant and free radical scavenging activity of S. glauca seeds. Petroleum ether was used as a solvent to extract plant material using hot extraction method. In our investigation, phytochemical analysis was carried out qualitatively and quantitatively and for the evaluation of antioxidant profile carried out in vitro studies on free radical scavenging potential by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging, decolourization potential of 2,2’-azino-bis[3-ethyl benzthiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant potential (FRAP) assay were determined in in vitro studies. The qualitative phytochemical analysis of this plant was positive for flavonoids, fatty acids, proteins, steroids and terpenoids and in quantitative analysis total flavonoid content was 17.32±0.12 mg/μg quercetin equivalent, total proanthocyanidin content exhibited 62.91±0.61 µg catechin equivalent, total phenol content exhibited 17.75±5.82 μg gallic acid equivalent and the total flavonol content was 1.54±0.01 µg quercetin equivalent of the extract. In the antioxidant profile, the maximum DPPH scavenging activity exhibited was 74% with an IC 50 value 137.89 µg/mL, the maximum ABTS scavenging activity exhibited was 35% with an IC 50 value 337.29 µg/mL and FRAP scavenging activity exhibited 62.5 µg/mL as ascorbic acid equivalents (AAE/ml) concentration. These findings evidenced that, the petroleum ether extract of S. glauca seeds has potential source of natural antioxidants and can be used it as therapeutic medicine.
{"title":"Phytochemical Analysis, In Vitro Evaluation of Antioxidant and Free Radical Scavenging Activity of Simarouba glauca Seeds","authors":"R. Haleshappa, Sharangouda J. Patil, K. Murthy","doi":"10.13189/APP.2021.090101","DOIUrl":"https://doi.org/10.13189/APP.2021.090101","url":null,"abstract":"Traditional Indian medicinal plant Simarouba glauca is a highly sacred plant known as “Paradise Tree or Lakshmi Taru” which is recognized for its pharmacological and pharmaceutical properties. The present study was envisaged to know the in vitro phytochemical, antioxidant and free radical scavenging activity of S. glauca seeds. Petroleum ether was used as a solvent to extract plant material using hot extraction method. In our investigation, phytochemical analysis was carried out qualitatively and quantitatively and for the evaluation of antioxidant profile carried out in vitro studies on free radical scavenging potential by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging, decolourization potential of 2,2’-azino-bis[3-ethyl benzthiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant potential (FRAP) assay were determined in in vitro studies. The qualitative phytochemical analysis of this plant was positive for flavonoids, fatty acids, proteins, steroids and terpenoids and in quantitative analysis total flavonoid content was 17.32±0.12 mg/μg quercetin equivalent, total proanthocyanidin content exhibited 62.91±0.61 µg catechin equivalent, total phenol content exhibited 17.75±5.82 μg gallic acid equivalent and the total flavonol content was 1.54±0.01 µg quercetin equivalent of the extract. In the antioxidant profile, the maximum DPPH scavenging activity exhibited was 74% with an IC 50 value 137.89 µg/mL, the maximum ABTS scavenging activity exhibited was 35% with an IC 50 value 337.29 µg/mL and FRAP scavenging activity exhibited 62.5 µg/mL as ascorbic acid equivalents (AAE/ml) concentration. These findings evidenced that, the petroleum ether extract of S. glauca seeds has potential source of natural antioxidants and can be used it as therapeutic medicine.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"58 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2021-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80154867","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 : 2019-10-01DOI: 10.13189/APP.2019.070401
Iqra Iftikhar, A. Khalid, Zainab Bibi, A. Mehmood, Muhammad Rizwan, Sajid Khan, Anum Munir
Endometrial cancer is the fourth most common cancer in women. It arises from the endometrium and accompanied by the abnormal growth of the cells. Sign and symptoms include pelvic pain and abnormal vaginal bleeding. It has two categories. Type 1 tumors are estrogen-dependent and they have mutations in PTEN, PIK3CA while Type 2 tumors are more sensitive and have mutations in TP53. Overactivation of the signaling pathway (PI3K) results in anti-apoptosis. Here, this study aims to identify Tumor-Specific Antigen for germline mutations in endometrial cancer which can be used as a potential vaccine candidate. The germline mutations data are obtained from cancer gene census of the cosmic database. Genes mutating with crucial role in endometrial cancer are considered. Peptides libraries are generated using peptide design library. Human leukocyte antigen alleles are identified for the peptide library through NetMHC. Binding affinities of alleles with peptide are determined. Linear regression is performed to generate graphs. PTEN, TP53, PIK3CA, KRAS, and CTNNB1 proved to have critical role. About 575 overlapping peptide libraries are generated and each peptide has a length of 18-20 amino acids. Approximately 58 HLAs are identified, having strong interactions with HLAs. Regression analysis shows that the no. of mutations are directly associated with a binding affinity of peptides. From this, we suggest that the identified TSA can be used as personalized peptide vaccines that directly target the mutated genes in endometrial cancer. This research work can be used in the laboratories for further validation.
{"title":"Computational Prediction of Tumor-Specific Antigens as Potential Vaccine Candidates against Germ-line Mutations in Endometrial Cancer","authors":"Iqra Iftikhar, A. Khalid, Zainab Bibi, A. Mehmood, Muhammad Rizwan, Sajid Khan, Anum Munir","doi":"10.13189/APP.2019.070401","DOIUrl":"https://doi.org/10.13189/APP.2019.070401","url":null,"abstract":"Endometrial cancer is the fourth most common cancer in women. It arises from the endometrium and accompanied by the abnormal growth of the cells. Sign and symptoms include pelvic pain and abnormal vaginal bleeding. It has two categories. Type 1 tumors are estrogen-dependent and they have mutations in PTEN, PIK3CA while Type 2 tumors are more sensitive and have mutations in TP53. Overactivation of the signaling pathway (PI3K) results in anti-apoptosis. Here, this study aims to identify Tumor-Specific Antigen for germline mutations in endometrial cancer which can be used as a potential vaccine candidate. The germline mutations data are obtained from cancer gene census of the cosmic database. Genes mutating with crucial role in endometrial cancer are considered. Peptides libraries are generated using peptide design library. Human leukocyte antigen alleles are identified for the peptide library through NetMHC. Binding affinities of alleles with peptide are determined. Linear regression is performed to generate graphs. PTEN, TP53, PIK3CA, KRAS, and CTNNB1 proved to have critical role. About 575 overlapping peptide libraries are generated and each peptide has a length of 18-20 amino acids. Approximately 58 HLAs are identified, having strong interactions with HLAs. Regression analysis shows that the no. of mutations are directly associated with a binding affinity of peptides. From this, we suggest that the identified TSA can be used as personalized peptide vaccines that directly target the mutated genes in endometrial cancer. This research work can be used in the laboratories for further validation.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"15 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2019-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72953442","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 : 2019-10-01DOI: 10.13189/APP.2019.070402
M. Hamza, Azhar Mahmood, Sajid Khan, Muhammad Rizwan, Anum Munir
The p53 is also known as a tumor suppressor gene, involved in a variety of cellular processes and signaling pathways. p53 mutations are involved in almost all kinds of cancers, and several treatments are available for p53 mutations but have a number of limitations. Still, there is a need for better drugs. Computational methods are emerging and beneficial tools to guide and interpret experiments to fasten the drug design process. This study was undertaken to design a drug that targets p53 Ser121 and Val122 mutations. The compound was identified through virtual screening and several drug-like filters were applied. The identified compound is considered to be non-toxic in nature. ADMET properties and pharmacokinetics of the compound also describe the effectiveness of the compound. The results of this study, suggest that this compound can be used to treat p53 mutations and the compound is synthesized successfully in the lab to determine its adequacy and efficacy. Bis-(4-chlorophenyl)methyl-BLAH compound can be used as a strong inhibitor of p53 Ser 121 and Val 122 mutations.
p53也被称为肿瘤抑制基因，参与多种细胞过程和信号通路。几乎所有类型的癌症都与P53突变有关，目前有几种针对P53突变的治疗方法，但都有一些局限性。尽管如此，我们仍然需要更好的药物。计算方法是新兴的和有益的工具来指导和解释实验，以加快药物设计过程。本研究旨在设计一种靶向p53 Ser121和Val122突变的药物。该化合物通过虚拟筛选和几种类似药物的过滤器被识别出来。所鉴定的化合物被认为是无毒的。ADMET性质和药代动力学也描述了该化合物的有效性。本研究结果表明，该化合物可用于治疗p53突变，并在实验室中成功合成，以确定其充分性和有效性。双-(4-氯苯基)甲基- blah化合物可作为p53 Ser 121和Val 122突变的强抑制剂。
{"title":"Design and Synthesis of Novel Inhibitor against Ser121 and Val122 Mutations in P53 Cancer Gene","authors":"M. Hamza, Azhar Mahmood, Sajid Khan, Muhammad Rizwan, Anum Munir","doi":"10.13189/APP.2019.070402","DOIUrl":"https://doi.org/10.13189/APP.2019.070402","url":null,"abstract":"The p53 is also known as a tumor suppressor gene, involved in a variety of cellular processes and signaling pathways. p53 mutations are involved in almost all kinds of cancers, and several treatments are available for p53 mutations but have a number of limitations. Still, there is a need for better drugs. Computational methods are emerging and beneficial tools to guide and interpret experiments to fasten the drug design process. This study was undertaken to design a drug that targets p53 Ser121 and Val122 mutations. The compound was identified through virtual screening and several drug-like filters were applied. The identified compound is considered to be non-toxic in nature. ADMET properties and pharmacokinetics of the compound also describe the effectiveness of the compound. The results of this study, suggest that this compound can be used to treat p53 mutations and the compound is synthesized successfully in the lab to determine its adequacy and efficacy. Bis-(4-chlorophenyl)methyl-BLAH compound can be used as a strong inhibitor of p53 Ser 121 and Val 122 mutations.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"107 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2019-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76255454","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 : 2019-10-01DOI: 10.13189/APP.2019.070403
Z. Turk, M. Hamza, Anum Munir, Sajid Khan, Muhammad Rizwan, A. Mehmood
Lung Cancer is a type of serious cancer that causes 1.37 million deaths every year all over the world and accounts for almost 18% of all cancer death. PI3Ks establish a lipid kinase family that is important to integrate disparate dimensions of cell functions including cell survival, vesicular trafficking, proliferation, and cell migration. This is an essential pathway in the oncogenesis and advancement of lung cancer. In preclinical studies, PIK3 inhibitors deliver exploratory antitumor activity. The study was established to realize perception and molecular mechanisms that are crucial for potent inhibitors of PIK3CA. In this research work, mutated proteins of PIK3CA were selected, models of pharmacophore were designed and hit compounds were obtained against reference feature pharmacophore by virtual screening. These hit compounds were then docked with the mutated proteins of PIK3CA. Three important features were shown by Pharmacophores, Hydrogen bond donor (HBD), Hydrogen bond acceptors (HBA) and aromatic rings (AR). Through virtual screening, 8 hit compounds were obtained before docking Lipinski rule of five was applied and the compounds that achieved all properties were docked with mutated proteins of PIK3CA. 3 compounds fulfilled all properties and demonstrated the stability of ligands. It is suggested that these compounds can be used for curing PIK3CA involved in lung cancer and on the basis of shared feature novel compounds can be designed against a mutation in PIK3CA involved in lung cancer.
{"title":"Treatment against Mutation of PIK3CA Gene Involved in Lung Cancer by Structure Base Pharmacophore Modeling, Virtual Screening and Molecular Docking","authors":"Z. Turk, M. Hamza, Anum Munir, Sajid Khan, Muhammad Rizwan, A. Mehmood","doi":"10.13189/APP.2019.070403","DOIUrl":"https://doi.org/10.13189/APP.2019.070403","url":null,"abstract":"Lung Cancer is a type of serious cancer that causes 1.37 million deaths every year all over the world and accounts for almost 18% of all cancer death. PI3Ks establish a lipid kinase family that is important to integrate disparate dimensions of cell functions including cell survival, vesicular trafficking, proliferation, and cell migration. This is an essential pathway in the oncogenesis and advancement of lung cancer. In preclinical studies, PIK3 inhibitors deliver exploratory antitumor activity. The study was established to realize perception and molecular mechanisms that are crucial for potent inhibitors of PIK3CA. In this research work, mutated proteins of PIK3CA were selected, models of pharmacophore were designed and hit compounds were obtained against reference feature pharmacophore by virtual screening. These hit compounds were then docked with the mutated proteins of PIK3CA. Three important features were shown by Pharmacophores, Hydrogen bond donor (HBD), Hydrogen bond acceptors (HBA) and aromatic rings (AR). Through virtual screening, 8 hit compounds were obtained before docking Lipinski rule of five was applied and the compounds that achieved all properties were docked with mutated proteins of PIK3CA. 3 compounds fulfilled all properties and demonstrated the stability of ligands. It is suggested that these compounds can be used for curing PIK3CA involved in lung cancer and on the basis of shared feature novel compounds can be designed against a mutation in PIK3CA involved in lung cancer.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"14 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2019-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74574361","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 : 2019-07-01DOI: 10.13189/APP.2019.070301
M. Billah, M. A. Rayhan, S. Yousuf, Kashfia Nawrin, JohirRayhan, Elmabruk M. Khengari
Open Field, Hole Cross and EPM are three widely acceptable experimental methods used to evaluate sedative-anxiolytic potential. The theories behind introducing these fields were to challenge the rodents to a novel environment. However, the behavioral changes caused by these environments often get influenced by rodent's identical neurologic conditions. The major challenges faced by the researchers are variations due to first administration against repeated administration, utilizing same rodent for another experiment but in different time or using different rodent for different experiments. Keeping the drawbacks in consideration, the present study undertook a newly modified (OF-HC-EPM) approach to integrate the experimental fields so as to utilize the same rodents with single oral administration for exposure to different fields which had allowed nullifying the risk of individual and time dependent variance. Anxiolytics, atypical antidepressants, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants as well as the combined anxiolytics and antidepressants were administered to Swiss Albino Mice and their respective behavioral changes were observed. The new approach proved to be an essential tool for evaluating neuropharmacological potentials.
Open Field, Hole Cross和EPM是三种被广泛接受的用于评估镇静-焦虑电位的实验方法。引入这些磁场的理论是为了让啮齿动物适应一个新的环境。然而，由这些环境引起的行为变化往往受到啮齿动物相同的神经系统状况的影响。研究人员面临的主要挑战是由于第一次给药和重复给药造成的差异，在不同的时间使用同一只啮齿动物进行另一项实验，或使用不同的啮齿动物进行不同的实验。考虑到这些缺点，本研究采用了一种新改进的(of - hc - epm)方法来整合实验场，从而使同一啮齿动物在一次口服给药的情况下暴露于不同的场，从而可以消除个体和时间相关方差的风险。分别给予抗焦虑药、非典型抗抑郁药、选择性5 -羟色胺再摄取抑制剂、5 -羟色胺-去甲肾上腺素再摄取抑制剂、三环抗抑郁药以及抗焦虑药和抗抑郁药联合用药，观察其行为变化。新方法被证明是评估神经药理学潜力的重要工具。
{"title":"A Novel Integrated (OF-HC-EPM) Approach to Study Anxiety Related Depressive Behavior in Mice Model: A Comparison of Neuro Standards","authors":"M. Billah, M. A. Rayhan, S. Yousuf, Kashfia Nawrin, JohirRayhan, Elmabruk M. Khengari","doi":"10.13189/APP.2019.070301","DOIUrl":"https://doi.org/10.13189/APP.2019.070301","url":null,"abstract":"Open Field, Hole Cross and EPM are three widely acceptable experimental methods used to evaluate sedative-anxiolytic potential. The theories behind introducing these fields were to challenge the rodents to a novel environment. However, the behavioral changes caused by these environments often get influenced by rodent's identical neurologic conditions. The major challenges faced by the researchers are variations due to first administration against repeated administration, utilizing same rodent for another experiment but in different time or using different rodent for different experiments. Keeping the drawbacks in consideration, the present study undertook a newly modified (OF-HC-EPM) approach to integrate the experimental fields so as to utilize the same rodents with single oral administration for exposure to different fields which had allowed nullifying the risk of individual and time dependent variance. Anxiolytics, atypical antidepressants, selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants as well as the combined anxiolytics and antidepressants were administered to Swiss Albino Mice and their respective behavioral changes were observed. The new approach proved to be an essential tool for evaluating neuropharmacological potentials.","PeriodicalId":7378,"journal":{"name":"Advances in Pharmacology and Pharmacy","volume":"41 1","pages":""},"PeriodicalIF":0.1,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80773299","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：