Pub Date : 2023-09-19DOI: 10.9734/jpri/2023/v35i257429
Baraa Issam Abdulrahman
Introduction: Precancerous lesions, conditions, and early-stage oral cancer cannot be sufficiently identified solely through visual inspection and may be prone to be inadvertently disregarded. Distinguishing between early-stage cancer, precancerous lesions, and benign tumors can pose a challenge due to the striking resemblance in their visual characteristics. Using surgical biopsy as a diagnostic modality is widely regarded as the gold standard in the medical community. However, it is essential to acknowledge that acquiring professional services for this procedure can prove impractical in certain circumstances. Hence this paper presents a concise review of a wide range of advanced diagnostic aids employed in detection of Oral Premalignant Lesions (OPL).
Methods: The literature search utilized appropriate keywords to search online databases like PubMed, Medline, Google Scholar, EBSCO, Wiley science library, and Saudi digital library.
Results: Alternative screening methods that are noninvasive, readily executed, and exhibit a high degree of accuracy are the established criteria for considering a test as a viable substitute for histopathology. Early diagnosis is a paramount factor in the effective management of oral cancer. Vital staining, immunocytochemistry, fluorescence imaging, laser confocal microscopy, Raman spectroscopy, and Fourier transform infrared spectroscopy diagnostic modalities are employed for the timely identification of oral premalignant lesions.
Conclusion: Recent advances have improved the diagnostic aids in easy and accurate detection of oral premalignant lesions thereby facilitating effective management and mitigation strategies at an early stage of the lesion.
简介:癌前病变、状况和早期口腔癌不能仅仅通过目测充分识别,而且可能容易被忽视。区分早期癌症、癌前病变和良性肿瘤是一项挑战,因为它们的视觉特征非常相似。使用手术活检作为诊断方式被广泛认为是医学界的金标准。然而,重要的是要承认,在某些情况下,为这一程序获得专业服务可能是不切实际的。因此,本文简要介绍了用于检测口腔癌前病变(OPL)的各种先进诊断辅助工具。方法:利用合适的关键词检索PubMed、Medline、谷歌Scholar、EBSCO、Wiley science library、Saudi digital library等在线数据库。
结果:非侵入性的、易于执行的、表现出高度准确性的替代筛查方法是考虑将测试作为组织病理学可行替代品的既定标准。早期诊断是口腔癌有效治疗的重要因素。采用生命染色、免疫细胞化学、荧光成像、激光共聚焦显微镜、拉曼光谱、傅立叶变换红外光谱等诊断手段及时识别口腔癌前病变。
结论:近年来的研究进展提高了口腔癌前病变的诊断辅助手段,方便、准确地发现口腔癌前病变,从而促进了早期病变的有效管理和缓解策略。
{"title":"Advancement in Diagnostic Aids for Oral Premalignant Lesions","authors":"Baraa Issam Abdulrahman","doi":"10.9734/jpri/2023/v35i257429","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i257429","url":null,"abstract":"Introduction: Precancerous lesions, conditions, and early-stage oral cancer cannot be sufficiently identified solely through visual inspection and may be prone to be inadvertently disregarded. Distinguishing between early-stage cancer, precancerous lesions, and benign tumors can pose a challenge due to the striking resemblance in their visual characteristics. Using surgical biopsy as a diagnostic modality is widely regarded as the gold standard in the medical community. However, it is essential to acknowledge that acquiring professional services for this procedure can prove impractical in certain circumstances. Hence this paper presents a concise review of a wide range of advanced diagnostic aids employed in detection of Oral Premalignant Lesions (OPL).
 Methods: The literature search utilized appropriate keywords to search online databases like PubMed, Medline, Google Scholar, EBSCO, Wiley science library, and Saudi digital library.
 Results: Alternative screening methods that are noninvasive, readily executed, and exhibit a high degree of accuracy are the established criteria for considering a test as a viable substitute for histopathology. Early diagnosis is a paramount factor in the effective management of oral cancer. Vital staining, immunocytochemistry, fluorescence imaging, laser confocal microscopy, Raman spectroscopy, and Fourier transform infrared spectroscopy diagnostic modalities are employed for the timely identification of oral premalignant lesions.
 Conclusion: Recent advances have improved the diagnostic aids in easy and accurate detection of oral premalignant lesions thereby facilitating effective management and mitigation strategies at an early stage of the lesion.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"198 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135014206","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 : 2023-09-18DOI: 10.9734/jpri/2023/v35i257428
Samuel C. Iwuji, Kosisochukwu A. Uzokwe, Francis O. Nwokorie, Wilson C. Okafor, Sixtus A. Okafor
Aims: This study investigated the anti-anaemic and anti- leukopenic effects of hydromethanolic (1:4) extracts of Cyperus esculentus (Tiger nut) and Zingiber officinale (Ginger) on the alloxan- induced diabetic albino rats.
Place: The in vivo study took place in the Department of Biochemistry, Micheal Okpara University of Agriculture Umudike, Abia state.
Methods: Fresh Cyperus esculentus and Zingiber officinale was air dried at room temperature, grounded into fine powder and extracted with hydromethanol in ratio of 20:80 using Soxhlet extraction method. The albino rats (total number of 36) were randomly divided into 6 groups of 6 rats each: Group 1 (Normal control); Group 2 (Diabetic); Group 3 (Glibenclamide); Group 4 (500mg/dl Cyperus esculentus); Group 5 (500mg/dl Zingiber officinale) and Group 6 (250mg/dl Cyperus esculentus + 250 mg/dl Zingiber officinale, 50:50) were administered orally. Group 2 to 6 were administered with 160mg/kg alloxan monohydrate intraperitoneally to induce a diabetic state. The haematological parameters determined were PCV, HB, RBC, TWBC, MCV, MCH and MCHC.
Results: The diabetic group treated with the Glibenclamide and 500 mg/kg Zingiber officinale extract had significant recovery (compared with the normal control) from the diabetic- induced depletion of Hb, PCV and RBC than the diabetic group treated with 250 mg/kg Cyperus esculentus + 250 mg/kg Zingiber officinale extracts. 500 mg/kg Cyperus esculentus extract showed the least recovery from diabetic induced anaemia.
Conclusion: Ginger extract showed value in the recovery from anaemia and leucopenia associated with diabetes having significantly improved the values of RBC, PCV, haemoglobin and TWBC in the diabetic rats more than the effects of Tigernut and combined (ginger and tigernut) extracts. Ginger extract treatment might also increase the defense mechanism of the body against infections in diabetes.
{"title":"Anti-anaemic and Anti-leukopenic Effects of Hydromethanolic Extracts of Tiger Nut and Ginger on Alloxan- induced Diabetic Rats","authors":"Samuel C. Iwuji, Kosisochukwu A. Uzokwe, Francis O. Nwokorie, Wilson C. Okafor, Sixtus A. Okafor","doi":"10.9734/jpri/2023/v35i257428","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i257428","url":null,"abstract":"Aims: This study investigated the anti-anaemic and anti- leukopenic effects of hydromethanolic (1:4) extracts of Cyperus esculentus (Tiger nut) and Zingiber officinale (Ginger) on the alloxan- induced diabetic albino rats.
 Place: The in vivo study took place in the Department of Biochemistry, Micheal Okpara University of Agriculture Umudike, Abia state.
 Methods: Fresh Cyperus esculentus and Zingiber officinale was air dried at room temperature, grounded into fine powder and extracted with hydromethanol in ratio of 20:80 using Soxhlet extraction method. The albino rats (total number of 36) were randomly divided into 6 groups of 6 rats each: Group 1 (Normal control); Group 2 (Diabetic); Group 3 (Glibenclamide); Group 4 (500mg/dl Cyperus esculentus); Group 5 (500mg/dl Zingiber officinale) and Group 6 (250mg/dl Cyperus esculentus + 250 mg/dl Zingiber officinale, 50:50) were administered orally. Group 2 to 6 were administered with 160mg/kg alloxan monohydrate intraperitoneally to induce a diabetic state. The haematological parameters determined were PCV, HB, RBC, TWBC, MCV, MCH and MCHC.
 Results: The diabetic group treated with the Glibenclamide and 500 mg/kg Zingiber officinale extract had significant recovery (compared with the normal control) from the diabetic- induced depletion of Hb, PCV and RBC than the diabetic group treated with 250 mg/kg Cyperus esculentus + 250 mg/kg Zingiber officinale extracts. 500 mg/kg Cyperus esculentus extract showed the least recovery from diabetic induced anaemia.
 Conclusion: Ginger extract showed value in the recovery from anaemia and leucopenia associated with diabetes having significantly improved the values of RBC, PCV, haemoglobin and TWBC in the diabetic rats more than the effects of Tigernut and combined (ginger and tigernut) extracts. Ginger extract treatment might also increase the defense mechanism of the body against infections in diabetes.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"30 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135153718","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 : 2023-09-14DOI: 10.9734/jpri/2023/v35i247426
Ibrahim M. S. Shnawa
The macrophage, natural killer cells, B and T cells are the outstanding formed elements of human immune system. In normal immune homeostatic state these cells in a way or other recognize the host body components as self via the immune surveillance mechanisms. Though when there was a shift in immune homeostasis due to chronic induction by; i - environmental stimulus, ii –interplay of predisposing genetic elements, iii-family history, iv – bystander pathologic inflammatory system .Immune cells becomes prone to recognize the impart self or self as a non-self with subsequent induction of autoimmune diseases. The present opinion paper was aimed at vaccine and adjuvant mediated autoimmune diseases. Timelines for vaccine and adjuvant induced autoimmunity were made. Different human approved vaccines induce different autoimmune disease, more than on vaccine may induce same autoimmune disease. Shoenfeld Syndrome, the adjuvant induce autoimmune/ inflammatory syndrome. Under the umbrella of this syndrome five conditions grouped as; i – Postvaccination with an adjuvanated vaccine, ii – macrophagic myofasciitis, iii – sick building disease condition iv – Gulf war disease condition and v – siliconosis. Protocol for the practical evaluation of these diseases was suggested. Understanding Shoenfeld Syndrome is crucial for producing vaccines with a safer side effect profile.
{"title":"Vaccine and Adjuvant Mediated Autoimmunity","authors":"Ibrahim M. S. Shnawa","doi":"10.9734/jpri/2023/v35i247426","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i247426","url":null,"abstract":"The macrophage, natural killer cells, B and T cells are the outstanding formed elements of human immune system. In normal immune homeostatic state these cells in a way or other recognize the host body components as self via the immune surveillance mechanisms. Though when there was a shift in immune homeostasis due to chronic induction by; i - environmental stimulus, ii –interplay of predisposing genetic elements, iii-family history, iv – bystander pathologic inflammatory system .Immune cells becomes prone to recognize the impart self or self as a non-self with subsequent induction of autoimmune diseases. The present opinion paper was aimed at vaccine and adjuvant mediated autoimmune diseases. Timelines for vaccine and adjuvant induced autoimmunity were made. Different human approved vaccines induce different autoimmune disease, more than on vaccine may induce same autoimmune disease. Shoenfeld Syndrome, the adjuvant induce autoimmune/ inflammatory syndrome. Under the umbrella of this syndrome five conditions grouped as; i – Postvaccination with an adjuvanated vaccine, ii – macrophagic myofasciitis, iii – sick building disease condition iv – Gulf war disease condition and v – siliconosis. Protocol for the practical evaluation of these diseases was suggested. Understanding Shoenfeld Syndrome is crucial for producing vaccines with a safer side effect profile.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"145 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134913492","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 : 2023-09-14DOI: 10.9734/jpri/2023/v35i247427
Mohannad A. Alsalmi, Hisham N. Altayb
Objectives: Antibiotic resistance is a major public health problem worldwide. There is little data on the incidence, sources, and importance of antibiotic-resistant bacteria on the Red Sea coast of Jeddah. This study aims to identify drug-resistant microbes found on the Red Sea coast in Jeddah and to screen their resistance profile against different antibiotics.
Methodology: Forty-eight samples were obtained from different locations on the Red Sea coast in Jeddah. Antimicrobial susceptibility tests were performed against the following antibiotic discs (Oxoid): cefotaxime (CTX) (30g); meropenem (MEM) (10g); gentamicin (CN) (10g) and chloramphenicol (C) (30g).
Results: The isolates showed resistance to Gentamicin 10 mcg (39.47%; 15/38), Cefotaxime 30 mcg (18.42%; 7/38), Meropenem 10 mcg (0%; 0/38) and Chloramphenicol 30 mcg (5.26%; 2/38).
Conclusion: From this study there is a high resistance rate to cefotaxime, chloramphenicol and gentamicin 39%. This research has substantiated the existence of a substantial prevalence of resistance to various microbial agents within our environment, specifically within the Red Sea in Jeddah. We propose conducting future studies across diverse geographic regions, utilizing extensive sample sizes, to gain a deeper insight into the potential impact of environmental factors and pollution on the propagation of drug-resistant bacteria. Additionally, the identification of these bacterial strains is essential for understanding their characteristics and devising strategies to combat them effectively, thereby assisting in curtailing their proliferation.
目的:抗生素耐药性是世界范围内的一个主要公共卫生问题。关于吉达红海沿岸耐抗生素细菌的发生率、来源和重要性的数据很少。本研究旨在鉴定吉达红海沿岸发现的耐药微生物,并筛选它们对不同抗生素的耐药谱。方法:从吉达红海沿岸不同地点采集48份样本。对以下抗生素片(Oxoid)进行抗菌药敏试验:头孢噻肟(CTX) (30g);美罗培南(MEM) 10g;庆大霉素(CN) (10g)和氯霉素(C) (30g);
结果:分离株对庆大霉素10 mcg的耐药率为39.47%;15/38),头孢噻肟30 mcg (18.42%;7/38),美罗培南10微克(0%;0/38)和氯霉素30 mcg (5.26%;2/38)强生# x0D;结论:本研究对头孢噻肟、氯霉素和庆大霉素的耐药率较高,为39%。这项研究证实,在我们的环境中,特别是在吉达的红海地区,对各种微生物制剂的耐药性普遍存在。我们建议未来在不同的地理区域开展研究,利用广泛的样本量,以更深入地了解环境因素和污染对耐药细菌传播的潜在影响。此外,鉴定这些菌株对于了解它们的特性和制定有效对抗它们的策略至关重要,从而有助于减少它们的增殖。
{"title":"Screening of Antimicrobial Resistance in Bacterial Isolates from Red Sea Coast in Jeddah, Saudi Arabia","authors":"Mohannad A. Alsalmi, Hisham N. Altayb","doi":"10.9734/jpri/2023/v35i247427","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i247427","url":null,"abstract":"Objectives: Antibiotic resistance is a major public health problem worldwide. There is little data on the incidence, sources, and importance of antibiotic-resistant bacteria on the Red Sea coast of Jeddah. This study aims to identify drug-resistant microbes found on the Red Sea coast in Jeddah and to screen their resistance profile against different antibiotics.
 Methodology: Forty-eight samples were obtained from different locations on the Red Sea coast in Jeddah. Antimicrobial susceptibility tests were performed against the following antibiotic discs (Oxoid): cefotaxime (CTX) (30g); meropenem (MEM) (10g); gentamicin (CN) (10g) and chloramphenicol (C) (30g).
 Results: The isolates showed resistance to Gentamicin 10 mcg (39.47%; 15/38), Cefotaxime 30 mcg (18.42%; 7/38), Meropenem 10 mcg (0%; 0/38) and Chloramphenicol 30 mcg (5.26%; 2/38).
 Conclusion: From this study there is a high resistance rate to cefotaxime, chloramphenicol and gentamicin 39%. This research has substantiated the existence of a substantial prevalence of resistance to various microbial agents within our environment, specifically within the Red Sea in Jeddah. We propose conducting future studies across diverse geographic regions, utilizing extensive sample sizes, to gain a deeper insight into the potential impact of environmental factors and pollution on the propagation of drug-resistant bacteria. Additionally, the identification of these bacterial strains is essential for understanding their characteristics and devising strategies to combat them effectively, thereby assisting in curtailing their proliferation.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"30 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134913189","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 : 2023-09-12DOI: 10.9734/jpri/2023/v35i247425
Adonu Cyril, Onwusoba Restus, Onyi Patrick, Ali Ibeabuchi, Omeh Romanus
Background: Essential oil (EO) of Cymbopogon citratus has been demonstrated to have antibacterial activities against both Gram negative and Gram positive bacteria. The study was, therefore, conducted to evaluate the effects of combined use of C. citratus and ciprofloxacin against fluoroquinolone-resistant Staphylococcus aureus (FQRSA) and Escherichia coli (FQREC).
Methods: The antibacterial activity of the essential oil was evaluated by agar dilution method while the combination studies were done using Checker-board agar dilution technique.
Results: The mean MIC values of EO against the FQRSA and FQREC were 0.043 + 0.01 mg/ml and 0.049 mg/ml respectively. When ciprofloxacin was combined with EO of lemongrass, 53.9, 28.3, 17.8 and 0.0 % of the FQRSA isolates showed indifference, additive, synergistic and antagonistic effects respectively. Similarly, when ciprofloxacin was combined with EO of lemongrass at different ratios, 44, 35.5, 20.6 and 0.0 % of the FQREC isolates showed combined effects of additivity, synergism, indifference and antagonism respectively.
Conclusions: The results revealed the invitro antibacterial potency of Cymbopogon citratus oil against fluoroquinolone resistant S. aureus and E. coli. More importantly, the study has proved that the combined use of ciprofloxacin and essential oil of lemongrass has increased the sensitivity of both FQRSA and FQREC bacteria.
{"title":"Potentiation of Antibacterial Activity of Ciprofloxacin by Essential Oil of Cymbopogon citratus against Fluoroquinolone-resistant Staphylococcus aureus and Escherichia coli","authors":"Adonu Cyril, Onwusoba Restus, Onyi Patrick, Ali Ibeabuchi, Omeh Romanus","doi":"10.9734/jpri/2023/v35i247425","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i247425","url":null,"abstract":"Background: Essential oil (EO) of Cymbopogon citratus has been demonstrated to have antibacterial activities against both Gram negative and Gram positive bacteria. The study was, therefore, conducted to evaluate the effects of combined use of C. citratus and ciprofloxacin against fluoroquinolone-resistant Staphylococcus aureus (FQRSA) and Escherichia coli (FQREC).
 Methods: The antibacterial activity of the essential oil was evaluated by agar dilution method while the combination studies were done using Checker-board agar dilution technique.
 Results: The mean MIC values of EO against the FQRSA and FQREC were 0.043 + 0.01 mg/ml and 0.049 mg/ml respectively. When ciprofloxacin was combined with EO of lemongrass, 53.9, 28.3, 17.8 and 0.0 % of the FQRSA isolates showed indifference, additive, synergistic and antagonistic effects respectively. Similarly, when ciprofloxacin was combined with EO of lemongrass at different ratios, 44, 35.5, 20.6 and 0.0 % of the FQREC isolates showed combined effects of additivity, synergism, indifference and antagonism respectively.
 Conclusions: The results revealed the invitro antibacterial potency of Cymbopogon citratus oil against fluoroquinolone resistant S. aureus and E. coli. More importantly, the study has proved that the combined use of ciprofloxacin and essential oil of lemongrass has increased the sensitivity of both FQRSA and FQREC bacteria.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"32 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135827313","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 : 2023-09-11DOI: 10.9734/jpri/2023/v35i247424
Eric Ziki, Ludovic Akonan, Koffi Charles Kouman, Brice Dali, Eugene Megnassan, Rita Kakou-Yao, Abodou Jules Tenon, Vladimir Frecer, Stanislav Miertus
Background: We have carried out virtual design of coumarinyl-substituted sulfonamides (CSAM) analogs as inhibitors of human carbonic anhydrase II (hCA II) endowed with favorable predicted pharmacokinetic profiles and potential therapeutic effects against glaucoma.
Methods: modifying in situ the x-ray structure of 2-(7-methoxy-2-oxo-2H-chromen-4-yl)-N-(4-sulfamoyl-phenyl)-acetamide (CSAM0)-hCA II complex (PDB entry 3ML2), permitted 3D models of hCA II-CSAMx complexes preparation for a TS of 14 CSAMs the experimental activities of which are available in the literature (IC50exp). Active bound conformation of the CSAM1-14 assessment led to linear correlation between computed enthalpy of hCA II-CSAMx complexes formation in gas phase (ΔΔHMM) with the IC50exp. Moreover, considering the solvation and ligand loss of entropy upon binding led to a superior QSAR model where a better linear correlation is established between calculated GFE (ΔΔGcom) and IC50exp. The successive 3D-pharmacophore (PH4) built from CSAMs active conformations helped to virtually screen CSAM populating a sulfonamides scaffolds virtual combinatorial library (VCL), focused by Lipinski’s rule-of-five to reach novel CSAMs.
Results: Enthalpy QSAR model: pIC50exp = -0.068×ΔΔHMM + 7.722, R2 = 0.82; GFE QSAR model: pIC50exp = - 0.061× ΔΔGcom + 7.647, R2 = 0.92 and PH4 model: pIC50exp = 1.095×pIC50pre – 0.680, R2 = 0.87. The VCL of more than 1,500,625 CSAMs was lowered to 865,670 drug likely compounds by the Lipinski’s rule (except the restriction Mw ≤ 500 g/mol). The three-point PH4-based screening identified 81 novel CSAMs with predicted IC50pre reaching 78-times better than CSAM1 potency (IC50exp = 23 nM). Computed pharmacokinetic profile of the new candidates showed enhanced cell membrane permeability and high human oral absorption compared to current anti-glaucoma agents.
Conclusions: Combination of QSAR models of the CSAMs’ affinity to the hCA II, pharmacophore model, and ADME profile guided to the sulfonamides inhibitors identification and helped to in silico screen VCL sulfonamides scaffold bearing analogs and allowed emerging of novel more potent compounds with predicted IC50 and favorable pharmacokinetic profiles.
{"title":"Virtual Design of Novel Coumarinyl-Substituted Sulfonamide Inhibitors of Carbonic Anhydrase II as Potential Drugs against Glaucoma","authors":"Eric Ziki, Ludovic Akonan, Koffi Charles Kouman, Brice Dali, Eugene Megnassan, Rita Kakou-Yao, Abodou Jules Tenon, Vladimir Frecer, Stanislav Miertus","doi":"10.9734/jpri/2023/v35i247424","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i247424","url":null,"abstract":"Background: We have carried out virtual design of coumarinyl-substituted sulfonamides (CSAM) analogs as inhibitors of human carbonic anhydrase II (hCA II) endowed with favorable predicted pharmacokinetic profiles and potential therapeutic effects against glaucoma.
 Methods: modifying in situ the x-ray structure of 2-(7-methoxy-2-oxo-2H-chromen-4-yl)-N-(4-sulfamoyl-phenyl)-acetamide (CSAM0)-hCA II complex (PDB entry 3ML2), permitted 3D models of hCA II-CSAMx complexes preparation for a TS of 14 CSAMs the experimental activities of which are available in the literature (IC50exp). Active bound conformation of the CSAM1-14 assessment led to linear correlation between computed enthalpy of hCA II-CSAMx complexes formation in gas phase (ΔΔHMM) with the IC50exp. Moreover, considering the solvation and ligand loss of entropy upon binding led to a superior QSAR model where a better linear correlation is established between calculated GFE (ΔΔGcom) and IC50exp. The successive 3D-pharmacophore (PH4) built from CSAMs active conformations helped to virtually screen CSAM populating a sulfonamides scaffolds virtual combinatorial library (VCL), focused by Lipinski’s rule-of-five to reach novel CSAMs.
 Results: Enthalpy QSAR model: pIC50exp = -0.068×ΔΔHMM + 7.722, R2 = 0.82; GFE QSAR model: pIC50exp = - 0.061× ΔΔGcom + 7.647, R2 = 0.92 and PH4 model: pIC50exp = 1.095×pIC50pre – 0.680, R2 = 0.87. The VCL of more than 1,500,625 CSAMs was lowered to 865,670 drug likely compounds by the Lipinski’s rule (except the restriction Mw ≤ 500 g/mol). The three-point PH4-based screening identified 81 novel CSAMs with predicted IC50pre reaching 78-times better than CSAM1 potency (IC50exp = 23 nM). Computed pharmacokinetic profile of the new candidates showed enhanced cell membrane permeability and high human oral absorption compared to current anti-glaucoma agents.
 Conclusions: Combination of QSAR models of the CSAMs’ affinity to the hCA II, pharmacophore model, and ADME profile guided to the sulfonamides inhibitors identification and helped to in silico screen VCL sulfonamides scaffold bearing analogs and allowed emerging of novel more potent compounds with predicted IC50 and favorable pharmacokinetic profiles.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"18 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135981953","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 : 2023-09-08DOI: 10.9734/jpri/2023/v35i247423
S. R, A. N
Introduction: For stepping towards a healthy living, parameters like good food, sound sleep and right mind, all plays major role to attain health and eternity, which were spelled by Siddhars since ancient times. Additionally, Sleep is the best, fruitful meditation for a quality of life. But, getting quality sleep with sufficient period is a matter of concern in the modern civilized world, irrespective of ages, which leads to serious consequences. When you're constantly losing sleep because of insomnia, your brain doesn't cooperate your body, thereby disturbing to perform important tasks. Hence, Insomnia is a significant health problem because of its high prevalence and management challenges. The aim of the study was to evaluate the effectiveness of Siddha medicine Kasa Kasa Kudineer (KKK), in treating insomnia patients, attending OPD at AAGHIM, Chennai. Study Design: This was a Pilot study with a sample size of 20, with the intervention of Siddha Medicine Kasa Kasa Kudineer, and the outcome was assessed by the Insomnia Severity Index Score. Place of Study: The study was conducted at Arignar Anna Government Hospital of Indian Medicine and Homeopathy, attached with Government Siddha Medical College (AAGHIM attached with GSMC), Chennai- 106. Materials and Methods: The study was conducted at the Arignar Anna Govt. Hospital of Indian Medicine (AAGHIM), attached with Govt. Siddha Medical College, Chennai 106, with a sample size of 20. The study protocol and informed consent were reviewed and approved by IEC (with a waiver from IEC). Patients attending the OPD of AAGHIM with complaints of sleep disturbances were chosen for enrollment based on their insomnia severity index score of more than 15. Siddha Medicine Kasa Kasa Kudineer were adminstrated and the observations were made before and after the treatment using the score. Results: Results were analyzed. Descriptive statistics, Paired t- test were analyzed using SPSS trial version 25, and out of 20 patients, 17 patients shown significant improvement in their sleep pattern and the total score were also moved to no clinically significant category of Insomnia severity index score. All parameters whose p value is less than 0.05 reject the null hypothesis. Results were encouraging, as it shown considerable improvement by the end of the study. Conclusion: This study reveals the significant effectiveness of treating Clinically significant insomnia patients, attending OPD at AAGHIM, Chennai with Kasa Kasa Kudineer (KKK), which may ignite a new Siddha medicine for a better quality of life.
引言:对于健康的生活,良好的食物、良好的睡眠和正确的心态等参数都对实现健康和永恒起着重要作用,这是悉达尔自古以来所拼写的。此外,睡眠是提高生活质量的最佳、富有成效的冥想。但是,在现代文明世界,无论年龄大小,获得充足时间的优质睡眠都是一个令人担忧的问题,这会导致严重的后果。当你因为失眠而不断失眠时,你的大脑与你的身体不协调,从而干扰你执行重要任务。因此,失眠是一个重要的健康问题,因为它的高发病率和管理挑战。本研究的目的是评估Siddha medicine Kasa Kasa Kudineer(KKK)在金奈AAGHIM门诊治疗失眠患者的有效性。研究设计:这是一项试点研究,样本量为20,由Siddha Medicine Kasa Kasa Kudineer干预,结果通过失眠严重程度指数评分进行评估。研究地点:该研究在Arignar Anna政府印度医学与顺势疗法医院进行,附属政府悉达医学院(AAGHIM附属GSMC),钦奈-106。材料和方法:该研究在Arignar Anna Govt.印度医学院(AAGHIM)进行,附属于钦奈106 Siddha医学院,样本量为20。IEC审查并批准了研究方案和知情同意书(IEC豁免)。根据失眠严重程度指数得分超过15分,选择患有睡眠障碍的AAGHIM门诊患者进行登记。服用Siddha Medicine Kasa Kasa Kudineer,并在治疗前后使用评分进行观察。结果:对结果进行分析。描述性统计,配对t检验使用SPSS试验版本25进行分析,在20名患者中,17名患者的睡眠模式有显著改善,总分也转移到失眠严重程度指数得分的无临床意义类别。p值小于0.05的所有参数都拒绝零假设。结果令人鼓舞,因为研究结束时情况有了相当大的改善。结论:本研究揭示了用Kasa Kasa Kudineer(KKK)在金奈AAGHIM参加门诊治疗临床显著失眠患者的显著有效性,这可能会点燃一种新的Siddha药物,提高生活质量。
{"title":"Effectiveness of Kasa Kasa Kudineer in Treating Insomnia Patients – A Pilot Study","authors":"S. R, A. N","doi":"10.9734/jpri/2023/v35i247423","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i247423","url":null,"abstract":"Introduction: For stepping towards a healthy living, parameters like good food, sound sleep and right mind, all plays major role to attain health and eternity, which were spelled by Siddhars since ancient times. Additionally, Sleep is the best, fruitful meditation for a quality of life. But, getting quality sleep with sufficient period is a matter of concern in the modern civilized world, irrespective of ages, which leads to serious consequences. When you're constantly losing sleep because of insomnia, your brain doesn't cooperate your body, thereby disturbing to perform important tasks. Hence, Insomnia is a significant health problem because of its high prevalence and management challenges. The aim of the study was to evaluate the effectiveness of Siddha medicine Kasa Kasa Kudineer (KKK), in treating insomnia patients, attending OPD at AAGHIM, Chennai. \u0000Study Design: This was a Pilot study with a sample size of 20, with the intervention of Siddha Medicine Kasa Kasa Kudineer, and the outcome was assessed by the Insomnia Severity Index Score. \u0000Place of Study: The study was conducted at Arignar Anna Government Hospital of Indian Medicine and Homeopathy, attached with Government Siddha Medical College (AAGHIM attached with GSMC), Chennai- 106. \u0000Materials and Methods: The study was conducted at the Arignar Anna Govt. Hospital of Indian Medicine (AAGHIM), attached with Govt. Siddha Medical College, Chennai 106, with a sample size of 20. The study protocol and informed consent were reviewed and approved by IEC (with a waiver from IEC). Patients attending the OPD of AAGHIM with complaints of sleep disturbances were chosen for enrollment based on their insomnia severity index score of more than 15. Siddha Medicine Kasa Kasa Kudineer were adminstrated and the observations were made before and after the treatment using the score. \u0000Results: Results were analyzed. Descriptive statistics, Paired t- test were analyzed using SPSS trial version 25, and out of 20 patients, 17 patients shown significant improvement in their sleep pattern and the total score were also moved to no clinically significant category of Insomnia severity index score. All parameters whose p value is less than 0.05 reject the null hypothesis. Results were encouraging, as it shown considerable improvement by the end of the study. \u0000Conclusion: This study reveals the significant effectiveness of treating Clinically significant insomnia patients, attending OPD at AAGHIM, Chennai with Kasa Kasa Kudineer (KKK), which may ignite a new Siddha medicine for a better quality of life.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43598603","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 : 2023-08-31DOI: 10.9734/jpri/2023/v35i237422
W. S. Al-Thubiani
Multidrug resistance (MDR), as is well known, is regarded as the primary factor in cancer therapy failure. A common mechanism of MDR in anticancer drugs is the expression of P-glycoprotein (P-gp), a class of ATP-dependent membrane transport efflux pumps called adenosine triphosphate (ATP)-binding cassette (ABC) transporters. It pumps xenobiotics outside the cell and plays part in typical physiological detoxification and host defense activities. This transporter is distributed in gastrointestinal mucosa epithelial cell surfaces, blood-tissue barriers, hepatic biliary epithelium, proximal tubules of the kidney, and the adrenal cortex. P-gp is known to be responsible for MDR because of its over-expression in malignant cells. It functions as an efflux pump lowering the concentration of drugs intracellularly, thus decreasing the effectiveness of cancer chemotherapy. Although using multiple anticancer medications is a good strategy, Cancerous cells are able to develop MDR. A number of chemically synthesized P-gp inhibitors were investigated to overcome MDR in clinical studies. Additionally, certain natural compounds have been observed to modulate P-gp. Numerous investigations on strategies to modulate MDR have been conducted as a result of the significant impact of chemotherapeutic drug resistance. This review discusses the role of P-gp in cancer MDR and challenges for inhibiting P-gp in the context of overcoming MDR mediated by P-gp. It is concluded that the discovery of selective, safe, and potent inhibitors of P-gp remains necessary.
{"title":"The Role of P-Glycoprotein (P-gp) in Cancer Multidrug Resistance (MDR): Challenges for Inhibiting P-gp in the Context of Overcoming MDR","authors":"W. S. Al-Thubiani","doi":"10.9734/jpri/2023/v35i237422","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i237422","url":null,"abstract":"Multidrug resistance (MDR), as is well known, is regarded as the primary factor in cancer therapy failure. A common mechanism of MDR in anticancer drugs is the expression of P-glycoprotein (P-gp), a class of ATP-dependent membrane transport efflux pumps called adenosine triphosphate (ATP)-binding cassette (ABC) transporters. It pumps xenobiotics outside the cell and plays part in typical physiological detoxification and host defense activities. This transporter is distributed in gastrointestinal mucosa epithelial cell surfaces, blood-tissue barriers, hepatic biliary epithelium, proximal tubules of the kidney, and the adrenal cortex. P-gp is known to be responsible for MDR because of its over-expression in malignant cells. It functions as an efflux pump lowering the concentration of drugs intracellularly, thus decreasing the effectiveness of cancer chemotherapy. Although using multiple anticancer medications is a good strategy, Cancerous cells are able to develop MDR. A number of chemically synthesized P-gp inhibitors were investigated to overcome MDR in clinical studies. Additionally, certain natural compounds have been observed to modulate P-gp. Numerous investigations on strategies to modulate MDR have been conducted as a result of the significant impact of chemotherapeutic drug resistance. This review discusses the role of P-gp in cancer MDR and challenges for inhibiting P-gp in the context of overcoming MDR mediated by P-gp. It is concluded that the discovery of selective, safe, and potent inhibitors of P-gp remains necessary.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71204544","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 : 2023-08-29DOI: 10.9734/jpri/2023/v35i237421
Saloni T. Mehta, Shaji Mathew, Suvajit Podder, D. Shetty
Background: Laparoscopy procedures have gained an increasing demand over the years and rightly so due to its numerous advantages proving it superior to open surgeries. This is therefore important to all the anaesthesiologists to learn the physiological changes during laparoscopic surgery as well how to manipulate and blunt the hemodynamics as well. Methods: We have taken one such drug, an alpha agonist, oral clonidine and compared its 3 different doses to conclude the most efficacious and safe dosage amongst it. Results: 100 mcg dose of oral Clonidine is the most safest and most effective amongst the 3 doses of 50, 100 and 150 mcg. Conclusion: 1) Premedication with oral clonidine is a safe and effective method that provides haemodynamic stability against the neuroendocrine responses due to carboperitoneum in patients undergoing laparoscopic cholecystectomy. 2) Escalation of doses from 100 microgram to 150 microgram increases adverse effects and does not enhance efficacy.
{"title":"Efficacy of Different Doses of Oral Clonidine as Premedication in Attenuating Haemodynamic Response to Pneumoperitoneum in Patients During Laparoscopic Cholecystectomy","authors":"Saloni T. Mehta, Shaji Mathew, Suvajit Podder, D. Shetty","doi":"10.9734/jpri/2023/v35i237421","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i237421","url":null,"abstract":"Background: Laparoscopy procedures have gained an increasing demand over the years and rightly so due to its numerous advantages proving it superior to open surgeries. This is therefore important to all the anaesthesiologists to learn the physiological changes during laparoscopic surgery as well how to manipulate and blunt the hemodynamics as well.\u0000Methods: We have taken one such drug, an alpha agonist, oral clonidine and compared its 3 different doses to conclude the most efficacious and safe dosage amongst it.\u0000Results: 100 mcg dose of oral Clonidine is the most safest and most effective amongst the 3 doses of 50, 100 and 150 mcg.\u0000Conclusion: 1) Premedication with oral clonidine is a safe and effective method that provides haemodynamic stability against the neuroendocrine responses due to carboperitoneum in patients undergoing laparoscopic cholecystectomy.\u00002) Escalation of doses from 100 microgram to 150 microgram increases adverse effects and does not enhance efficacy.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42919772","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 : 2023-08-28DOI: 10.9734/jpri/2023/v35i237420
Mohamed Ali Ahmed Hassabo, Abdulrhman Mohamed Ali Mohamed, Massab Bashir Khaira
Background: Delirium is a frequent acute neuropsychiatric illness that affects attention, consciousness, and cognition. Objectives: The 4AT evaluation tool's validity and reliability in hospitalized non-ICU patients over 65 were assessed in this systematic study. Method: PRISMA guidelines and the PICO framework were used, and relevant research papers were found utilizing several databases (PubMed, Scopus, Web of Sciences, and ScienceDirect). The Mixed Methods Appraisal Tool was used to evaluate the study's quality. Results: 257 relevant publications were found, and only ten articles were selected based on inclusion criteria after the screening. Several studies were reported from various regions, including Asia, Europe, Canada, and Australia. Furthermore, studies found varying prevalence levels for 4AT and control groups, with the greatest for the 4AT group being 40.32%. Moreover, most research employed DSM-5 criteria, while some relied on CAM, DSM-4, and Psychiatric examination by qualified clinicians. Meanwhile, the sensitivity varied from 70% to 100%, and the specificity ranged from 71.6% to 99.2%. In contrast, other assessment tools, such as CAM and OBS, also demonstrated sensitivity and specificity. The main advantage was the time to complete the 4AT tool, which required 2-3 minutes, whereas the other tools took 3.6 and 12.46 minutes, respectively. The 4AT tool was a rapid, validated, easy patient assessment tool. In addition, it was found to improve delirium diagnosis. Conclusion: The tool has been found to have good sensitivity and specificity, and it may be completed quickly by non-specialists.
背景:谵妄是一种常见的影响注意力、意识和认知的急性神经精神疾病。目的:本系统研究评估了4AT评估工具在65岁以上住院非ICU患者中的有效性和可靠性。方法:使用PRISMA指南和PICO框架,并利用多个数据库(PubMed、Scopus、Web of Sciences和ScienceDirect)找到相关研究论文。使用混合方法评估工具来评估研究的质量。结果:共发现257篇相关文献,筛选后仅根据纳入标准筛选出10篇。来自亚洲、欧洲、加拿大和澳大利亚等不同地区的几项研究报告。此外,研究发现,4AT组和对照组的患病率不同,其中4AT组最高为40.32%。此外,大多数研究采用DSM-5标准,而一些研究依赖于合格临床医生的CAM、DSM-4和精神病检查。同时,敏感性从70%到100%不等,特异性从71.6%到99.2%不等。相比之下,其他评估工具,如CAM和OBS,也表现出敏感性和特异性。主要优点是完成4AT工具的时间,需要2-3分钟,而其他工具分别需要3.6和12.46分钟。4AT工具是一种快速、有效、简单的患者评估工具。此外,它被发现可以改善谵妄的诊断。结论:该工具具有良好的敏感性和特异性,非专家可以快速完成。
{"title":"4 AT Delirium Assessment Tool in Hospitalized Non-ICU Patients (≥65 Years): A Systematic Review on Validity and Reliability","authors":"Mohamed Ali Ahmed Hassabo, Abdulrhman Mohamed Ali Mohamed, Massab Bashir Khaira","doi":"10.9734/jpri/2023/v35i237420","DOIUrl":"https://doi.org/10.9734/jpri/2023/v35i237420","url":null,"abstract":"Background: Delirium is a frequent acute neuropsychiatric illness that affects attention, consciousness, and cognition. \u0000Objectives: The 4AT evaluation tool's validity and reliability in hospitalized non-ICU patients over 65 were assessed in this systematic study. \u0000Method: PRISMA guidelines and the PICO framework were used, and relevant research papers were found utilizing several databases (PubMed, Scopus, Web of Sciences, and ScienceDirect). The Mixed Methods Appraisal Tool was used to evaluate the study's quality. \u0000Results: 257 relevant publications were found, and only ten articles were selected based on inclusion criteria after the screening. Several studies were reported from various regions, including Asia, Europe, Canada, and Australia. Furthermore, studies found varying prevalence levels for 4AT and control groups, with the greatest for the 4AT group being 40.32%. Moreover, most research employed DSM-5 criteria, while some relied on CAM, DSM-4, and Psychiatric examination by qualified clinicians. Meanwhile, the sensitivity varied from 70% to 100%, and the specificity ranged from 71.6% to 99.2%. In contrast, other assessment tools, such as CAM and OBS, also demonstrated sensitivity and specificity. The main advantage was the time to complete the 4AT tool, which required 2-3 minutes, whereas the other tools took 3.6 and 12.46 minutes, respectively. The 4AT tool was a rapid, validated, easy patient assessment tool. In addition, it was found to improve delirium diagnosis. \u0000Conclusion: The tool has been found to have good sensitivity and specificity, and it may be completed quickly by non-specialists.","PeriodicalId":16718,"journal":{"name":"Journal of Pharmaceutical Research International","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45790833","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}