Pub Date : 2024-07-24DOI: 10.3897/pharmacia.71.e118795
Emy Oktaviani, K. Anggadiredja, Lia Amalia
Drug-resistant tuberculosis is a condition in which Mycobacterium tuberculosis is resistant to first-line anti-tuberculosis drugs, namely isoniazid and rifampicin, which are the two most effective anti-tuberculosis agents. Conversion time is a parameter to assess whether the therapeutic effect of injection has been achieved by carrying out two acid-resistant bacilli (ARB) sputum examinations within a maximum period of 2 consecutive months. Kanamycin and capreomycin are injectable drugs that are used in the intensive phase. This cross-sectional study aimed to evaluate the therapeutic effect of injection using ARB sputum conversion time and to analyze other factors related to ARB sputum conversion time. The study used retrospective data from patients’ medical records, collected with purposive sampling technique. The results of the study showed that from 101 patients who met the inclusion criteria 57.4% used kanamycin and 42.6% received capreomycin. The therapeutic effect was achieved in 87.1%. There was no significant correlation between the type of injection therapy and therapeutic effectiveness (p-value = 0.983). In conclusion, therapy using injections for drug-resistant tuberculosis is effective but still requires close monitoring due to the high adverse drug reaction (ADR).
{"title":"Evaluation of therapeutic effectiveness of antituberculosis injection based on conversion time in drug-resistant tuberculosis","authors":"Emy Oktaviani, K. Anggadiredja, Lia Amalia","doi":"10.3897/pharmacia.71.e118795","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e118795","url":null,"abstract":"Drug-resistant tuberculosis is a condition in which Mycobacterium tuberculosis is resistant to first-line anti-tuberculosis drugs, namely isoniazid and rifampicin, which are the two most effective anti-tuberculosis agents. Conversion time is a parameter to assess whether the therapeutic effect of injection has been achieved by carrying out two acid-resistant bacilli (ARB) sputum examinations within a maximum period of 2 consecutive months. Kanamycin and capreomycin are injectable drugs that are used in the intensive phase. This cross-sectional study aimed to evaluate the therapeutic effect of injection using ARB sputum conversion time and to analyze other factors related to ARB sputum conversion time. The study used retrospective data from patients’ medical records, collected with purposive sampling technique. The results of the study showed that from 101 patients who met the inclusion criteria 57.4% used kanamycin and 42.6% received capreomycin. The therapeutic effect was achieved in 87.1%. There was no significant correlation between the type of injection therapy and therapeutic effectiveness (p-value = 0.983). In conclusion, therapy using injections for drug-resistant tuberculosis is effective but still requires close monitoring due to the high adverse drug reaction (ADR).","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141806840","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 : 2024-07-23DOI: 10.3897/pharmacia.71.e131544
Rada Nedelcheva, Y. Zarev, I. Ionkova
This research investigates the production and optimization of justicidin B from L. austriacum and L. alpinum in vitro cultures, aiming for high yields of this pharmacologically significant arylnaphthalene lignan. Various cultivation techniques were employed, including shoot, root, and callus cultures, with different media formulations to induce justicidin B biosynthesis. In vitro shoots, callus, and root cultures of both Linum species were successfully established to enhance justicidin B production. Quantification of the lignan was performed using LC-HRESI-MS analysis, comparing the quantities to those of isolated and identified justicidin B from L. leonii hairy root extract. The results show that the in vitro root cultures of L. alpinum produced 1.3 times more justicidin B than those of L. austriacum (7.24 μg/mg DW and 5.31 μg/mg DW, respectively). Additionally, the shoot cultures of L. alpinum yielded 4.5 times more justicidin B than those of L. austriacum (4.34 μg/mg DW and 0.96 μg/mg DW, respectively).
本研究调查了从奥斯特里亚库藻和阿尔平藻体外培养物中生产和优化刚毛苷 B 的情况,目的是高产这种具有重要药理作用的芳香萘木脂素。我们采用了多种培养技术,包括芽、根和胼胝体培养,并使用不同的培养基配方来诱导刚毛苷 B 的生物合成。成功建立了两种亚麻属植物的离体嫩枝、胼胝体和根培养物,以提高刚毛苷 B 的产量。利用 LC-HRESI-MS 分析法对木脂素进行定量,并将其数量与从 L. leonii 毛根提取物中分离和鉴定的刚毛苷 B 的数量进行比较。结果表明,L. alpinum 的离体根培养物产生的刚毛苷 B 是 L. austriacum 的 1.3 倍(分别为 7.24 μg/mg DW 和 5.31 μg/mg DW)。此外,L. alpinum 的嫩枝培养物产生的抗坏血酸 B 是 L. austriacum 的 4.5 倍(分别为 4.34 μg/mg DW 和 0.96 μg/mg DW)。
{"title":"Comparative quantitative profiling of rare justicidin B in in vitro cultivated Linum species","authors":"Rada Nedelcheva, Y. Zarev, I. Ionkova","doi":"10.3897/pharmacia.71.e131544","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e131544","url":null,"abstract":"This research investigates the production and optimization of justicidin B from L. austriacum and L. alpinum in vitro cultures, aiming for high yields of this pharmacologically significant arylnaphthalene lignan. Various cultivation techniques were employed, including shoot, root, and callus cultures, with different media formulations to induce justicidin B biosynthesis. In vitro shoots, callus, and root cultures of both Linum species were successfully established to enhance justicidin B production. Quantification of the lignan was performed using LC-HRESI-MS analysis, comparing the quantities to those of isolated and identified justicidin B from L. leonii hairy root extract. The results show that the in vitro root cultures of L. alpinum produced 1.3 times more justicidin B than those of L. austriacum (7.24 μg/mg DW and 5.31 μg/mg DW, respectively). Additionally, the shoot cultures of L. alpinum yielded 4.5 times more justicidin B than those of L. austriacum (4.34 μg/mg DW and 0.96 μg/mg DW, respectively).","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141811024","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 : 2024-07-23DOI: 10.3897/pharmacia.71.e126255
Huu Lac Thuy Nguyen, Thi Thu Phuong Ha, Ngoc Phuc Nguyen, Nguyen Hoang Linh Phan, Dang Thuy Hien Nguyen, Van Dat Truong, Minh-Nhut Truong, Thao-My Nguyen-Hoang, Thi Nghia Luu, Ngoc Phuc Nguyen, Thanh Binh Nguyen, H. Mai
Diabetes has always been a matter of concern to health experts as well as the community due to the increasing number of patients with diabetes and the severe consequences it may cause. Many attempts have been made to discover new treatment options for diabetes, and herbal medicines are currently considered to have great potential. This study was conducted to evaluate the effect of Camellia flava flower extract on the degeneration of the islets of Langerhans and insulin resistance in an alloxan-induced hyperglycemia model in Swiss albino mice. Hyperglycemic conditions were induced by alloxan (55 mg/kg, i.v.). The animals were then treated with glibenclamide (10 mg/kg, p.o.) and flower extract at doses of 1.09 and 2.19 g/kg, p.o. The results showed that the blood glucose, AUC, HbA1c, and HOMA-IR levels of two groups of mice receiving flower extract were considerably lower than those of the hyperglycemic untreated group (p < 0.05). The body weights of these two groups were also lower than the untreated group on the last day of the experiment, though the differences were not significant (p > 0.05). However, this was not observed when assessing insulin levels as well as relative organ weights. In biochemical tests, creatinine and AST and ALT concentrations were evaluated. There was no significant variation in creatinine and AST concentrations between the five experimental groups, whereas mice treated with glibenclamide and flower extract at both doses showed a remarkable decline in ALT concentration (p < 0.05). The hepatic histomicrographs were consistent with ALT results, while the H&E staining of kidneys showed no difference between groups. Histomicrographs of the pancreas revealed that the treatment groups using glibenclamide and flower extract had larger islets of Langerhans than those of the alloxan-treated group. Based on these results, this study demonstrated that Camellia flava flower extract exerted several beneficial effects, including blood sugar level reduction, weight loss promotion, and organ protection, hence making it a new potential herbal medication for the management of diabetes.
{"title":"Effect of Camellia flava (Pitard) Sealy flower extract on the degeneration of Islets of Langerhans and insulin resistance in alloxan-induced hyperglycemia model on Swiss albino mice","authors":"Huu Lac Thuy Nguyen, Thi Thu Phuong Ha, Ngoc Phuc Nguyen, Nguyen Hoang Linh Phan, Dang Thuy Hien Nguyen, Van Dat Truong, Minh-Nhut Truong, Thao-My Nguyen-Hoang, Thi Nghia Luu, Ngoc Phuc Nguyen, Thanh Binh Nguyen, H. Mai","doi":"10.3897/pharmacia.71.e126255","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e126255","url":null,"abstract":"Diabetes has always been a matter of concern to health experts as well as the community due to the increasing number of patients with diabetes and the severe consequences it may cause. Many attempts have been made to discover new treatment options for diabetes, and herbal medicines are currently considered to have great potential. This study was conducted to evaluate the effect of Camellia flava flower extract on the degeneration of the islets of Langerhans and insulin resistance in an alloxan-induced hyperglycemia model in Swiss albino mice. Hyperglycemic conditions were induced by alloxan (55 mg/kg, i.v.). The animals were then treated with glibenclamide (10 mg/kg, p.o.) and flower extract at doses of 1.09 and 2.19 g/kg, p.o. The results showed that the blood glucose, AUC, HbA1c, and HOMA-IR levels of two groups of mice receiving flower extract were considerably lower than those of the hyperglycemic untreated group (p < 0.05). The body weights of these two groups were also lower than the untreated group on the last day of the experiment, though the differences were not significant (p > 0.05). However, this was not observed when assessing insulin levels as well as relative organ weights. In biochemical tests, creatinine and AST and ALT concentrations were evaluated. There was no significant variation in creatinine and AST concentrations between the five experimental groups, whereas mice treated with glibenclamide and flower extract at both doses showed a remarkable decline in ALT concentration (p < 0.05). The hepatic histomicrographs were consistent with ALT results, while the H&E staining of kidneys showed no difference between groups. Histomicrographs of the pancreas revealed that the treatment groups using glibenclamide and flower extract had larger islets of Langerhans than those of the alloxan-treated group. Based on these results, this study demonstrated that Camellia flava flower extract exerted several beneficial effects, including blood sugar level reduction, weight loss promotion, and organ protection, hence making it a new potential herbal medication for the management of diabetes.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141810432","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 : 2024-07-18DOI: 10.3897/pharmacia.71.e118323
Rashad M. Kaoud, Mustafa Hasan Alwan, Mohammed Amran, Hayder Adnan Fawzi
Hydrogels have gained much focus as a gastro-retentive technology for drug delivery. The current study aimed to design an oral mucoadhesive sustained-release dosage form to lower peptic ulcer complications (PUC). Using the Box-Behnken statistical design, the preparation method was developed by incorporating pantoprazole sodium (PZS) into hydrogel microcapsules (HGMC). The PZS was incorporated into the HGMC via an ion gelation technique, with sodium alginate as the gelling agent, calcium chloride as the crosslinking agent, and chitosan as the agent for sustained release. The optimized formulation of PZS-HGMC showed a diameter of 2.506 mm, a swelling rate of 838.2%, and an encapsulation efficiency of 93.8%. Scanning electron microscopy images revealed the microcapsules’ spherical shape. The in vitro release of the PZS from the HGMC after two hours in a simulated gastric fluid was 13.2%1±0.08%, compared with the apparent solubility of the pure PZS under the same conditions (95.24%±3.2%). After 24 hours, the percent of PZS released from the optimized formula was 69.84±2.4%, which indicates a sustained release pattern. The results from the in vivo study demonstrated improved healing of the induced ulcers in rats when treated with the PZS-HGMC formulation as compared to the standard PZS therapy; therefore, the obtained mucoadhesive HGMC was considered a potential drug delivery strategy for PUC therapy.
{"title":"Design and optimization of pantoprazole sodium mucoadhesive hydrogel microcapsules for the healing of peptic ulcers","authors":"Rashad M. Kaoud, Mustafa Hasan Alwan, Mohammed Amran, Hayder Adnan Fawzi","doi":"10.3897/pharmacia.71.e118323","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e118323","url":null,"abstract":"Hydrogels have gained much focus as a gastro-retentive technology for drug delivery. The current study aimed to design an oral mucoadhesive sustained-release dosage form to lower peptic ulcer complications (PUC). Using the Box-Behnken statistical design, the preparation method was developed by incorporating pantoprazole sodium (PZS) into hydrogel microcapsules (HGMC). The PZS was incorporated into the HGMC via an ion gelation technique, with sodium alginate as the gelling agent, calcium chloride as the crosslinking agent, and chitosan as the agent for sustained release.\u0000 The optimized formulation of PZS-HGMC showed a diameter of 2.506 mm, a swelling rate of 838.2%, and an encapsulation efficiency of 93.8%. Scanning electron microscopy images revealed the microcapsules’ spherical shape. The in vitro release of the PZS from the HGMC after two hours in a simulated gastric fluid was 13.2%1±0.08%, compared with the apparent solubility of the pure PZS under the same conditions (95.24%±3.2%). After 24 hours, the percent of PZS released from the optimized formula was 69.84±2.4%, which indicates a sustained release pattern. The results from the in vivo study demonstrated improved healing of the induced ulcers in rats when treated with the PZS-HGMC formulation as compared to the standard PZS therapy; therefore, the obtained mucoadhesive HGMC was considered a potential drug delivery strategy for PUC therapy.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141824114","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 : 2024-07-16DOI: 10.3897/pharmacia.71.e127997
D. Momekova, Viliana Gugleva, Petar Petrov
Vesicular carriers are a well-established approach to improving the technological and biopharmaceutical characteristics of the loaded cargo. The current manuscript is focused on the development and evaluation in a comparative aspect of two types of vesicles—ethosomes and transfersomes loaded with the phytoconstituent curcumin. The formulation variables affecting their physiochemical and cytotoxic properties are outlined as well. A series of ethosomes and transfersomes based on Lipoid S75 and ethanol, or edge activator, were prepared using the thin film hydration method and subjected to comprehensive evaluation by dynamic light scattering (DLS) analysis, transmission electron microscopy (TEM), entrapment efficiency evaluation, in vitro release, and cytotoxicity studies. Ethosomes based on Lipoid S75 (4% w/w) and ethanol (30% v/v) showed suitable physicochemical characteristics (hydrodynamic diameter of 578.6 nm, monomodal size distribution, high curcumin entrapment efficiency (78.2%)), and superior antiproliferative activity compared to free drug and transfersomal nanocarriers.
{"title":"Development and evaluation of curcumin-loaded vesicular carriers: impact of formulation variables","authors":"D. Momekova, Viliana Gugleva, Petar Petrov","doi":"10.3897/pharmacia.71.e127997","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127997","url":null,"abstract":"Vesicular carriers are a well-established approach to improving the technological and biopharmaceutical characteristics of the loaded cargo. The current manuscript is focused on the development and evaluation in a comparative aspect of two types of vesicles—ethosomes and transfersomes loaded with the phytoconstituent curcumin. The formulation variables affecting their physiochemical and cytotoxic properties are outlined as well. A series of ethosomes and transfersomes based on Lipoid S75 and ethanol, or edge activator, were prepared using the thin film hydration method and subjected to comprehensive evaluation by dynamic light scattering (DLS) analysis, transmission electron microscopy (TEM), entrapment efficiency evaluation, in vitro release, and cytotoxicity studies. Ethosomes based on Lipoid S75 (4% w/w) and ethanol (30% v/v) showed suitable physicochemical characteristics (hydrodynamic diameter of 578.6 nm, monomodal size distribution, high curcumin entrapment efficiency (78.2%)), and superior antiproliferative activity compared to free drug and transfersomal nanocarriers.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141640722","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 : 2024-07-15DOI: 10.3897/pharmacia.71.e127395
Kurnia Agustini, Frangky Sangande, Nuralih Nuralih, Armansyah Maulana Harahap, Sri Ningsih, Anton Bahtiar
Breast cancer (BC) is a multifactorial disease involving many pathways and target molecules. Multi-target therapy through multi-compound herbal medicines is an alternative strategy to treat BC. In the present study, we elucidate the molecular mechanism of Ocimum basilicum (OB) as an anticancer agent using system bioinformatic approach and investigate its cytotoxic effect against MCF-7 cells. We performed network pharmacology (NP) and molecular docking studies to provide scientific information regarding the underlying anti-BC mechanism of OB. Based on topology parameters obtained from protein-protein interaction (PPI), we identified six potential targets that play a significant role in the network including SRC, PI3KCA, EGFR, ESR1, AKT1, and MAPK1. Furthermore, consensus docking suggested rutin, quercetin-3-O-diglucoside, and kaempferol-3-O-β-D-rutinoside as the potential compounds of OB. Moreover, Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis demonstrated that the cytotoxic effect of OB might be related to the modulation of several pathways such as PI3K-Akt, VEGF, and HIF-1, breast cancer, and estrogen signaling pathways. The in vitro assay revealed that various extracts of OB demonstrated cytotoxic effects against MCF-7 with IC50 = 231 µg/mL (OB ethanolic extract), 408 µg/mL (OB methanolic extract), 479 µg/mL (OB ethyl acetate extract), 1887 µg/mL (OB n-hexanoic extract) and 767 µg/mL (OB butanolic extract) respectively.
{"title":"Molecular mechanism elucidation of Ocimum basilicum as anticancer using system bioinformatic approach supported by in vitro assay","authors":"Kurnia Agustini, Frangky Sangande, Nuralih Nuralih, Armansyah Maulana Harahap, Sri Ningsih, Anton Bahtiar","doi":"10.3897/pharmacia.71.e127395","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e127395","url":null,"abstract":"Breast cancer (BC) is a multifactorial disease involving many pathways and target molecules. Multi-target therapy through multi-compound herbal medicines is an alternative strategy to treat BC. In the present study, we elucidate the molecular mechanism of Ocimum basilicum (OB) as an anticancer agent using system bioinformatic approach and investigate its cytotoxic effect against MCF-7 cells. We performed network pharmacology (NP) and molecular docking studies to provide scientific information regarding the underlying anti-BC mechanism of OB. Based on topology parameters obtained from protein-protein interaction (PPI), we identified six potential targets that play a significant role in the network including SRC, PI3KCA, EGFR, ESR1, AKT1, and MAPK1. Furthermore, consensus docking suggested rutin, quercetin-3-O-diglucoside, and kaempferol-3-O-β-D-rutinoside as the potential compounds of OB. Moreover, Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis demonstrated that the cytotoxic effect of OB might be related to the modulation of several pathways such as PI3K-Akt, VEGF, and HIF-1, breast cancer, and estrogen signaling pathways. The in vitro assay revealed that various extracts of OB demonstrated cytotoxic effects against MCF-7 with IC50 = 231 µg/mL (OB ethanolic extract), 408 µg/mL (OB methanolic extract), 479 µg/mL (OB ethyl acetate extract), 1887 µg/mL (OB n-hexanoic extract) and 767 µg/mL (OB butanolic extract) respectively.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141646802","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 : 2024-07-15DOI: 10.3897/pharmacia.71.e124486
Ali Mohammed, Laith Saleh Alkaaby, Nada Alshawi
Surgical site infection (SSI) is a serious postoperative complication after cardiac surgery. The objective of this research is to examine the efficacy of administering gentamicin in minimizing the incidence of SSI while closely monitoring the therapeutic level of the drug. Prospective research included 50 Iraqi patients divided into two groups, 25 in each: Group 1 received a combination of flucloxacillin and ceftriaxone, while Group 2 received a combination of flucloxacillin and gentamicin 2 mg/kg of ideal body weight given before surgery, then 80 mg*3 for 48 hours after surgery. A total of five patients had an infection at the surgical site, with four patients in Group 1 and one patient in Group 2. Additionally, two patients in each group exhibited increased renal indices. Among the patients in Group 2, the highest concentration of gentamicin in the blood was ≤ 2.5 µg/ml for eight patients, while for 17 patients, the gentamicin concentration in the blood ranged from 3 to 4.4 µg/ml.
{"title":"The pharmacological and clinical aspects of using gentamicin in cardiac surgery","authors":"Ali Mohammed, Laith Saleh Alkaaby, Nada Alshawi","doi":"10.3897/pharmacia.71.e124486","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e124486","url":null,"abstract":"Surgical site infection (SSI) is a serious postoperative complication after cardiac surgery. The objective of this research is to examine the efficacy of administering gentamicin in minimizing the incidence of SSI while closely monitoring the therapeutic level of the drug. Prospective research included 50 Iraqi patients divided into two groups, 25 in each: Group 1 received a combination of flucloxacillin and ceftriaxone, while Group 2 received a combination of flucloxacillin and gentamicin 2 mg/kg of ideal body weight given before surgery, then 80 mg*3 for 48 hours after surgery. A total of five patients had an infection at the surgical site, with four patients in Group 1 and one patient in Group 2. Additionally, two patients in each group exhibited increased renal indices. Among the patients in Group 2, the highest concentration of gentamicin in the blood was ≤ 2.5 µg/ml for eight patients, while for 17 patients, the gentamicin concentration in the blood ranged from 3 to 4.4 µg/ml.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141646734","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 : 2024-07-12DOI: 10.3897/pharmacia.71.e123737
Saif Aldeen Jaber
Metabolomics is a technique used to compare the chemical profiles of different extracts. Natural sources like plants can be used, after being linked with metabolomics, to enhance the ability of drug discovery. A multivariate analysis and metabolomics profiling were performed on Quercus coccifera leaf extracts using LC-HRMS and NMR raw data using the SIMCA 14.0 program. All multivariate analyses were guided by the results of the α-amylase and -glucosidase inhibitory activity of the produced extracts. Both boiled water and methanolic extracts were selected to be active, with a percentage of inhibition higher than 80% upon using 1 mg/ml of each extract. The rest of the extract was found to be inactive and failed to obtain biological activity greater than 40%. Only methanolic extract was found to have a unique chemical profile and was found as an outlayer in both the supervised and unsupervised PCA scatter plots. The rest of the extracts were found to exert a known chemical profile and were found inside the domain. In addition, the OPLS-DA loading plot and heat map indicate the presence of a highly diverse chemical profile in methanol, with higher and lower chemical shifts and molecular weights. Both boiled water and methanol extracts were found to exert similar activity, but metabolomics profiling shows that methanolic extract contains a unique chemical profile and should be selected for a further fraction for the possible discovery of a new antidiabetic compound.
{"title":"Implementing metabolomics techniques in the acceleration of the discovery of new antidiabetic bioactive metabolites obtained from Quercus coccifera","authors":"Saif Aldeen Jaber","doi":"10.3897/pharmacia.71.e123737","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e123737","url":null,"abstract":"Metabolomics is a technique used to compare the chemical profiles of different extracts. Natural sources like plants can be used, after being linked with metabolomics, to enhance the ability of drug discovery. A multivariate analysis and metabolomics profiling were performed on Quercus coccifera leaf extracts using LC-HRMS and NMR raw data using the SIMCA 14.0 program. All multivariate analyses were guided by the results of the α-amylase and -glucosidase inhibitory activity of the produced extracts. Both boiled water and methanolic extracts were selected to be active, with a percentage of inhibition higher than 80% upon using 1 mg/ml of each extract. The rest of the extract was found to be inactive and failed to obtain biological activity greater than 40%. Only methanolic extract was found to have a unique chemical profile and was found as an outlayer in both the supervised and unsupervised PCA scatter plots. The rest of the extracts were found to exert a known chemical profile and were found inside the domain. In addition, the OPLS-DA loading plot and heat map indicate the presence of a highly diverse chemical profile in methanol, with higher and lower chemical shifts and molecular weights. Both boiled water and methanol extracts were found to exert similar activity, but metabolomics profiling shows that methanolic extract contains a unique chemical profile and should be selected for a further fraction for the possible discovery of a new antidiabetic compound.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141653403","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 : 2024-07-12DOI: 10.3897/pharmacia.71.e125421
I. Parvova, T. Delyiski, Parvoleta Peteva, Lubomir Marinchev, E. Hristov, E. Yordanov, V. Petkova
Systemic vasculitides are rare and heterogeneous diseases affecting different organs and systems with varying degrees of severity depending on the type of vessels affected. The etiology and pathogenesis are unclear. Immunе mechanisms play a role in the pathogenesis: deposition of immune complexes, autoantibodies (anti-endothelial and anti-neutrophil cytoplasmic antibody, cellular and molecular responses, granulomas, and endothelial cell damage. All vasculitides are “rare diseases”. ANCA- associated vasculitis has an incidence of 20 cases/1 million population. Without treatment, mortality is >90% within up to 5 years. We conducted a two-centre, retrospective, observational, non- interventional, epidemiological, health-demographic, clinical-pharmacological study to evaluate ANCA-associated vasculitis in Bulgaria. From 2018 to 2021, we screened 12 individuals with Wegener’s granulomatosis. The analyzed population is approximately 60% of the patients in Bulgaria. The time from symptom onset to diagnosis is short, but the diagnosis is made at an advanced stage of the disease - the measured BVAS version 3 activity is moderate-severe.
{"title":"Systemic vasculitis associated with anti neutrophil cytoplasmic antibodies in Bulgaria – epidemiological, health-demographic and clinical-pharmacological real-world data","authors":"I. Parvova, T. Delyiski, Parvoleta Peteva, Lubomir Marinchev, E. Hristov, E. Yordanov, V. Petkova","doi":"10.3897/pharmacia.71.e125421","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e125421","url":null,"abstract":"Systemic vasculitides are rare and heterogeneous diseases affecting different organs and systems with varying degrees of severity depending on the type of vessels affected. The etiology and pathogenesis are unclear. Immunе mechanisms play a role in the pathogenesis: deposition of immune complexes, autoantibodies (anti-endothelial and anti-neutrophil cytoplasmic antibody, cellular and molecular responses, granulomas, and endothelial cell damage. All vasculitides are “rare diseases”. ANCA- associated vasculitis has an incidence of 20 cases/1 million population. Without treatment, mortality is >90% within up to 5 years. We conducted a two-centre, retrospective, observational, non- interventional, epidemiological, health-demographic, clinical-pharmacological study to evaluate ANCA-associated vasculitis in Bulgaria. From 2018 to 2021, we screened 12 individuals with Wegener’s granulomatosis. The analyzed population is approximately 60% of the patients in Bulgaria. The time from symptom onset to diagnosis is short, but the diagnosis is made at an advanced stage of the disease - the measured BVAS version 3 activity is moderate-severe.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141655236","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 : 2024-07-12DOI: 10.3897/pharmacia.71.e124595
Anuragh Singh, Vellapandian Chitra, K. Ilango
The hepatic manifestation of metabolic syndrome, associated with various metabolic diseases such as type 2 diabetes, insulin resistance, and high cholesterol, is called non-alcoholic fatty liver disease (NAFLD). Despite several research efforts, no approved medicine is currently available for the treatment of this illness. Swiss Target Prediction was used to screen phytochemicals. To examine potential targets, the protein-protein interaction (PPI) network was developed. Cytoscape was used to create the component-target-pathway (C-T-P) network, and AutoDock was used to assess molecular docking. Antioxidant and anti-inflammatory qualities were tested in vitro. Naringenin, ellagic acid, and cyanidin were found to be the main active components. As important targets, PPARA, PPARG, and AKT1 were selected. Through enrichment analysis, a total of 20 crucial signaling pathways, including insulin resistance (IR), NAFLD, relaxin, PI3K-Akt, HIF-1, AGE-RAGE, and MAPK, were identified. The in silico computational techniques predicted the molecular pathway for the active ingredients and the disease targets, thus helping to further research.
{"title":"Network pharmacology exploration to reveal molecular insights of Phyllanthus niruri in non-alcoholic fatty liver: In vitro and in silico evidence","authors":"Anuragh Singh, Vellapandian Chitra, K. Ilango","doi":"10.3897/pharmacia.71.e124595","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e124595","url":null,"abstract":"The hepatic manifestation of metabolic syndrome, associated with various metabolic diseases such as type 2 diabetes, insulin resistance, and high cholesterol, is called non-alcoholic fatty liver disease (NAFLD). Despite several research efforts, no approved medicine is currently available for the treatment of this illness. Swiss Target Prediction was used to screen phytochemicals. To examine potential targets, the protein-protein interaction (PPI) network was developed. Cytoscape was used to create the component-target-pathway (C-T-P) network, and AutoDock was used to assess molecular docking. Antioxidant and anti-inflammatory qualities were tested in vitro. Naringenin, ellagic acid, and cyanidin were found to be the main active components. As important targets, PPARA, PPARG, and AKT1 were selected. Through enrichment analysis, a total of 20 crucial signaling pathways, including insulin resistance (IR), NAFLD, relaxin, PI3K-Akt, HIF-1, AGE-RAGE, and MAPK, were identified. The in silico computational techniques predicted the molecular pathway for the active ingredients and the disease targets, thus helping to further research.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141654395","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}