C. Tipbunjong, Rattanaporn Sengkhim, Sitthiwach Thantongsakul, S. Peerakietkhajorn, J. Mayakun, N. Huipao, P. Khuituan
Purpose: To provide valid scientific evidence for the safety of Sargassum plagiophyllum extract in an animal model. Methods: Sargassum plagiophyllum extract (SPE) was obtained via water extraction using an autoclave at 121°C for 20 min. The SPE was administered to 4 groups of adult male mice via gavage once a day for 21 days. The treatment groups received different doses of SPE, i.e., 100, 500, 1000, and 2000 mg/kg. Control mice were given distilled water. Body weight, and feed and water intakes were recorded. The toxicity of SPE was assessed by determining blood, biochemical, and histopathological indices. Results: Intake of SPE for 21 days did not produce any impact on body mass, feed intake and water intake, even at 2000 mg/kg. Hematological parameters were also unaffected. Biochemical analysis of blood/serum revealed normal levels of blood urea nitrogen (BUN), creatinine, alanine transaminase (ALT), aspartate transaminase (AST), and alkaline phosphatase (ALP) in all treatment groups, when compared to control group. Moreover, histopathological studies confirmed healthy conditions of the liver, kidney, colon, and other organs in all treatment groups. Conclusion: These results from a mouse model provide basic scientific evidence of the safety of consuming Sargassum plagiophyllum extract, even at high doses thus expanding its potential use as a medication for improving health.
{"title":"Toxicological evaluation of Sargassum plagiophyllum extract in male mice","authors":"C. Tipbunjong, Rattanaporn Sengkhim, Sitthiwach Thantongsakul, S. Peerakietkhajorn, J. Mayakun, N. Huipao, P. Khuituan","doi":"10.4314/tjpr.v22i11.11","DOIUrl":"https://doi.org/10.4314/tjpr.v22i11.11","url":null,"abstract":"Purpose: To provide valid scientific evidence for the safety of Sargassum plagiophyllum extract in an animal model. \u0000Methods: Sargassum plagiophyllum extract (SPE) was obtained via water extraction using an autoclave at 121°C for 20 min. The SPE was administered to 4 groups of adult male mice via gavage once a day for 21 days. The treatment groups received different doses of SPE, i.e., 100, 500, 1000, and 2000 mg/kg. Control mice were given distilled water. Body weight, and feed and water intakes were recorded. The toxicity of SPE was assessed by determining blood, biochemical, and histopathological indices. \u0000Results: Intake of SPE for 21 days did not produce any impact on body mass, feed intake and water intake, even at 2000 mg/kg. Hematological parameters were also unaffected. Biochemical analysis of blood/serum revealed normal levels of blood urea nitrogen (BUN), creatinine, alanine transaminase (ALT), aspartate transaminase (AST), and alkaline phosphatase (ALP) in all treatment groups, when compared to control group. Moreover, histopathological studies confirmed healthy conditions of the liver, kidney, colon, and other organs in all treatment groups. \u0000Conclusion: These results from a mouse model provide basic scientific evidence of the safety of consuming Sargassum plagiophyllum extract, even at high doses thus expanding its potential use as a medication for improving health.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"92 23","pages":""},"PeriodicalIF":0.6,"publicationDate":"2024-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139440168","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To determine the effect of paclitaxel octreotide conjugate (POC) on human ovarian paclitaxelresistant cell xenograft tumor model and the mechanism underlying reversal of paclitaxel resistance.
Methods: Forty female BALB/c-nu/nu mice were subcutaneously inoculated with 106 paclitaxel-resistant cells (a2780/taxol) per mouse during the logarithmic growth phase of ovarian cancer. They were randomly divided into four groups (control, octreotide, paclitaxel and POC). Immunohistochemical streptavidin-peroxidase (SP) method was used to determine expression of nuclear proliferation antigen (PCNA) while TUNEL method was used to assess apoptosis of human ovarian cancer metastasis. Realtime polymerase chain reaction (PCR) was used to assay mRNA expression levels of somatostatin receptor 2 (SSTR2), multidrug-resistant gene (MDR1), vascular endothelial growth factor (VEGF), matrix metalloproteinase-9 (MMP-9), and acetylated tubulin (α-tubulin and β-III-tubulin), while the corresponding protein expressions were assayed using western blotting.
Results: Immunohistochemical SP showed significantly lower PCNA levels in octreotide, paclitaxel and POC groups than in control mice, but that of POC mice was significantly reduced, relative to those of octreotide and paclitaxel groups (p < 0.05). There were significantly higher expression levels of SSTR2 mRNA and protein in octreotide, paclitaxel and POC groups than in control mice, but they were significantly higher in POC group than in octreotide and paclitaxel groups (p < 0.05). The mRNA and protein expressions of other factors in POC mice were significantly lower than those in both octreotide and paclitaxel groups (p < 0.05).
Conclusion: Paclitaxel-octreotide conjugate effectively inhibits the growth of a2780/taxol xenografts in nude mice, induces tumor cell apoptosis, and suppresses tumor cell growth via mechanism involving enhancement of SSTR2 expression, and decreases in levels of acetylated tubulin, matrix metalloproteinase-9, and vascular endothelial growth factor.
目的:探讨紫杉醇奥曲肽偶联物(POC)对人卵巢紫杉醇耐药细胞异种移植瘤模型的影响及逆转紫杉醇耐药的机制;方法:40只雌性BALB/c-nu/nu小鼠在卵巢癌对数生长期皮下接种106个紫杉醇耐药细胞(a2780/紫杉醇)。随机分为对照组、奥曲肽组、紫杉醇组和POC组。采用免疫组化streptavidin-peroxidase (SP)法检测增殖抗原(PCNA)表达，TUNEL法检测人卵巢癌转移灶细胞凋亡。采用实时聚合酶链反应(real - time polymerase chain reaction, PCR)检测生长抑素受体2 (SSTR2)、多药耐药基因(MDR1)、血管内皮生长因子(VEGF)、基质金属蛋白酶-9 (MMP-9)、乙酰化微管蛋白(α-微管蛋白和β- iii -微管蛋白)mRNA表达水平，同时采用western blotting检测相应蛋白表达水平。
结果:免疫组化SP显示，奥曲肽组、紫杉醇组和POC组小鼠的PCNA水平明显低于对照组，而POC组小鼠的PCNA水平明显低于奥曲肽组和紫杉醇组(p <0.05)。SSTR2 mRNA和蛋白在奥曲肽、紫杉醇和POC组的表达水平均显著高于对照组，但POC组显著高于奥曲肽和紫杉醇组(p <0.05)。与奥曲肽组和紫杉醇组相比，POC小鼠其他因子的mRNA和蛋白表达均显著降低(p <0.05)强生# x0D;结论:紫杉醇-奥曲肽偶联物能有效抑制裸小鼠a2780/紫杉醇异种移植物的生长，诱导肿瘤细胞凋亡，抑制肿瘤细胞生长的机制可能与增强SSTR2的表达，降低乙酰化微管蛋白、基质金属蛋白酶-9、血管内皮生长因子水平有关。
{"title":"Effect of paclitaxel octreotide conjugate on human ovarian paclitaxel-resistant cell xenograft tumor model and the mechanism underlying reversal of paclitaxel resistance","authors":"Hui Guo, Jing Ma, Shifa Yuan, Ying Wang","doi":"10.4314/tjpr.v22i10.13","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.13","url":null,"abstract":"Purpose: To determine the effect of paclitaxel octreotide conjugate (POC) on human ovarian paclitaxelresistant cell xenograft tumor model and the mechanism underlying reversal of paclitaxel resistance.
 Methods: Forty female BALB/c-nu/nu mice were subcutaneously inoculated with 106 paclitaxel-resistant cells (a2780/taxol) per mouse during the logarithmic growth phase of ovarian cancer. They were randomly divided into four groups (control, octreotide, paclitaxel and POC). Immunohistochemical streptavidin-peroxidase (SP) method was used to determine expression of nuclear proliferation antigen (PCNA) while TUNEL method was used to assess apoptosis of human ovarian cancer metastasis. Realtime polymerase chain reaction (PCR) was used to assay mRNA expression levels of somatostatin receptor 2 (SSTR2), multidrug-resistant gene (MDR1), vascular endothelial growth factor (VEGF), matrix metalloproteinase-9 (MMP-9), and acetylated tubulin (α-tubulin and β-III-tubulin), while the corresponding protein expressions were assayed using western blotting.
 Results: Immunohistochemical SP showed significantly lower PCNA levels in octreotide, paclitaxel and POC groups than in control mice, but that of POC mice was significantly reduced, relative to those of octreotide and paclitaxel groups (p < 0.05). There were significantly higher expression levels of SSTR2 mRNA and protein in octreotide, paclitaxel and POC groups than in control mice, but they were significantly higher in POC group than in octreotide and paclitaxel groups (p < 0.05). The mRNA and protein expressions of other factors in POC mice were significantly lower than those in both octreotide and paclitaxel groups (p < 0.05).
 Conclusion: Paclitaxel-octreotide conjugate effectively inhibits the growth of a2780/taxol xenografts in nude mice, induces tumor cell apoptosis, and suppresses tumor cell growth via mechanism involving enhancement of SSTR2 expression, and decreases in levels of acetylated tubulin, matrix metalloproteinase-9, and vascular endothelial growth factor.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"90 5","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685376","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To investigate the effect of gold nanocomposite carrying hypoxia-inducible factor-1α (HIF-1α) siRNA on radiosensitivity of nasopharynx cancer (NPC) cells.
Methods: Gold nanocomposite (AuNRs-(PEI-PEG)/RGD) or (AuPPR) was first synthesized and its cytotoxicity was evaluated. Then, the expression of HIF-1α in hypoxic NPC cells was assessed. In addition, the radiation sensitivity of AuPPR bearing HIF-1α siRNA on the cells was examined under xray exposure.
Result: Gold nanocomposite (AuPPR) carrying HIF-1α siRNA (AuPPR-HIF-1α siRNA) significantly down-regulated HIF-1α expression. Under irradiation treatment, AuPPR-HIF-1α siRNA significantly enhanced apoptosis of NPC cells by 33.76 ± 3.65 %, when compared to the control and simple AuPPR group (22.5 ± 4.16 %, p < 0.01). Furthermore, cell cycle was significantly blocked in the sub-G1 phase in AuPPR-HIF-1α siRNA radiotherapy groups, indicating severe cell damage.
Conclusion: This study has demonstrated that AuPPR-HIF-1α siRNA is effective in improving the radiosensitivity of nasopharyngeal carcinoma cells under hypoxia, and therefore can potentially be used to improve the radiotherapy of this carcinoma
{"title":"Effect of gold nanocomposite bearing HIF-1α siRNA on radiotherapy in nasopharyngeal carcinoma cell","authors":"Haosheng Zhang, Fangzheng Zhou","doi":"10.4314/tjpr.v22i10.10","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.10","url":null,"abstract":"Purpose: To investigate the effect of gold nanocomposite carrying hypoxia-inducible factor-1α (HIF-1α) siRNA on radiosensitivity of nasopharynx cancer (NPC) cells.
 Methods: Gold nanocomposite (AuNRs-(PEI-PEG)/RGD) or (AuPPR) was first synthesized and its cytotoxicity was evaluated. Then, the expression of HIF-1α in hypoxic NPC cells was assessed. In addition, the radiation sensitivity of AuPPR bearing HIF-1α siRNA on the cells was examined under xray exposure.
 Result: Gold nanocomposite (AuPPR) carrying HIF-1α siRNA (AuPPR-HIF-1α siRNA) significantly down-regulated HIF-1α expression. Under irradiation treatment, AuPPR-HIF-1α siRNA significantly enhanced apoptosis of NPC cells by 33.76 ± 3.65 %, when compared to the control and simple AuPPR group (22.5 ± 4.16 %, p < 0.01). Furthermore, cell cycle was significantly blocked in the sub-G1 phase in AuPPR-HIF-1α siRNA radiotherapy groups, indicating severe cell damage.
 Conclusion: This study has demonstrated that AuPPR-HIF-1α siRNA is effective in improving the radiosensitivity of nasopharyngeal carcinoma cells under hypoxia, and therefore can potentially be used to improve the radiotherapy of this carcinoma","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"90 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jia Wang, Yan Li, Yangsong Ou, Wan Qin, Wukui Huang, Cengceng Lu, Rongyan Ma, Rui Han, Hu Han
Purpose: To investigate the biological function and mechanisms of circPDSS1 in triggering malignant progression of renal cell carcinoma (RCC).
Methods: Quantitative real-time polymerase chain reaction (qRT-PCR) was conducted to determine circPDSS1 levels in 50 pairs of RCC and para-cancerous tissues. The relationship between circPDSS1 level and pathological indices in RCC patients was analyzed, while the in vitro effect of circPDSS1 in regulating RCC proliferation was assessed using cell counting kit-8 (CCK-8), colony formation and 5- ethynyl-2’- deoxyuridine (EdU) assay. The sponge effect of circPDSS1 on miR-182-5p was examined by bioinformatics analysis and dual- luciferase reporter assay, while their involvement in mediating malignant progression of RCC was analyzed using rescue experiments. In vivo, the influence of circPDSS1 on RCC growth was determined by establishing a xenograft model in nude mice. Thereafter, RCC tissues were harvested from mice to assess relative levels of miR-182-5p and Ki-67.
Results: CircPDSS1 was highly expressed in RCC tissues (p < 0.05). A high level of circPDSS1 correlated with advanced tumor staging and low overall survival. Knockdown of circPDSS1 inhibited RCC cell proliferation, and CircPDSS1 sponged and negatively regulated miR-182-5p (p < 0.05). MiR182-5p was able to abolish regulatory effect of circPDSS1 on malignant proliferative potential in RCC cells. In nude mice bearing RCC, in vivo knockdown of circPDSS1 slowed down tumor growth and decreased positive expression of Ki-67 in tumor tissues (p < 0.05).
Conclusion: CircPDSS1 predicts tumor stage and prognosis in RCC patients. It triggers malignant progression of RCC through sponging of miR-182-5p.
{"title":"CircPDSS1 accelerates malignant progression of renal cell carcinoma through sponging of miR-182-5p","authors":"Jia Wang, Yan Li, Yangsong Ou, Wan Qin, Wukui Huang, Cengceng Lu, Rongyan Ma, Rui Han, Hu Han","doi":"10.4314/tjpr.v22i10.3","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.3","url":null,"abstract":"Purpose: To investigate the biological function and mechanisms of circPDSS1 in triggering malignant progression of renal cell carcinoma (RCC).
 Methods: Quantitative real-time polymerase chain reaction (qRT-PCR) was conducted to determine circPDSS1 levels in 50 pairs of RCC and para-cancerous tissues. The relationship between circPDSS1 level and pathological indices in RCC patients was analyzed, while the in vitro effect of circPDSS1 in regulating RCC proliferation was assessed using cell counting kit-8 (CCK-8), colony formation and 5- ethynyl-2’- deoxyuridine (EdU) assay. The sponge effect of circPDSS1 on miR-182-5p was examined by bioinformatics analysis and dual- luciferase reporter assay, while their involvement in mediating malignant progression of RCC was analyzed using rescue experiments. In vivo, the influence of circPDSS1 on RCC growth was determined by establishing a xenograft model in nude mice. Thereafter, RCC tissues were harvested from mice to assess relative levels of miR-182-5p and Ki-67.
 Results: CircPDSS1 was highly expressed in RCC tissues (p < 0.05). A high level of circPDSS1 correlated with advanced tumor staging and low overall survival. Knockdown of circPDSS1 inhibited RCC cell proliferation, and CircPDSS1 sponged and negatively regulated miR-182-5p (p < 0.05). MiR182-5p was able to abolish regulatory effect of circPDSS1 on malignant proliferative potential in RCC cells. In nude mice bearing RCC, in vivo knockdown of circPDSS1 slowed down tumor growth and decreased positive expression of Ki-67 in tumor tissues (p < 0.05).
 Conclusion: CircPDSS1 predicts tumor stage and prognosis in RCC patients. It triggers malignant progression of RCC through sponging of miR-182-5p.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"91 7","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To investigate the safety and efficacy of salvianolate injection in preventing deep vein thrombosis (DVT) following total hip replacement.
Methods: A total of 114 patients who underwent total hip replacement at Department of Trauma, Fengfeng General Hospital of North China Medical and Health Group, Handan City, China from March 2019 to March 2022 were enrolled. Patients were randomly divided into study group (n = 57) and control group (n = 57). The control group received conventional treatment (low molecular weight heparin) while the study group was administered salvianolate injection combined with conventional treatment. Incidence of deep vein thrombosis (DVT) at 7 and 14 days after surgery, platelet function indices, including platelet count, glycoprotein Ⅱb/Ⅲa (GPⅡb/Ⅲa), and CD62P, coagulation function indices (prothrombin time (PT), fibrinogen (FIB) and D-dimer), and hemodynamics indices, viz, peak blood flow velocity (Vp) and average velocity (Va) were investigated and compared.
Results: Incidence of DVT was 1.75 % (1/57) at 7 days and 5.26 % (3/57) at 14 days in the study group, and 5.26 % (3/57) at 7 days and 17.54 % (10/57) at 14 days in control group. Incidence of DVT in the study group was significantly reduced compared to control group 14 days after surgery (p < 0.05). Also, the study group had significantly lower visual analog scale (VAS) scores at 7 days and 1 month after surgery compared to control group (p < 0.05). Platelet count, GPⅡb/Ⅲa, and CD62P in the study group were significantly lower than in control group (p < 0.05).
Conclusion: Salvianolate injection significantly prevents DVT after total hip replacement, improves hemodynamics, and coagulation function, and thus contributes to recovery of hip function. Further clinical trials are, however, required to validate these findings.
{"title":"Safety and efficacy of salvianolate injection in preventing deep vein thrombosis after total hip replacement","authors":"Xiaoning Liu, Yang Ju, Xiaoyong Yin, Hui Yang, Shoujiang Han, Deming Kong, Hongbo Zhao","doi":"10.4314/tjpr.v22i10.20","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.20","url":null,"abstract":"Purpose: To investigate the safety and efficacy of salvianolate injection in preventing deep vein thrombosis (DVT) following total hip replacement.
 Methods: A total of 114 patients who underwent total hip replacement at Department of Trauma, Fengfeng General Hospital of North China Medical and Health Group, Handan City, China from March 2019 to March 2022 were enrolled. Patients were randomly divided into study group (n = 57) and control group (n = 57). The control group received conventional treatment (low molecular weight heparin) while the study group was administered salvianolate injection combined with conventional treatment. Incidence of deep vein thrombosis (DVT) at 7 and 14 days after surgery, platelet function indices, including platelet count, glycoprotein Ⅱb/Ⅲa (GPⅡb/Ⅲa), and CD62P, coagulation function indices (prothrombin time (PT), fibrinogen (FIB) and D-dimer), and hemodynamics indices, viz, peak blood flow velocity (Vp) and average velocity (Va) were investigated and compared.
 Results: Incidence of DVT was 1.75 % (1/57) at 7 days and 5.26 % (3/57) at 14 days in the study group, and 5.26 % (3/57) at 7 days and 17.54 % (10/57) at 14 days in control group. Incidence of DVT in the study group was significantly reduced compared to control group 14 days after surgery (p < 0.05). Also, the study group had significantly lower visual analog scale (VAS) scores at 7 days and 1 month after surgery compared to control group (p < 0.05). Platelet count, GPⅡb/Ⅲa, and CD62P in the study group were significantly lower than in control group (p < 0.05).
 Conclusion: Salvianolate injection significantly prevents DVT after total hip replacement, improves hemodynamics, and coagulation function, and thus contributes to recovery of hip function. Further clinical trials are, however, required to validate these findings.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"88 5","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685273","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To determine the effect of Hederagenin (Hed) on rheumatoid arthritis (RA) in a cell model, and to elucidate the mechanism of action of Hed.
Methods: MTT, EDU, and Immunoblot assays were used to determine the effects of Hed on the viability of fibroblast-like synovial cells, while the effects of Hed on inflammation were examined by enzymelinked immunosorbent assay (ELISA) and immunoblot assay. The influence of Hed on cell motility angiogenesis was evaluated by Transwell and tube formation assays, while immunoblot analysis was used to determine the mechanism of action of Hed.
Results: Hed inhibited the viability of RA-FLS cells and suppressed the inflammation of RA-FLS cells (p < 0.05). Furthermore, Hed suppressed the migration and angiogenesis of RA-FLSl cells, as well as regulated MAPK pathway (p < 0.05).
Conclusion: Hed inhibits the proliferation, angiogenesis and inflammation of fibroblast-like synovial cells in RA by regulating MAPK pathway. Therefore, Hed is a drug for the treatment of RA, However, in vivo studies to validate these findings are recommended
{"title":"Hederagenin inhibits proliferation, angiogenesis and inflammation of fibroblast-like synovial cells in rheumatoid arthritis","authors":"Ping Wang, Junli Yang, Xiaomeng Zhang","doi":"10.4314/tjpr.v22i10.4","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.4","url":null,"abstract":"Purpose: To determine the effect of Hederagenin (Hed) on rheumatoid arthritis (RA) in a cell model, and to elucidate the mechanism of action of Hed.
 Methods: MTT, EDU, and Immunoblot assays were used to determine the effects of Hed on the viability of fibroblast-like synovial cells, while the effects of Hed on inflammation were examined by enzymelinked immunosorbent assay (ELISA) and immunoblot assay. The influence of Hed on cell motility angiogenesis was evaluated by Transwell and tube formation assays, while immunoblot analysis was used to determine the mechanism of action of Hed.
 Results: Hed inhibited the viability of RA-FLS cells and suppressed the inflammation of RA-FLS cells (p < 0.05). Furthermore, Hed suppressed the migration and angiogenesis of RA-FLSl cells, as well as regulated MAPK pathway (p < 0.05).
 Conclusion: Hed inhibits the proliferation, angiogenesis and inflammation of fibroblast-like synovial cells in RA by regulating MAPK pathway. Therefore, Hed is a drug for the treatment of RA, However, in vivo studies to validate these findings are recommended","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"91 6","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685457","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To isolate, characterize, and investigate the hepatoprotective effect of phyto-constituents from fruits of Cordia obliqua Wild in paracetamol-induced hepatotoxicity in Wistar rats.
Methods: Ethanol and aqueous extracts of C. obliqua fruits were screened for phytochemicals. The extracts were subjected to column chromatography and preparative thin-layer chromatography (TLC) to isolate four novel compounds. Compounds were characterized using infrared spectroscopy (IR), mass spectroscopy (MS), as well as 1H and 13C nuclear magnetic resonance (NMR). The isolated compounds were assessed for acute toxicity, in vivo hepatoprotective and antioxidant potential (dose: 5 mg/kg) in paracetamol-induced (75 mg/kg) hepatotoxicity through oral route in Wistar rats.
Results: Phytochemical analysis of ethanol (COE) indicated the presence of fatty acids, anthraquinones, glycosides, saponins, alkaloids, tannins, flavonoids, coumarins, phenolics, triterpenes, and sterols. Compounds A, B, and C were identified from COE. Treatment at 50 mg/kg significantly reduced aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGTP), and total bilirubin (TB), as well as increased total protein and total alkalinity levels in serum compared to the positive control. Liver histo-architecture showed improvements compared to the positive control, indicating hepatic protection.
Conclusion: The isolated compounds (A, B and C) from COE exhibit hepatoprotective effects attributed to flavonoids and phenolics with free radical scavenging properties. Further research is needed to identify key mechanisms responsible for hepatoprotective effects.
{"title":"Isolation, characterization, structural elucidation and in vivo hepatoprotective studies of phytoconstituents obtained from the fruits of <i>Cordia obliqua</i> Willd","authors":"G. Tharun Babu, S. Sivakrishnan, J.V.C. Sharma","doi":"10.4314/tjpr.v22i10.15","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.15","url":null,"abstract":"Purpose: To isolate, characterize, and investigate the hepatoprotective effect of phyto-constituents from fruits of Cordia obliqua Wild in paracetamol-induced hepatotoxicity in Wistar rats.
 Methods: Ethanol and aqueous extracts of C. obliqua fruits were screened for phytochemicals. The extracts were subjected to column chromatography and preparative thin-layer chromatography (TLC) to isolate four novel compounds. Compounds were characterized using infrared spectroscopy (IR), mass spectroscopy (MS), as well as 1H and 13C nuclear magnetic resonance (NMR). The isolated compounds were assessed for acute toxicity, in vivo hepatoprotective and antioxidant potential (dose: 5 mg/kg) in paracetamol-induced (75 mg/kg) hepatotoxicity through oral route in Wistar rats.
 Results: Phytochemical analysis of ethanol (COE) indicated the presence of fatty acids, anthraquinones, glycosides, saponins, alkaloids, tannins, flavonoids, coumarins, phenolics, triterpenes, and sterols. Compounds A, B, and C were identified from COE. Treatment at 50 mg/kg significantly reduced aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma-glutamyl transferase (GGTP), and total bilirubin (TB), as well as increased total protein and total alkalinity levels in serum compared to the positive control. Liver histo-architecture showed improvements compared to the positive control, indicating hepatic protection.
 Conclusion: The isolated compounds (A, B and C) from COE exhibit hepatoprotective effects attributed to flavonoids and phenolics with free radical scavenging properties. Further research is needed to identify key mechanisms responsible for hepatoprotective effects.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"91 3","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685460","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Caifeng Jia, Sen Zhang, Wenpan Li, Chun Chu, Haiyang Hu, Mingxia Wang, Dawei Chen
Purpose: To investigate a novel co-delivery system using nanostructured lipid carriers (NLCs) for simultaneous administration of two potent anti-cancer drugs, combretastatin A-4 (CA-4) and docetaxel (DTX), against tumor cells and vasculature.
Methods: The CA-4 and DTX co-loaded NLCs (C-D-NLC) were formulated and investigated for physical properties, stability, and drug release. Safety and efficacy of C-D-NLC were investigated on Lewis Lung Carcinoma (LLC) tumor cells in vitro and in vivo using cytotoxicity and anti-tumor assays. The pharmacokinetics of CA-4 and DTX in rats after intravenous injection of C-D-NLC were also studied to evaluate potential drug interactions.
Results: The C-D-NLC was successfully prepared with a spherical shape, mean size of 130 nm, negative charge, high encapsulation efficiency and drug loading of 94.89, 88.16, 2.44, and 4.52 for DTX and CA-4, respectively. Also, C-D-NLC had a significant inhibitory effect on LLC cells, superior to a single drug or solution group. Combretastatin A4 did not affect the pharmacokinetics of DTX, but combretastatin–docetaxel nanostructured lipid carriers (C-D-NLC) reduced plasma clearance of CA-4 and DTX, prolonged half-life, mean residence time, and increased area under concentration curves (AUC) values. Furthermore, combretastatin–docetaxel nanostructured lipid carriers (C-D-NLC) inhibited the growth of LLC tumors in mice and reduced drug toxicity.
Conclusion: Combretastatin–docetaxel nanostructured lipid carriers (C-D-NLC) sustain drug release and enhance tumor growth inhibition of CA-4 and DTX by targeting both tumor cells and vasculature. The co-delivery system prolongs drug circulation compared to solution administration. Thus, nanostructured lipid carriers (NLCs) with dual drug loading may be a promising strategy for clinical combination chemotherapy in future.
{"title":"Co-delivery of combretastatin A4 and docetaxel with pegylated nanostructured lipid carriers in tumor cells","authors":"Caifeng Jia, Sen Zhang, Wenpan Li, Chun Chu, Haiyang Hu, Mingxia Wang, Dawei Chen","doi":"10.4314/tjpr.v22i10.2","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.2","url":null,"abstract":"Purpose: To investigate a novel co-delivery system using nanostructured lipid carriers (NLCs) for simultaneous administration of two potent anti-cancer drugs, combretastatin A-4 (CA-4) and docetaxel (DTX), against tumor cells and vasculature.
 Methods: The CA-4 and DTX co-loaded NLCs (C-D-NLC) were formulated and investigated for physical properties, stability, and drug release. Safety and efficacy of C-D-NLC were investigated on Lewis Lung Carcinoma (LLC) tumor cells in vitro and in vivo using cytotoxicity and anti-tumor assays. The pharmacokinetics of CA-4 and DTX in rats after intravenous injection of C-D-NLC were also studied to evaluate potential drug interactions.
 Results: The C-D-NLC was successfully prepared with a spherical shape, mean size of 130 nm, negative charge, high encapsulation efficiency and drug loading of 94.89, 88.16, 2.44, and 4.52 for DTX and CA-4, respectively. Also, C-D-NLC had a significant inhibitory effect on LLC cells, superior to a single drug or solution group. Combretastatin A4 did not affect the pharmacokinetics of DTX, but combretastatin–docetaxel nanostructured lipid carriers (C-D-NLC) reduced plasma clearance of CA-4 and DTX, prolonged half-life, mean residence time, and increased area under concentration curves (AUC) values. Furthermore, combretastatin–docetaxel nanostructured lipid carriers (C-D-NLC) inhibited the growth of LLC tumors in mice and reduced drug toxicity.
 Conclusion: Combretastatin–docetaxel nanostructured lipid carriers (C-D-NLC) sustain drug release and enhance tumor growth inhibition of CA-4 and DTX by targeting both tumor cells and vasculature. The co-delivery system prolongs drug circulation compared to solution administration. Thus, nanostructured lipid carriers (NLCs) with dual drug loading may be a promising strategy for clinical combination chemotherapy in future.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"90 9","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685464","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To investigate the therapeutic effect of cisatracurium, (a neuromuscular blocking agent) in the treatment of acute respiratory distress syndrome (ARDS).
Methods: A total of 94 ARDS patients admitted to The Third People's Hospital of Honghe Hani and Yi Autonomous Prefecture ICU from March 2020 to December 2021 were randomly assigned to study and control groups (47 patients each). Both groups received mechanical ventilation, but the study group also received continuous intravenous cisatracurium for 48 h. Health parameters, such as blood gas levels, respiratory mechanics, duration of stay in intensive care unit ICU), mortality rate, and the occurrence of complications, were monitored at 3, 6, and 12 months after treatment.
Results: The study group showed significant improvements compared to control group. Study group also had reduced duration of mechanical ventilation, duration of ICU stay, ICU mortality rate, and incidence of complications (p < 0.05). There were no significant differences in pre-treatment health parameters, but post-treatment, study group had significantly higher levels of blood gas levels and improved lung function (p < 0.05). Study group also had lower scores of illness severity and reduced total mortality rate at 3, 6, and 12 months (p < 0.05).
Conclusion: Administering cisatracurium reduces mechanical ventilation, duration of ICU stay and mortality rate, as well as improves lung function in ARDS patients. Future research involving larger sample size, and takes into consideration regional/environmental differences, is required to validate these findings for reliability.
{"title":"Therapeutic effect of cisatracurium in patients with acute respiratory distress syndrome","authors":"Yanping Li, Jiping Li, Zhongmei Ni","doi":"10.4314/tjpr.v22i10.19","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.19","url":null,"abstract":"Purpose: To investigate the therapeutic effect of cisatracurium, (a neuromuscular blocking agent) in the treatment of acute respiratory distress syndrome (ARDS).
 Methods: A total of 94 ARDS patients admitted to The Third People's Hospital of Honghe Hani and Yi Autonomous Prefecture ICU from March 2020 to December 2021 were randomly assigned to study and control groups (47 patients each). Both groups received mechanical ventilation, but the study group also received continuous intravenous cisatracurium for 48 h. Health parameters, such as blood gas levels, respiratory mechanics, duration of stay in intensive care unit ICU), mortality rate, and the occurrence of complications, were monitored at 3, 6, and 12 months after treatment.
 Results: The study group showed significant improvements compared to control group. Study group also had reduced duration of mechanical ventilation, duration of ICU stay, ICU mortality rate, and incidence of complications (p < 0.05). There were no significant differences in pre-treatment health parameters, but post-treatment, study group had significantly higher levels of blood gas levels and improved lung function (p < 0.05). Study group also had lower scores of illness severity and reduced total mortality rate at 3, 6, and 12 months (p < 0.05).
 Conclusion: Administering cisatracurium reduces mechanical ventilation, duration of ICU stay and mortality rate, as well as improves lung function in ARDS patients. Future research involving larger sample size, and takes into consideration regional/environmental differences, is required to validate these findings for reliability.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"89 6","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685383","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Purpose: To study the influence of microRNA-138 (miR-138) on the migration and invasion of cervical cancer cells, and the underlying mechanism.
Methods: Fifteen cervical carcinoma subjects were enrolled in the study. Control group comprised cervical epithelial cell line (End1/E6E7) while cervical cancer group was human cervical squamous cell carcinoma cell line c33a. Both were cultured routinely without any treatment. In miR-138 overexpression group, cells were cultured in progeny of human cervical squamous carcinoma cell line c33a infected with miR-138 gene overexpression lentivirus. Expression levels of miR-138 in excised cervical cancer tissues were determined using qPCR. Cell proliferation was determined with CCK8 assay. Immunoblotting was utilized to assay protein expression levels. Quantitative real-time polymerase chain reaction (qRT-PCR) was used to determine mRNA expression levels, while cell migration and invasion were assessed by Transwell method.
Results: There was significant down-regulation of miR-138 expression in cervical cancer tissue, relative to nearby tissues (p < 0.05). In miR-138 overexpression group, cell proliferation, number of migrated and invaded cells were significantly reduced, relative to corresponding levels in cervical cancer cells. There were significantly higher expression levels of apoptosis-related proteins FAS, Bax and FasL in miR-138 overexpression group than in cervical cancer cells, while Bcl-2 was significantly downregulated, relative to cervical cancer group (p < 0.05). In cervical cancer cells, mRNA and protein levels of SIRT1 and HIF-1α were significantly up-regulated, relative to corresponding control, but levels of HIF1α and miR-138 were significantly reduced in overexpression group when compared to cervical cancer group (p < 0.05).
Conclusion: Up-regulating miR-138 in cervical cancer cells reduces HIF-1α through inhibition of SIRT1 signaling, resulting in suppression of multiplication, migration and invasion of cervical cancer cells, while enhancing apoptotic changes.
{"title":"Effect of miR-138 on migration and invasion of cervical cancer cells, and the underlying mechanism","authors":"Yanxi Li, Jun Peng, Yong Huang, Yichun Man, Yaqi Li, Ping Chen, Erqing Peng","doi":"10.4314/tjpr.v22i10.6","DOIUrl":"https://doi.org/10.4314/tjpr.v22i10.6","url":null,"abstract":"Purpose: To study the influence of microRNA-138 (miR-138) on the migration and invasion of cervical cancer cells, and the underlying mechanism.
 Methods: Fifteen cervical carcinoma subjects were enrolled in the study. Control group comprised cervical epithelial cell line (End1/E6E7) while cervical cancer group was human cervical squamous cell carcinoma cell line c33a. Both were cultured routinely without any treatment. In miR-138 overexpression group, cells were cultured in progeny of human cervical squamous carcinoma cell line c33a infected with miR-138 gene overexpression lentivirus. Expression levels of miR-138 in excised cervical cancer tissues were determined using qPCR. Cell proliferation was determined with CCK8 assay. Immunoblotting was utilized to assay protein expression levels. Quantitative real-time polymerase chain reaction (qRT-PCR) was used to determine mRNA expression levels, while cell migration and invasion were assessed by Transwell method.
 Results: There was significant down-regulation of miR-138 expression in cervical cancer tissue, relative to nearby tissues (p < 0.05). In miR-138 overexpression group, cell proliferation, number of migrated and invaded cells were significantly reduced, relative to corresponding levels in cervical cancer cells. There were significantly higher expression levels of apoptosis-related proteins FAS, Bax and FasL in miR-138 overexpression group than in cervical cancer cells, while Bcl-2 was significantly downregulated, relative to cervical cancer group (p < 0.05). In cervical cancer cells, mRNA and protein levels of SIRT1 and HIF-1α were significantly up-regulated, relative to corresponding control, but levels of HIF1α and miR-138 were significantly reduced in overexpression group when compared to cervical cancer group (p < 0.05).
 Conclusion: Up-regulating miR-138 in cervical cancer cells reduces HIF-1α through inhibition of SIRT1 signaling, resulting in suppression of multiplication, migration and invasion of cervical cancer cells, while enhancing apoptotic changes.","PeriodicalId":23347,"journal":{"name":"Tropical Journal of Pharmaceutical Research","volume":"88 6","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135685391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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