Mycobacterium smegmatis and Mycobacterium avium offer an advantage in examining tuberculosis-like effects and host immune defense. Therefore, the study aims to examine the effect of ursolic acid (UA) on the host immune system by analyzing cytokines concentration, such as TNF-α, IL-6, IL-1β, and nitrite oxide produced by murine macrophages infected with Mycobacterium smegmatis and Mycobacterium avium. Femurs of female C57BL/6 mice aged 6–8 weeks were used to culture the Bone marrow-derived macrophages (BMDM). On day 10, BMDM was infected with Mycobacterium smegmatis and Mycobacterium avium using a multiplicity of infection (MOI) amounting to 8:1, then TNF-α, IL-6, and IL-1β were analyzed using ELISA and nitrite oxide with Griess reagent. The results showed that UA decreased the production of three respective pro-inflammatory cytokines used in the study, both in BMDM infected by Mycobacterium smegmatis and Mycobacterium avium. For TNF-α, the reduction was nearly 65%-90% compared to the control. The decrease in the production of IL-6 occurred from 2700 pg/ml to 750 pg/ml for BMDM infected with Mycobacterium smegmatis, while the reduction was more significant in those infected using Mycobacterium avium with approximately 150 pg/ml compared to the control. Moreover, UA reduced by over 90% of IL-1β and this result was in line with the reduction of nitrite. UA decreases the production of pro-inflammatory cytokines such as TNF-α, IL-6, IL-1β, and nitrite. This result is preliminary but supports further study on the role of UA in immune defense from pathogenic and non-pathogenic mycobacterial infections.
{"title":"Comparing Responses of Ursolic Acid in Murine Macrophages Infected with Mycobacterium smegmatis and Mycobacterium avium","authors":"D. Pitaloka, M. Jihadah","doi":"10.22146/ijp.3507","DOIUrl":"https://doi.org/10.22146/ijp.3507","url":null,"abstract":"Mycobacterium smegmatis and Mycobacterium avium offer an advantage in examining tuberculosis-like effects and host immune defense. Therefore, the study aims to examine the effect of ursolic acid (UA) on the host immune system by analyzing cytokines concentration, such as TNF-α, IL-6, IL-1β, and nitrite oxide produced by murine macrophages infected with Mycobacterium smegmatis and Mycobacterium avium. Femurs of female C57BL/6 mice aged 6–8 weeks were used to culture the Bone marrow-derived macrophages (BMDM). On day 10, BMDM was infected with Mycobacterium smegmatis and Mycobacterium avium using a multiplicity of infection (MOI) amounting to 8:1, then TNF-α, IL-6, and IL-1β were analyzed using ELISA and nitrite oxide with Griess reagent. The results showed that UA decreased the production of three respective pro-inflammatory cytokines used in the study, both in BMDM infected by Mycobacterium smegmatis and Mycobacterium avium. For TNF-α, the reduction was nearly 65%-90% compared to the control. The decrease in the production of IL-6 occurred from 2700 pg/ml to 750 pg/ml for BMDM infected with Mycobacterium smegmatis, while the reduction was more significant in those infected using Mycobacterium avium with approximately 150 pg/ml compared to the control. Moreover, UA reduced by over 90% of IL-1β and this result was in line with the reduction of nitrite. UA decreases the production of pro-inflammatory cytokines such as TNF-α, IL-6, IL-1β, and nitrite. This result is preliminary but supports further study on the role of UA in immune defense from pathogenic and non-pathogenic mycobacterial infections.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87171165","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}
A. Dogara, A. A. Lema, H. Hama, S. Hamad, Nor Hasima Mahmod Mohammad, Mohammad Moneruzzaman Khandaker, Wandayi Emmanuel Amlabu
The Burseraceae family consists of 18 genera and 540 species. Boswellia dalzielii is a medicinal plant used in tropical and subtropical areas for the treatment and management of various ailments. Despite the medicinal value of B. dalzielii, there is no comprehensive documentation. The study aimed to review the ethnopharmacology, biological evaluation and chemical composition of B. dalzielii. Scopus, Web of Science, BioMed Central, Science Direct, PubMed, Springer Link, and Google Scholar were searched to find published articles. The results showed that the leaves, stem bark, and root of B. dalzielii have been traditionally used in Nigeria, Cameroon, Burkina Faso, Benin, Sudan, and Guinee for the treatment and management of antirheumatic, antispasmodic, analgesic, antiseptic, hypotensive, malarial mental illness, ulcer, pain, and fever. It is also found that leaves, stem bark, and root have antioxidant, antibacterial, antifungal, and antimalarial properties with stembark having the highest activity. Chemically, it was revealed the leaf has high contents of monoterpenes hydrocarbons with alpha-pinene as the major compound. The species were largely studied in vitro, according to the literature survey. A well-designed clinical experiment is required to obtain conclusive evidence on the efficacy of stembark. The standard dose and safety of the stembark should be established.
刺虫科有18属540种。Boswellia dalzielii是热带和亚热带地区用于治疗和管理各种疾病的药用植物。尽管dalzielii具有药用价值，但没有全面的文献记载。本文综述了黄刺莲的民族药理学、生物学评价及化学成分。检索了Scopus、Web of Science、BioMed Central、Science Direct、PubMed、Springer Link和Google Scholar来查找已发表的文章。结果表明，在尼日利亚、喀麦隆、布基纳法索、贝宁、苏丹和几内亚，达尔齐莱叶、茎皮和根传统上用于治疗和管理抗风湿、抗痉挛、镇痛、防腐、降压、疟疾性精神疾病、溃疡、疼痛和发烧。叶、茎、皮、根均具有抗氧化、抗菌、抗真菌、抗疟等作用，其中以茎叶活性最高。化学成分分析表明，黄芪叶中单萜化合物含量较高，主要成分为α -蒎烯。根据文献调查，该物种主要是在体外研究的。需要精心设计的临床实验来获得结论性证据。应建立登机的标准剂量和安全性。
{"title":"Ethnopharmacology, Biological evaluation and Chemical composition of Boswellia dalzielii Hutch: A Review","authors":"A. Dogara, A. A. Lema, H. Hama, S. Hamad, Nor Hasima Mahmod Mohammad, Mohammad Moneruzzaman Khandaker, Wandayi Emmanuel Amlabu","doi":"10.22146/ijp.4279","DOIUrl":"https://doi.org/10.22146/ijp.4279","url":null,"abstract":"The Burseraceae family consists of 18 genera and 540 species. Boswellia dalzielii is a medicinal plant used in tropical and subtropical areas for the treatment and management of various ailments. Despite the medicinal value of B. dalzielii, there is no comprehensive documentation. The study aimed to review the ethnopharmacology, biological evaluation and chemical composition of B. dalzielii. Scopus, Web of Science, BioMed Central, Science Direct, PubMed, Springer Link, and Google Scholar were searched to find published articles. The results showed that the leaves, stem bark, and root of B. dalzielii have been traditionally used in Nigeria, Cameroon, Burkina Faso, Benin, Sudan, and Guinee for the treatment and management of antirheumatic, antispasmodic, analgesic, antiseptic, hypotensive, malarial mental illness, ulcer, pain, and fever. It is also found that leaves, stem bark, and root have antioxidant, antibacterial, antifungal, and antimalarial properties with stembark having the highest activity. Chemically, it was revealed the leaf has high contents of monoterpenes hydrocarbons with alpha-pinene as the major compound. The species were largely studied in vitro, according to the literature survey. A well-designed clinical experiment is required to obtain conclusive evidence on the efficacy of stembark. The standard dose and safety of the stembark should be established.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86168862","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}
Food and drug control authorities in each country have issued warnings about the toxic effect potential of using commonly consumed traditional medicines. The safety assurance, standardization, and market regulation of herbal medicines being sold need to be determined. This study's goal is to investigate the acute and subchronic toxicity of cold-processed snakehead fish (Channa striata) flesh. In-vivo rats models were given dosages of 350, 1400, and 5600 mg/kg processed snakehead fish (SF) and were monitored for toxic symptoms and mortality for 14 days. Meanwhile, regarding subchronic toxicity, doses of 350, 700, and 1400 mg/kg SF were administered orally for 28 days. Afterward, the animal subjects were sacrificed for histopathological, hematological, and biochemical examinations. There were no evidence of toxicity or mortality in rats during the acute examination, which lasted 14 days. The subchronic toxicity results showed no significant changes in most of the hematological, biochemical, and histological profiles of the organs. Some changes observed in blood biochemistry and relative organ weight were assumed as a temporary effect and not a sign of toxicity. The overall results showed that the SF was non-toxic up to 1400 mg/kg, which can be considered a safe dose for the application of health supplement raw materials.
{"title":"Oral acute and subchronic (28-day) toxicity studies of snakehead fish (Channa striata)","authors":"H. Sasongko","doi":"10.22146/ijp.3905","DOIUrl":"https://doi.org/10.22146/ijp.3905","url":null,"abstract":"Food and drug control authorities in each country have issued warnings about the toxic effect potential of using commonly consumed traditional medicines. The safety assurance, standardization, and market regulation of herbal medicines being sold need to be determined. This study's goal is to investigate the acute and subchronic toxicity of cold-processed snakehead fish (Channa striata) flesh. In-vivo rats models were given dosages of 350, 1400, and 5600 mg/kg processed snakehead fish (SF) and were monitored for toxic symptoms and mortality for 14 days. Meanwhile, regarding subchronic toxicity, doses of 350, 700, and 1400 mg/kg SF were administered orally for 28 days. Afterward, the animal subjects were sacrificed for histopathological, hematological, and biochemical examinations. There were no evidence of toxicity or mortality in rats during the acute examination, which lasted 14 days. The subchronic toxicity results showed no significant changes in most of the hematological, biochemical, and histological profiles of the organs. Some changes observed in blood biochemistry and relative organ weight were assumed as a temporary effect and not a sign of toxicity. The overall results showed that the SF was non-toxic up to 1400 mg/kg, which can be considered a safe dose for the application of health supplement raw materials.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81464148","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}
The excessive oxidative processes and the lack of cellular antioxidative mechanisms are significantly observed in diabetes. In addition, long-term medication required for the treatment might harm the hepatic tissues. This study evaluated the selected pharmacognostic characters, antioxidant activities, total phenolic content, and the hepatic safety of a polyherbal formulation containing seven plant constituents used by Klinik Wisata Kesehatan Jamu Kalibakung, Tegal, Indonesia, to treat diabetes patients. The pharmacognostic properties of the formulation were characterized according to the WHO quality control methods for herbal materials. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH RSA), ferric reducing antioxidant power (FRAP), and total phenolic content (TPC) were evaluated as per the standard method. The effect of formulation on the hepatic HepG2 cells was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay. The pharmacognostic properties of the formulation specified as follow: foreign matters (1.32±0.05%), loss on drying (11.50±0.07%), total ash (5.68±0.07%), acid-insoluble ash (0.94±0.04%), water-soluble extractable (18.22±0.60%), and ethanol-soluble extractable (16.90±0.77%). The ethanol extract showed a superior DPPH RSA (960.70±2.58 mM Trolox equivalent (TE)/ g dry weight (DW)), FRAP (1112.69±8.39 mM TE/g DW), and TPC (1768.40±32.40 mg gallic acid equivalent (GAE)/g DW) over its water counterpart. However, the water extract was safer for HepG2 cells than the ethanol one, with the IC50 values of 218.25±14.03 and 40.24±3.53 µg/ml, respectively. This study set the pharmacognostic standards for an antidiabetic polyherbal formulation with excellent antioxidant activities, in which its traditional use as a decoction was safe for the hepatic cells.
过度的氧化过程和缺乏细胞抗氧化机制在糖尿病中被显著观察到。此外，治疗所需的长期药物可能会损害肝组织。本研究评价了Klinik Wisata Kesehatan Jamu Kalibakung, Tegal, Indonesia用于治疗糖尿病患者的含有七种植物成分的多草药配方的生药学特性、抗氧化活性、总酚含量和肝脏安全性。按照世界卫生组织中药材质量控制方法对制剂的生药学性质进行了表征。按照标准方法测定了2,2-二苯基-1-苦味酰肼基自由基清除能力(DPPH RSA)、铁还原抗氧化能力(FRAP)和总酚含量(TPC)。采用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑(MTT)还原法测定制剂对HepG2细胞的影响。其生药学性质为:杂质(1.32±0.05%)、干燥损失(11.50±0.07%)、总灰分(5.68±0.07%)、酸不溶灰分(0.94±0.04%)、水溶性可提物(18.22±0.60%)、醇溶性可提物(16.90±0.77%)。乙醇提取物的DPPH RSA(960.70±2.58 mM Trolox当量(TE)/ g干重(DW))、FRAP(1112.69±8.39 mM TE/g DW)和TPC(1768.40±32.40 mg没食子酸当量(GAE)/g DW)均优于水提取物。水提物对HepG2细胞的IC50值分别为218.25±14.03µg/ml和40.24±3.53µg/ml，比乙醇提物对HepG2细胞更安全。本研究确定了抗氧化活性良好的抗糖尿病复方制剂的生药学标准，其传统煎剂对肝细胞是安全的。
{"title":"THE PHARMACOGNOSTIC STANDARDS, ANTIOXIDANT ACTIVITY, AND HEPATIC SAFETY PROFILE OF AN INDONESIAN ANTIDIABETIC POLYHERBAL FORMULATION","authors":"D. Hartanti","doi":"10.22146/ijp.3243","DOIUrl":"https://doi.org/10.22146/ijp.3243","url":null,"abstract":"The excessive oxidative processes and the lack of cellular antioxidative mechanisms are significantly observed in diabetes. In addition, long-term medication required for the treatment might harm the hepatic tissues. This study evaluated the selected pharmacognostic characters, antioxidant activities, total phenolic content, and the hepatic safety of a polyherbal formulation containing seven plant constituents used by Klinik Wisata Kesehatan Jamu Kalibakung, Tegal, Indonesia, to treat diabetes patients. The pharmacognostic properties of the formulation were characterized according to the WHO quality control methods for herbal materials. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH RSA), ferric reducing antioxidant power (FRAP), and total phenolic content (TPC) were evaluated as per the standard method. The effect of formulation on the hepatic HepG2 cells was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay. The pharmacognostic properties of the formulation specified as follow: foreign matters (1.32±0.05%), loss on drying (11.50±0.07%), total ash (5.68±0.07%), acid-insoluble ash (0.94±0.04%), water-soluble extractable (18.22±0.60%), and ethanol-soluble extractable (16.90±0.77%). The ethanol extract showed a superior DPPH RSA (960.70±2.58 mM Trolox equivalent (TE)/ g dry weight (DW)), FRAP (1112.69±8.39 mM TE/g DW), and TPC (1768.40±32.40 mg gallic acid equivalent (GAE)/g DW) over its water counterpart. However, the water extract was safer for HepG2 cells than the ethanol one, with the IC50 values of 218.25±14.03 and 40.24±3.53 µg/ml, respectively. This study set the pharmacognostic standards for an antidiabetic polyherbal formulation with excellent antioxidant activities, in which its traditional use as a decoction was safe for the hepatic cells.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83767881","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}
In this study, Syzygium polyanthum was standardized against gallic acid (GA), and a complete pharmacokinetic test was conducted using in vitro and in vivo models against this phytochemical. High-performance liquid chromatography showed that GA is a major phytochemical in aqueous extract of S. polyanthum. It exhibited a low equilibrium solubility and physiochemical stability at pH 2.0 and 7.4, but it deteriorated rapidly at pH 9.2. It showed low permeability toward Caco-2 intestinal absorption with eight times slower absorption in oral than intravenous administration. GA was unstable in mouse, rat, and dog plasma sera with in vitro half-lives (t1/2) of 60, 53, and 56 min, respectively, but was relatively stable in human plasma serum (t1/2 = 185 min). Approximately 5.6% of GA (10 µM) bound to the human plasma proteins. GA was stable in mouse, rat, dog, and human microsomal extracts with in vitro microsomal intrinsic clearance values of 72, 68, 6, and 22 µL/min/mg, respectively. GA selectively inhibited or stimulated the activity of the tested CYP450 enzymes. The in vivo oral bioavailability of GA was 54%, with short elimination half-life and a high volume of distribution. Thus, the mention pharmacokinetic features of GA must be considered during the development of GA-based products to yield the optimum dosage and pharmacological effect.
{"title":"Favourable drug-lead pharmacokinetic features for designing gallic acid-standardized Syzygium polyanthum aqueous extract-based product","authors":"Hassan Fahmi Ismail, A. Fadhlina, Siti Nurazwa Zainol, Archan Kumar Mamillapalli, Vijayabalaji Venkatesan, Rajesh Eswarappa, Renuka Pillai, Fadzilah Adibah Abdul Majid","doi":"10.22146/ijp.3639","DOIUrl":"https://doi.org/10.22146/ijp.3639","url":null,"abstract":"In this study, Syzygium polyanthum was standardized against gallic acid (GA), and a complete pharmacokinetic test was conducted using in vitro and in vivo models against this phytochemical. High-performance liquid chromatography showed that GA is a major phytochemical in aqueous extract of S. polyanthum. It exhibited a low equilibrium solubility and physiochemical stability at pH 2.0 and 7.4, but it deteriorated rapidly at pH 9.2. It showed low permeability toward Caco-2 intestinal absorption with eight times slower absorption in oral than intravenous administration. GA was unstable in mouse, rat, and dog plasma sera with in vitro half-lives (t1/2) of 60, 53, and 56 min, respectively, but was relatively stable in human plasma serum (t1/2 = 185 min). Approximately 5.6% of GA (10 µM) bound to the human plasma proteins. GA was stable in mouse, rat, dog, and human microsomal extracts with in vitro microsomal intrinsic clearance values of 72, 68, 6, and 22 µL/min/mg, respectively. GA selectively inhibited or stimulated the activity of the tested CYP450 enzymes. The in vivo oral bioavailability of GA was 54%, with short elimination half-life and a high volume of distribution. Thus, the mention pharmacokinetic features of GA must be considered during the development of GA-based products to yield the optimum dosage and pharmacological effect.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89492957","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}
Dhania Novitasari, R. Jenie, Jun Kato, E. Meiyanto
Recent studies present that the CCA-1.1 (a curcumin derivative) impedes the proliferation of breast cancer cells (luminal, HER2-overexpressed, and TNBC cells). Currently, we analyze the possible target of action of CCA-1.1, particularly in breast cancer cells with HER2 amplification using bioinformatics analysis. The differentially expressed genes (DEGs) of HER2-positive breast cancer were retrieved from TCGA-BRCA data (via UALCAN). We used three web-based tools (Swiss Target Prediction, BindingDB, and TargetNet) to predict the potential target of CCA-1.1 using the SMILE-similarity feature. The functional annotation and network enrichment were processed in WebGestalt. The alteration of selected genes was observed in CBioPortal. The protein-protein interaction (PPI) network was constructed in STRING, then ranked based on the degree score using Cytohubba feature in Cytoscape. The survival analysis from the hub-gene was collected in GEPIA2 with selection only for HER2-positive breast cancer cases. The correlation between the hub genes and tumor-infiltrating immune markers was determined using TIMER web tools. The pathway network analysis highlighted the cell cycle regulation in mitosis as affected signaling amid the putative CCA-1.1 targets. We denoted eight potential genes that could be responsible for inhibiting mitosis regulation upon CCA-1.1 treatment, including AURKA, AURKB, PLK1, TPX2, KIF11, MELK, CDK1, and CHEK1. Several of the potential markers (AURKB, AURKA, CDK1, and CHEK1) revealed to be correlated with the immune cells’ infiltration markers. CCA-1.1 might regulate mitosis to induce cell cycle arrest and lead to cell death. The predicted targets of CCA-1.11 gave insight into the potency of CCA-1.1 to be with immunotherapy. Further validation of the data presented in the study is essentially needed to develop CCA-1.1 for breast cancer.
{"title":"Network Pharmacological Analysis Identifies the Curcumin Analog CCA-1.1 Targeting Mitosis Regulatory Process in HER2-Positive Breast Cancer","authors":"Dhania Novitasari, R. Jenie, Jun Kato, E. Meiyanto","doi":"10.22146/ijp.4453","DOIUrl":"https://doi.org/10.22146/ijp.4453","url":null,"abstract":"Recent studies present that the CCA-1.1 (a curcumin derivative) impedes the proliferation of breast cancer cells (luminal, HER2-overexpressed, and TNBC cells). Currently, we analyze the possible target of action of CCA-1.1, particularly in breast cancer cells with HER2 amplification using bioinformatics analysis. The differentially expressed genes (DEGs) of HER2-positive breast cancer were retrieved from TCGA-BRCA data (via UALCAN). We used three web-based tools (Swiss Target Prediction, BindingDB, and TargetNet) to predict the potential target of CCA-1.1 using the SMILE-similarity feature. The functional annotation and network enrichment were processed in WebGestalt. The alteration of selected genes was observed in CBioPortal. The protein-protein interaction (PPI) network was constructed in STRING, then ranked based on the degree score using Cytohubba feature in Cytoscape. The survival analysis from the hub-gene was collected in GEPIA2 with selection only for HER2-positive breast cancer cases. The correlation between the hub genes and tumor-infiltrating immune markers was determined using TIMER web tools. The pathway network analysis highlighted the cell cycle regulation in mitosis as affected signaling amid the putative CCA-1.1 targets. We denoted eight potential genes that could be responsible for inhibiting mitosis regulation upon CCA-1.1 treatment, including AURKA, AURKB, PLK1, TPX2, KIF11, MELK, CDK1, and CHEK1. Several of the potential markers (AURKB, AURKA, CDK1, and CHEK1) revealed to be correlated with the immune cells’ infiltration markers. CCA-1.1 might regulate mitosis to induce cell cycle arrest and lead to cell death. The predicted targets of CCA-1.11 gave insight into the potency of CCA-1.1 to be with immunotherapy. Further validation of the data presented in the study is essentially needed to develop CCA-1.1 for breast cancer.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80844675","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}
Cosmetic foundation is a type of decorative makeup and commonly include a sunscreen agent. Ethyl cinnamate is one of the potential organic essential oil sunscreens. Nevertheless, there is little study on ethyl cinnamate usage in cosmetics, particularly oil-in-water foundation cream. Using an emulsifier in oil-in-water foundation cream a higher concentration does not guarantee higher oil phase recovery. However, using two combinations of emulsifier such as polysorbate 80 and sorbitan monooleate 80 with the optimum combination can be the right solution. This study aims to optimize polysorbate 80 and sorbitan monooleate 80 in a cream foundation using ethyl cinnamate as an active ingredient designed to have an effective ability to protect facial skin from ultraviolet radiation and are safe to use. The optimization formulas design of the emulsifier combination in foundation cream was made using the Simplex Lattice Design method with help Design Expert version 10.0.1. Parameter optimization were the value of pH, viscosity, spreadability, adhesion, and Sun Protection Factor (SPF) value. The stability test and skin irritation test of optimum formula were also conducted. As a positive control, Revlon Colorstay Foundation as a brand cosmetic foundation was used (National Food and Drug Agency of Indonesia number : NA18140300519). The optimum ratio of polysorbate 80 and sorbitan monooleat 80 were 9.565 and 1.435 with the physical characteristics of pH 6.478+0.008; viscosity 5844.2+31.82 cPs; spreadability 6.16+0.11 cm; adhesion 3.346+0.14 seconds; SPF Value 22.385+0.48, and no irritation symptoms. The ethyl cinnamate foundation created was physically stable, had a pleasing look, and did not irritate the skin, making it safe to wear. It also provides efficient UV radiation protection.
{"title":"Optimization of Polysorbate 80 and Sorbitan Monooleate 80 aas Emulsifiers in Foundation Makeup Containing Ethyl Cinnamate","authors":"Ungsari Rizki Eka Purwanto, Intan Martha Cahyani, Y. Purwaningsih, Berliana Ganita Fatika Sandhi, Fitria Febryana","doi":"10.22146/ijp.3308","DOIUrl":"https://doi.org/10.22146/ijp.3308","url":null,"abstract":"Cosmetic foundation is a type of decorative makeup and commonly include a sunscreen agent. Ethyl cinnamate is one of the potential organic essential oil sunscreens. Nevertheless, there is little study on ethyl cinnamate usage in cosmetics, particularly oil-in-water foundation cream. Using an emulsifier in oil-in-water foundation cream a higher concentration does not guarantee higher oil phase recovery. However, using two combinations of emulsifier such as polysorbate 80 and sorbitan monooleate 80 with the optimum combination can be the right solution. This study aims to optimize polysorbate 80 and sorbitan monooleate 80 in a cream foundation using ethyl cinnamate as an active ingredient designed to have an effective ability to protect facial skin from ultraviolet radiation and are safe to use. The optimization formulas design of the emulsifier combination in foundation cream was made using the Simplex Lattice Design method with help Design Expert version 10.0.1. Parameter optimization were the value of pH, viscosity, spreadability, adhesion, and Sun Protection Factor (SPF) value. The stability test and skin irritation test of optimum formula were also conducted. As a positive control, Revlon Colorstay Foundation as a brand cosmetic foundation was used (National Food and Drug Agency of Indonesia number : NA18140300519). The optimum ratio of polysorbate 80 and sorbitan monooleat 80 were 9.565 and 1.435 with the physical characteristics of pH 6.478+0.008; viscosity 5844.2+31.82 cPs; spreadability 6.16+0.11 cm; adhesion 3.346+0.14 seconds; SPF Value 22.385+0.48, and no irritation symptoms. The ethyl cinnamate foundation created was physically stable, had a pleasing look, and did not irritate the skin, making it safe to wear. It also provides efficient UV radiation protection.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85298115","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}
Pulutan (Urena lobata) is a medicinal plant used to treat fever, infection and swelling traditionally, although the pre-clinical study about the herbs as analgesic and anti-inflammatory are still limited. The objective of this study is to measure analgesic and anti-inflammatory activity of U. lobata leaf extract through in vivo study and in silico. This study was performed using male wistar rats divided into eight groups (two control groups and six test groups) (n=5). U. lobata leaf was extracted by water and ethanol, each prepared in dose of 125, 250, 500 mg/kg body weight. Anti-inflammatory activity was evaluated by plethysmometer for 6 hours, meanwhile analgesic activity was examined by analgesymeter for 4 hours. The data was analyzed using one way ANOVA test continued with LSD test (p < 0.05). Following active compound identification using Liquid Chromatography-Mass Spectra (LC-MS/MS), several compounds were used in an in silico study using docking server. Both aqueous and ethanolic extract of U.lobata at 125 and 250 mg/kg bw inhibited paw edema with an Area Under Curve (AUC) volume about 10 % and 5%, respectively, compared to control group (p<0.05). For analgesic activity, aqueous extract of U. lobata were able to increase the AUC for pain threshold of about 30-100 % compared to control group (p<0.05), whereas the activity of ethanolic extract lower than aqueous extract. Stigmasterol and beta-sitosterol in U. lobata potentially inhibited Cycloxygenase-2 (COX-2) as a pro-inflammatory mediator and pain. Aqueous and ethanolic extract of U. lobata have analgesic activity and anti-inflammation, the mechanism was predicted through inhibitory activity of COX-2.
{"title":"ANALGESIC AND ANTI-INFLAMMATION ACTIVITY OF Urena lobata LEAF EXTRACT: STUDY IN VIVO AND IN SILICO","authors":"Y. Purnomo, Andri Tilaqza","doi":"10.22146/ijp.2145","DOIUrl":"https://doi.org/10.22146/ijp.2145","url":null,"abstract":"Pulutan (Urena lobata) is a medicinal plant used to treat fever, infection and swelling traditionally, although the pre-clinical study about the herbs as analgesic and anti-inflammatory are still limited. The objective of this study is to measure analgesic and anti-inflammatory activity of U. lobata leaf extract through in vivo study and in silico. This study was performed using male wistar rats divided into eight groups (two control groups and six test groups) (n=5). U. lobata leaf was extracted by water and ethanol, each prepared in dose of 125, 250, 500 mg/kg body weight. Anti-inflammatory activity was evaluated by plethysmometer for 6 hours, meanwhile analgesic activity was examined by analgesymeter for 4 hours. The data was analyzed using one way ANOVA test continued with LSD test (p < 0.05). Following active compound identification using Liquid Chromatography-Mass Spectra (LC-MS/MS), several compounds were used in an in silico study using docking server. Both aqueous and ethanolic extract of U.lobata at 125 and 250 mg/kg bw inhibited paw edema with an Area Under Curve (AUC) volume about 10 % and 5%, respectively, compared to control group (p<0.05). For analgesic activity, aqueous extract of U. lobata were able to increase the AUC for pain threshold of about 30-100 % compared to control group (p<0.05), whereas the activity of ethanolic extract lower than aqueous extract. Stigmasterol and beta-sitosterol in U. lobata potentially inhibited Cycloxygenase-2 (COX-2) as a pro-inflammatory mediator and pain. Aqueous and ethanolic extract of U. lobata have analgesic activity and anti-inflammation, the mechanism was predicted through inhibitory activity of COX-2.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82855351","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}
F. Keshavarzi, Vithyah Nadaraja, Aliza Alias, M. Farrukh, C. S. Yap
Background & Objectives: Recently published IDSA guidelines on vancomycin dosing no longer advocates the use of trough concentrations as surrogate markers for clinical efficacy. Protocols developed prior to revised targets may not reflect to the true efficacy marker for vancomycin that is AUC/MIC 400-600. This study aimed to evaluate the local vancomycin dosing protocol in achieving the target trough concentration and extrapolated AUC/MIC of 400-600 in patients with haemodialysis. Methods: A retrospective analysis of therapeutic drug monitoring forms and individual medical records of haemodialysis patients was conducted. Vancomycin AUC of each individual was extrapolated via the use of a pharmacokinetic modelling software, PrecisePK®. Chi-square test of independence was used to determine the association of factors affecting AUC/MIC. A p value of 0.05 was considered statistically significant. Results: A total number of 80 haemodialysis-dependent cases who were on vancomycin were recruited. More than 62% of haemodialysis patients showed AUC/MIC > 800. AUC/MIC was heavily influenced by minimum inhibitory concentration of the infecting microorganism. Interpretation & Conclusions: Exclusive trough-guided dosing may not translate well in achieving clinical efficacy of vancomycin in haemodialysis patients. Other contributing factors, especially MIC should be factored, as small MIC values account for greater reciprocal AUC/MIC values that increase the risk of loss of residual kidney function; a factor which is associated with overall mortality of HD patients.
{"title":"Evaluation of trough-based vancomycin therapy in achieving targeted area under the curve in haemodialysis cases.","authors":"F. Keshavarzi, Vithyah Nadaraja, Aliza Alias, M. Farrukh, C. S. Yap","doi":"10.22146/ijp.4433","DOIUrl":"https://doi.org/10.22146/ijp.4433","url":null,"abstract":"Background & Objectives: Recently published IDSA guidelines on vancomycin dosing no longer advocates the use of trough concentrations as surrogate markers for clinical efficacy. Protocols developed prior to revised targets may not reflect to the true efficacy marker for vancomycin that is AUC/MIC 400-600. This study aimed to evaluate the local vancomycin dosing protocol in achieving the target trough concentration and extrapolated AUC/MIC of 400-600 in patients with haemodialysis. \u0000Methods: A retrospective analysis of therapeutic drug monitoring forms and individual medical records of haemodialysis patients was conducted. Vancomycin AUC of each individual was extrapolated via the use of a pharmacokinetic modelling software, PrecisePK®. Chi-square test of independence was used to determine the association of factors affecting AUC/MIC. A p value of 0.05 was considered statistically significant. \u0000Results: A total number of 80 haemodialysis-dependent cases who were on vancomycin were recruited. More than 62% of haemodialysis patients showed AUC/MIC > 800. AUC/MIC was heavily influenced by minimum inhibitory concentration of the infecting microorganism. Interpretation & Conclusions: Exclusive trough-guided dosing may not translate well in achieving clinical efficacy of vancomycin in haemodialysis patients. Other contributing factors, especially MIC should be factored, as small MIC values account for greater reciprocal AUC/MIC values that increase the risk of loss of residual kidney function; a factor which is associated with overall mortality of HD patients.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86368878","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}
Alzheimer's disease (AD) is a neurological illness that causes a wide range of cognitive symptoms linked to amyloid plaque deposition, neurofibrillary tangles, oxidative stress, and neuron death in the whole brain. Curcumin has shown promising efficacy in preclinical studies for AD treatment. However, it failed to exhibit expected clinical outcomes in clinical studies. Besides, this molecule has low stability, solubility, and bioavailability properties. Hence, scientists have synthesized several curcumin analogues to improve their bioavailability and biological activity. The purpose of this narrative review is to discuss the development of curcumin analogue synthesis published in 2016-2021 and its efficacy that reveals its effect as an anti-Alzheimer's candidate through in vitro, cell-based and in vivo studies. Pubmed and Scopus database search engine with the keywords "curcumin" AND "analogues" OR "analogs" AND "Alzheimer's" were used to find the relevant studies. In our review, we include sixteen eligible journal articles to discuss. Fifteen curcumin analogues exhibited promise efficacy in preclinical studies and are suitable for development as anti-Alzheimer's candidates. Further study should explore to confirm the curcumin analogues toxicity, develop an appropriate dosage form, and initiate clinical trials.
{"title":"Curcumin Analogues as Novel Anti-Alzheimer's Candidates: Synthesis Development Strategy, In Vitro, Cell-Based and In Vivo Studies","authors":"Yance Anas, Ratna Asmah Susidarti, Nunung Yuniarti, Ronny Martien","doi":"10.22146/ijp.4432","DOIUrl":"https://doi.org/10.22146/ijp.4432","url":null,"abstract":"Alzheimer's disease (AD) is a neurological illness that causes a wide range of cognitive symptoms linked to amyloid plaque deposition, neurofibrillary tangles, oxidative stress, and neuron death in the whole brain. Curcumin has shown promising efficacy in preclinical studies for AD treatment. However, it failed to exhibit expected clinical outcomes in clinical studies. Besides, this molecule has low stability, solubility, and bioavailability properties. Hence, scientists have synthesized several curcumin analogues to improve their bioavailability and biological activity. The purpose of this narrative review is to discuss the development of curcumin analogue synthesis published in 2016-2021 and its efficacy that reveals its effect as an anti-Alzheimer's candidate through in vitro, cell-based and in vivo studies. Pubmed and Scopus database search engine with the keywords \"curcumin\" AND \"analogues\" OR \"analogs\" AND \"Alzheimer's\" were used to find the relevant studies. In our review, we include sixteen eligible journal articles to discuss. Fifteen curcumin analogues exhibited promise efficacy in preclinical studies and are suitable for development as anti-Alzheimer's candidates. Further study should explore to confirm the curcumin analogues toxicity, develop an appropriate dosage form, and initiate clinical trials.","PeriodicalId":13520,"journal":{"name":"INDONESIAN JOURNAL OF PHARMACY","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2022-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84980999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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