Indonesian Journal of Pharmacy
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New curcumin analog, CCA-1.1, synergistically improves the antiproliferative effect of doxorubicin against T47D breast cancer cells
Get PDFAn improved compound of pentagamavunone-1 (PGV-1), chemoprevention-curcumin analog 1.1 (CCA-1.1), has been synthesized and proven to have antiproliferative effects against breast cancer cells. This study is designed to investigate the potency of CCA-1.1 alone and in combination with doxorubicin (Dox) on T47D cells in comparison with that of PGV-1. We used the MTT assay to assess cytotoxic activity. Propidium iodide (PI), annexin-V–PI, and DCFDA staining were respectively used to determine cell cycle profiles, apoptosis, and intracellular reactive oxygen species (ROS) levels. Senescent cells were identified using the SA-b-galactosidase assay. Our results revealed that CCA-1.1 possesses cytotoxic effects similar to those of PGV-1 on T47D cells. Synergistic effects during co-treatment with Dox were also observed. CCA-1.1 arrested cell cycle progression at the G2/M phase and limited sub-G1 accumulation, which is correlated with apoptosis. CCA-1.1 alone and in combination with Dox increased senescence and intracellular ROS to a similar level to those achieved by PGV-1. CCA-1.1 alone and in combination with Dox enhanced cytotoxic activity toward T47 cells compared to PGV-1. Thus, this curcumin analog may be a potential chemotherapeutic/co-chemotherapeutic candidate for estrogen receptor-positive (ER+) breast cancer therapy
An Explorative Qualitative Study on Pharmacist Active Engagement Approach in Primary Healthcare Diabetic Education
Get PDFThe conventional counseling method focuses on imparting knowledge meanwhile active engagement approach would enhance patient’s participation and control in the health management process. This study explored the various elements that affect the pharmacist-patient active engagement during diabetes counseling sessions in primary healthcare settings. A qualitative study using thematic analysis of semi-structured interviews was utilized. Subjects were recruited from five primary healthcare clinics in Kuala Lumpur. Ten pharmacists actively running the diabetes medication therapy adherence clinical (DMTAC) counseling and 15 patients who are currently enrolled under the DMTAC program participated in this study. A combination of computer software ATLAS.ti and hand-written methods were used in the mind mapping to assist with the development of the themes. The qualitative analysis identified themes associated with pharmacist active engagement approach include establish rapport (subthemes: introduction and greetings, ice-breaking, background check, attitude, pharmacist motivation), getting information to explore the patient problems (subthemes: giving attention, communication, the time factor, re-assess patients’ understanding), building relationship (subthemes: sharing of ideas, emotions, relationship, trust, sensitiveness, support and belief), explanation and planning (subthemes: making a decision and mutual discussion) and closing the session (subthemes: accessibility to pharmacists, DMTAC appointments). This study established areas of active engagement namely, shared decision-making, engaging communication, and motivational interview skills that should be imparted to the pharmacists to enhance the current diabetes counseling practice
The Effect of Anti Pollutant Gel from Sansevieria trifasciata on Malondialdehyde Level and Histopathology of Rats’ Liver and Lungs Induced by Cigarette, Coal, and Mosquito Smoke
Get PDFGas pollutants that accumulate in the room with restricted air circulation may cause respiratory system disorders. A pregnane glycoside compound from Sansevieria can reduce the pollutants. This study aims at producing gels from Sansevieria extract to neutralize indoor gas pollutants. Sansevieria extract is produced by the maceration process with composition 8 g simplicia and 100 ml ethanol 96%. The extract was processed into the gel with a 20% concentration. The gel was applied to rats (Rattus norvegicus) Wistar strain induced by cigarette, coal, and mosquito smoke with positive control and treatment groups. After 8 days, the Gross examination and histopathology of lungs and liver were observed quantitatively. MDA levels were measured with the TBARS method. Data were analyzed by independent sample T-test and Mann-Whitney test with p-value considered significant if <0,05. Gross examination of lungs showed a significant difference between the treatment and control group that was induced by coal smoke (p=0.031), and mosquito smoke (p=0.006), and the liver’s gross of cigarette smoke (p=0.040). Histopathology of lungs showed a significant difference in mosquito smoke (p=0.032) and no significant difference in histopathology of the liver. MDA levels showed significant difference in coal smoke (p=0.020) and mosquito smoke (p=0.000). In conclusion, anti pollutant gel reduces MDA levels and damage of the lungs induced by pollutants
An Efficient Directly Conversion of the Ethyl p-Methoxycinnamate into N,N-dimethyl-p-Methoxycinnamamide and study the structure-activity relationship on anti-inflammatory activity
Get PDFEthyl p-methoxycinnamate (EPMC) (1) is a major natural ester found in the rhizome of Kaempferia galanga and has been reported to have anti-inflammatory activity. Some of the structural modification of this compound has been carried out in order to study the structure-activity relationship on its anti-inflammatory activity. In the present study, we report a new, simple and efficient procedure in the conversion of the ethyl p-methoxycinnamate into N,N-dimethyl-p-methoxycinnamamide (5) and then study the structure-activity relationship on its anti-inflammatory activity. The reaction was carried out through a microwave-assisted direct amidation between (EPMC) (1) with dimethylformamide (DMF) in the basic condition. The mixture was irradiated by using unmodified microwave-oven at 300 W for 1 minute to obtain compound (5) in 88.8% yields. The extensive analysis of the GCMS and NMR data supported that the product of synthesis is N,N-dimethyl-p-methoxycinnamamide (5). Evaluation of the anti-inflammatory activity of compound 5 by using anti-denaturation of heat bovine serum albumin (BSA) assay indicated that N,N-dimethyl-p-methoxycinnamamide (5) still have anti-denaturation activity. Compound 5 has an amide functional group which is more slowly hydrolyzed if compared to 1. Hence, the reaction has successfully produced a more stable compound which still has anti-inflammatory activit
Acute Toxicity of Keladi Tikus (Typhonium flagelliforme (Lodd.) Blume) Ethanol Extract on Zebrafish (Danio rerio) Embryo In Vivo
Get PDFKeladi tikus (Typhonium flagelliforme (Lodd.) Blume) is an Indonesian medicinal plant that has various pharmacological properties. Zebrafish (Danio rerio) has been proposed as a model that can bridge the gap between cell assays and rodent assays. Evaluation of the toxic effects of natural products using the Zebrafish model can be assessed starting from the blastula stage of embryonic development. This study aims to investigate the potential acute toxicity effect of keladi tikus-ethanol extract (KTEE) using zebrafish embryos. A static non-replacement regime for acute toxicity testing was used. Wild-type zebrafish embryos were exposed to various concentrations of KTEE (50, 100, 200, 400, 800, 1600 µg/mL) starting at 6 hours post-fertilization (hpf) until 96 hpf. The results showed that the survival rate of zebrafish embryos decreased as the concentration of the test extract increased. The LC50 values of KTEE were 494.553 µg/mL at 96 hpf and 555.787 µg/mL at 72 hpf. Embryotoxicity effect of KTEE includes hatching delays and decreased heartrate on zebrafish embryos, especially at high concentrations. KTEE also caused abnormalities in embryo morphology, including pericardial edema, jaw and tail deformity
Effects of Health Informations System “Dosing Gama” on Time Efficiency in Dosage Adjustment Evaluation
Get PDFIndonesian Ministry of Health shows an increase in patients with impaired kidney and liver function by 10-50% since 2007. The increase is a challenge for pharmacists in conducting pharmaceutical care, which is that dose adjustment for these patients takes a long time. Dosing GAMA, an application that has been developed in 2018, is expected to overcome these obstacles. This study aims to identify the use of the Dosing GAMA application to assist pharmacists in making dose adjustments evaluation more efficient and to assess pharmacist's acceptance of the application. This study was a quasi-experimental study using post-test with control group design. Respondents were recruited by selecting pharmacists according to the inclusion criterion. The control group consisted of 26 pharmacists who made dose adjustments manually, and the intervention group consisted of 26 pharmacists who made dose adjustments using the Dosing GAMA application. Data were obtained by measuring the time required by the pharmacist to make dose adjustments. The intervention group was then asked to complete a perceived acceptance questionnaire. The study indicated that Dosing GAMA could reduce the time needed for dose adjustment evaluation (p<0.05). An average time spent by pharmacists with Dosing GAMA was shorter than that spent by those who made dose adjustments manually without application (13.81±0.78 min vs. 27.5±1.23 min). Overall, the pharmacists have high perceived acceptance of the application. The study results can be used as the basis for developing the application. Furthermore, it is expected that the Dosing GAMA can improve pharmacists’ performance in providing effective pharmaceutical care
Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
Get PDFGonorrhea is one of the most often sexually transmitted infection in the world. In 2016, WHO stated the Southeast Asia region as the fourth-highest incidence rate and prevalence of gonorrhea. One of the current problems with gonorrhea is related to its emerging resistance to first-line drugs such as cephalosporins, macrolides, and fluoroquinolones. This resistance has an impact on the difficulty of finding effective antibiotics to eradicate the infection, thus risking financial loss and infertility in sexually active age patients. This literature review will discuss solithromycin, the first fluoroketolide in phase III clinical trial, and show its potential as a new antibiotic against infection with resistant Neisseria gonorrhoeae. Literatures are searched using Pubmed and Google Scholar search engines with keywords: antibiotics, CEM-101, clinical trial, Neisseria gonorrhoeae, new treatment, pharmacology, pharmacokinetics, resistance, safety, and solithromycin. This semisynthetic antibiotic is supported by a different chemical structure from previous macrolides; improving solithromycin becomes more stable and able to bind easier with bacterial ribosomes. Pharmacologically, solithromycin provides an advantage in its high bioavailability, easy oral administration route, wide distribution, metabolism mainly in the liver, but not required dosage adjustments due to hepatic impairment, and a single dosage preparation that can increase patient compliance in healing gonorrhea infections. Also, its lower MIC50 than previous antibiotics makes it well-tolerated, therefore making this antibiotic as a potential recommendation for the management of multi-drug resistant gonorrhea in the future. Solithromycin is not inferior to the standard therapy (ceftriaxone and azithromycin), with 80% vs. 84% gonorrhea eradication rates. Per the anatomic site, the eradication rate is 92% in genital, 94% in the pharynx, and 83% in the rectum. However, special attention needs to be paid to the side effects of the gastrointestinal tract of solithromycin, as observed in phase III clinical trials at a dose of 1000 mg in the form of diarrhea (24%) and nausea (21%)
Liquisolid Tablets Formulation of Atorvastatin Calcium Using Polyethylene Glycol 400 as Solvent and Some Carrier Materials
Get PDFThe dissolution of atorvastatin calcium need to be improved since included BCS Class II drugs with low solubility and high permeability, meaning that the dissolution affects the bioavailability of drugs. This research aimed to develop a formulation of a liquisolid tablet using PEG 400 as a solvent and some carrier materials in various compositions to increase the dissolution of atorvastatin calcium. Different formulations of liquisolid tablets were conducted using different quantities of carrier and coating material for adsorbing liquid solvent to produce a free-flowing and compressible powder. Avicel PH 101, Avicel PH 102, Neusilin US2 were employed as the carrier and Aerosil 200 as the coating material. A disintegrant and lubricant were then added to the formed liquisolid system and compressed into tablets by the direct compressing method. The liquisolid tablets were characterized for their tableting properties and possible drug-excipient interaction by XRD and FTIR analysis. The tableting characteristics of atorvastatin calcium liquisolid tablets were within the acceptable limits criteria. The dissolution of AA4 and NA1 liquisolid tablets was higher compared to marketed tablets. Based on the XRD and FTIR analysis, no interactions between drug and excipient.  
Antidiabetes of Combination of Fractionated-extracts of Andrographis paniculata and Centella asiatica in Neonatal Streptozotocin-induced Diabetic Rats
Get PDFMany medicinal plants are widely grown in South- and Southeast Asia countries. Some of them are traditionally used for treatment of diabetes mellitus such as Andrographis paniculata and Centella asiatica. In the study, we provided fractionated-extracts of A. paniculata and C. asiatica to increase the concentration of their active compounds and eliminate unexpected substances. The aim of the study was to evaluate the antidiabetes effect of the combination of their fractionated-extracts in male neonatal streptozotocin (STZ)-induced diabetic rats. In the study, diabetes was injected intraperitoneally 90mg.kg-1 BWSTZ to two day-old rats. At the age of three months, the rats were administered with the combination of both fractionated-extracts for 14 consecutive days. We evaluated antidiabetes with parameters of blood glucose levels, morphology of pancreatic islet, β-cell density as well as immunohistochemical pancreatic insulin. The levels of MDA, SOD and GPx were also determined about oxidative stress change after treatment with the combination. In the study, the combination succeeded to lower the blood glucose level in neonatal STZ-induced diabetic rats. Inline with fact, improvement of rat pancreatic islets and β cells density, as well as moderate restoration of pancreatic insulin, were observed after treatment with the combination. The substance could decrease the level of MDA, and increase the levels of SOD and GPx. In conclusion, the combination of fractionated-extracts of A. paniculata and C. asiatica exhibited potential antidiabetic effect to its antioxidative effect in male neonatal STZ-induced diabetes rats
Synthesis and antitumor properties of some new N-(5-R-benzyl-1,3-thiazol-2-yl)-4,5-dihydro-1H-imidazole-2-carboxamides
Get PDFNew N-(5-R-benzyl-1,3-thiazol-2-yl)-2-morpholin-4-yl-2-oxoacetamides have been prepared in good yields via the reaction of N-(5-R-benzyl-1,3-thiazol-2-yl)-2-chloroacetamides with sulfur and morfoline. These compounds react with ethendiamine to form a series of novel N-[5-R-benzyl)-1,3-thiazol-2-yl]-4,5-dihydro-1H-imidazole-2-carboxamides with excellent yields. Anticancer activity screening of synthesized compounds was carried out within the framework of the Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was shown that compounds are promising for new anticancer agents' search