Indonesian Journal of Pharmacy
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The Potential of Tapak Dara (Catharanthus roseus) Leaves Endophytic Bacteria BETD5 as Antioxidant and Anticancer Against T47D Breast Cancer Cells
Get PDFThis study aimed to measure antioxidant activity, to characterize biochemical properties and to measure cytotoxicity activity in BETD5 isolates. The method used in this research was experimental method. Parameters observed were antioxidant activity and cytotoxicity activity consisting of IC50 (Inhibition Concentration) and biochemical properties. Isolate used was extract of endophytic bacteria of Tapak Dara (BETD5). antioxidant activity was conducted using various sample extract concentration, namely 5ppm, 10ppm, 25ppm, 50ppm and 100ppm. The biochemical tests carried out included Triple Sugar Iron Agar (TSIA) test, Simmons Citrate (SC) test, motility test, indole test, catalase test and Methyl Red (MR) test. Cytotoxicity test on cell line T47D was performed by MTT assay using concentration (%) of 3.125; 6.25; 12.5; 25 and 50. The results showed that antioxidant activity of BETD5 was strong because IC50 value obtained was 78.485 ppm. Based on biochemical tests, BETD5 was suspected belong to the genus Staphylococcus. Cytotoxicity activity of BETD5 obtained an IC50 value of 15.58 ppm. This indicates that endophytic bacterial extract of Tapak Dara (BETD5) had moderate cytotoxicity against the T47D breast cancer cell line. GCMS test results showed that the endophytic bacterial isolate BETD5 had the highest secondary metabolite content, namely cis-Ocimene (24.31%)
L-proline as Co-crystal Forming Amino Acid for Enhanced Dissolution Rate of Lamotrigine: Development of Buccal Tablet
No full textLamotrigine is an antiepileptic drug with slow dissolution rate which can reduce its oral bioavailability. In addition, it was reported to have first pass metabolism. Accordingly, the aim of this work was to enhance its dissolution rate utilizing co-crystallization technique to be suitable for incorporation in buccal dosage form. L-proline was selected as co-crystal co-former for enhancing dissolution in addition to its beneficial anticonvulsant properties. Formulations containing lamotrigine and L-proline at different molar ratios were prepared using ethanol assisted co-grinding. The prepared formulations were characterized using FTIR, X-Ray powder diffraction, differential scanning calorimetry and dissolution studies. The formulation recorded the highest dissolution rate was incorporated in fast disintegrating tablet for buccal use. Characterization techniques suggested the formation of lamotrigine-l-proline co-crystals with 1:2 molar ratio being optimum for interaction. This interaction resulted in significant enhancement in dissolution rate with the ratio of lamotrigine to proline at molar ratio of 1:4 showed greatest dissolution rate (% DE= 80.57). The prepared tablet utilizing lamotrigine and L-proline at molar ratio of 1:4 showed fast disintegration and rapid dissolution rate compared with control tablet containing lamotrigine alone. The study suggested L-proline as an efficient co-crystal co-former for enhancing dissolution rate of lamotrigine for buccal delivery.  
Co-Milling: A Successful Approach to Enhance Solubility of a Poorly Soluble Antihypertensive Drug
Get PDFThe aim of the work was to enhance the solubilization of Olmesartan-medoxomil (OM) and formulate stable, rapidly-dissolving-tablet formulations. OM, on the other hand, is classified as Biopharmaceutics Classification System (BCS) Class II drug, which indicates that it is characterized by water-insolubility. Therefore, increasing its solubilization has the potential to boost its bioavailability. For the OM evaluation, a new HPLC technique was invented and then validated in accordance with international standards. The formulation of tablets involved co-milling with certain superdisintegrants, specifically croscarmellose sodium (Ac-Di-Sol) and crospovidone in varying percentages, followed by mixing with pH-adjusting substances such as calcium carbonate to increase solubilization in cases where the drug is soluble in alkaline. Following the evaluation of the created formulations, the optimized formulations were selected for further stability assessment. Co-milling process with crospovidone greatly improved the olmesartan release. The optimized formulations were OD11 and OD12, which exhibited fast disintegration, and the release exceeded 90% within 10 min, while the release for Olmesartan medoxomil pure standard was 9.8% after 10 min. The OD11 and OD12 were chosen for further stability assessment and revealed good stability behavior, as the study on optimized formulations revealed that the degradation was less than 5% after storage for six months at 40 °C and 75% relative humidity. Some formulations exhibited good results in terms of disintegration and release. The results of the formulations (OD11 and OD12) suggested that co-grinding with crospovidone may increase the solubilization of OM to greater than 90% after 10 minutes
Study of 1-Formyl-2-Pyrazolines as Anticancer Drug Candidates
Get PDFThe development of novel anticancer agents is essential in cancer prevention. One versatile group of compounds, known for their significant bioactivity and several of its derivatives that have been clinically approved, is the group of pyrazolines. This study aimed to synthesize 1-formyl-2-pyrazoline derivatives (pyrazolines 1-2) using chalcone 1-2, hydrazine hydrate, and formic acid via cyclo-condensation. The synthesized compounds were characterized using Fourier Transform Infrared (FTIR), Gas Chromatography-Mass Spectrometry (GC-MS), and Nuclear Magnetic Resonance (1H- and 13C-NMR) spectrometers. Pyrazolines 1-2 were found to be drug-like compounds, satisfying Lipinski’s Rule of Five and possessing favourable absorption, distribution, metabolism, and excretion (ADME) properties, including good gastrointestinal absorption, blood-brain barrier permeability, and no interaction with P-glycoprotein. Furthermore, they were inactive against several toxicity endpoints in a normal body condition, such as immunotoxicity, mutagenicity, and cytotoxicity. In vitro cytotoxic evaluation of the pyrazolines 1-2 against HeLa and MCF7 cancer cell lines demonstrated moderate activity, with IC50 values of 25.01 µM and 82.87 µM, respectively. Pyrazolines 1-2 also showed good selectivity with selectivity index (SI) values of 8.92 and 14.45. The molecular docking study on epidermal growth factor receptor tyrosine kinase (EGFR-TK) (PDB ID: 4HJO) revealed that pyrazolines 1-2 had a binding affinity of -7.9 and -8.0 kcal/mol, respectively. The compounds interacted with Lys721 residue through hydrogen bonds and hydrophobic interactions due to the presence of the pyrazoline ring and the formyl group in their structures. These findings suggest that pyrazolines 1-2 scaffold has the potential to be further studied as a lead compound for anticancer drug candidates
Development and Validation of HPLC–Photodiode Array Method for Detecting Steroids in Skin Whitening Products Simultaneously
Get PDFSince steroids are prohibited to be present in cosmetic products, thus an identification of these outlawed compounds intentionally incorporated in skin whitening product is enough for market surveillance purpose. Simultaneous method for detecting prednisone (PRN), triamcinolone acetonide (TCA), hydrocortisone acetate (HCA), clobetasole propionate (CBP), and mometasone furoate (MTF) has not been developed until now. The goals of this study were to develop and to validate for screening these five steroid compounds in cosmetic product by using reverse phase (RP) high-performance liquid chromatography (HPLC) equipped with photo diode array (PDA) detector. Validation method was applied including the system suitability test, determination of specificity and selectivity, and determination of detection limit. . In optimization step, we succeeded distinguish and identify five steroid compounds with different retention time.The retention times of PRN, TCA, HCA, CBP and MTF were detected at 3.267, 4.260, 4.910, 15.360, and 16.707 min, respectively. The method performed good selectivity with resolution more than 1.5. While for determination of limit of detection (LOD) was carried out by calibration curve approach over the range 0.5-5 µg/ml and resulted in LOD value for PRN, TCA, HCA, CBP and MTF were 7.20, 8.85, 8.17, 9.30, and 8.42 µg/g, respectively. The developed method can be applied for routine analysis of PRN, TCA, HCA, CBP and MTF in various type of cosmetic products
The Effects of Zingiber Officinale and Propolis Supplementation on Hospitalized Covid-19 Patients' Oxygen Saturation
Get PDFAntiviral, anti-inflammatory, and supportive therapy are required in the Covid-19 management, whilst there is no available specific antiviral for Covid-19 patients. Zingiber officinale and Propolis were reported to suppress the pro-inflammatory cytokines and their safety profiles were considered in several toxicity studies. However, their efficacy in hospitalized Covid-19 patients has not been clarified yet. This study explored the activity of Z. officinale and Propolis in modulating the clinical signs and hematology parameters in hospitalized Covid-19 patients. A total of 22 subjects were divided into a control group (standard therapy), and a treatment group (standard therapy and supplemented with the combination of Z. officinale 500 mg/day and Propolis 1000 mg/day). We analyzed the differences in demographic characteristics, clinical signs, and hematology parameters at pre and post-treatment in both groups. The increased oxygen saturation in control and treatment groups were 0.45 ± 0.45 and 3.45 ± 1.16, respectively (p = 0.011). Moreover, the high-fluorescent lymphocyte count (HFLC) and mean platelet volume (MPV) in the treatment group tend to be lower compared to the control, although it is not statistically significant. The supplementation of Z. officinale and Propolis has beneficial effects in alleviating clinical signs of Covid-19 disease, especially in the enhancement of oxygen saturation, and tend to restore the hematological parameters
Steroidal Saponin Isolated from Dioscorea alata L. Extract Improve Digestive Tract Allergy in Balb/C Mice Induced by Ovalbumin
Get PDFSteroidal saponin compound in Dioscorea species is one of the crucial substance because it has some biological functions, such as immunomodulatory and anti-allergic agent. This study aims to analyze the effect of steroidal saponin of Dioscorea alata L. on CD4 T cells activation, cytokines IL-4, IL-5 and TGF-β. This study used primary lymphocyte cell which isolated from BALB/c mice spleen. Mice lymphocyte were cultured in the complete medium with presence of various concentrations (50, 25 and 12.5 µg/mL) of three isolate of steroidal saponin of D. alata for 24 h. Diosgenin was used as positive control. After 24 h of treatment, the activation of lymphocyte, IL-4 and IL-5 production was determined by Flowcytometry analysis. Data were analyzed using student t-test with p < 0.05 and p < 0.01. The results showed that the low concentration of Isolate 1 (12.5 µg/mL) was found to be effective to stimulate the activation of CD4 T cells, reduce the production of IL4 and IL-5 by CD4 T cells and increase TGF-β production. These results showed that a low concentration of steroidal saponin of D. alata could be considered as immunomodulatory and anti-allergic agent. Purification and identification of each isolate isolated from DAE is in progress
Optimization and Characterization of Extruded Partially Pregelatinized Cassava Starch as Filler-Binder
Get PDFIn order to use starch as a filler-binder, the pregelatinization method by extrusion can enhance the flow characteristics and compressibility of starch. This study aimed to find the optimum process parameter for producing partially pregelatinized cassava starch (PPCS) using twin screw extrusion and characterizing it as a filler-binder excipient. For arranging experimental trials, a three-level Box-Behnken design with three independent variables—starch moisture content (ranged from 20% to 40%), extrusion temperature (ranged from 50°C to 70°C), and screw speed (ranged from 10 rpm to 30 rpm)—was used to make PPCS. The response surface methodology approach was used for optimization. The desired filler-binder characteristic of PPCS was defined as having good flowability and compactibility properties. The most desirable process parameter was achieved by combining 39.9 percent starch moisture content, 70°C extrusion temperature, and 25.8 rpm screw speed. The results showed that optimized PPCS has good flow properties and also good water absorption capacity. The optimized PPCS had a polygonal shape and a size range of 149-400μm. PPCS showed birefringence characteristics under polarized light, indicating a large number of undamaged starch granules. The PPCS XRD pattern showed peaks at 15°, 17°, 18°, and 23°, and also a relative crystallinity of 27.3 percent. When analyzed with DSC, PPCS revealed glass transition curves and a gelatinization degree of 36.01 percent
An overview of the role of Zingiber officinale as an antimicrobial resistance (AMR) solution and a source of antioxidants
No full textIn this review, we describe the known mechanisms of antimicrobial resistance which was increasing in this era, due to the misuse of antimicrobial agents such as antibiotics, or genetic and phenotypic mechanisms. In this review, the concerns, especially addressed by designated researchers in their study and WHO in their observations and reports, regarding the types or strains of bacteria with antimicrobial resistances were described. In addition, the predicted mechanisms that promote the development and occurrence of antimicrobial resistances, such as bacterial biofilm formation, horizontal gene transfer, genetic mutations, free DNA which contains antimicrobial resistance genes, plasmids transfer through transformation or conjugation from bacterial cell to cell were well described. In addition, we also tried to describe the use of Z. officinale. The antimicrobial capabilities of this herbal plant are attributed to its capacity to create many secondary metabolites with rather complicated structures that have antibacterial and antioxidant characteristics. Z. officinale had been used for many kinds of diseases treatment traditionally. And along the way, the advance techniques of research in chemistry and biology fields had found out the composition and bioactive compound. In this review, the common online databases such as PubMed, Semantic Scholar, Crossref, Medline, Scopus, and Web of Science (WoS) were utilized to conduct literature searches. According to recent progress of antimicrobial cases observed, the efforts to strengthen the surveillance, general health systems, tightened the antimicrobial medicine distribution rules, and education for public are indeed needed
Detection of ACE Gene SNPs Using rhAmp Genotyping Platform and Their Association with I/D Polymorphism in COVID-19 Patients with Hypertension
Get PDFThe high activity of Angiotensin Converting Enzyme (ACE) in patients with hypertension is thought to affect the risk and severity of COVID-19. Insertion/deletion (I/D) and SNP polymorphisms of the ACE gene can affect ACE activity in the Renin-Angiotensin System (RAS). This study aims to identify linkage disequilibrium SNPs rs4331 (A/G), rs4341 (G/C), and rs4343 (G/A) with I/D polymorphisms reported in previous studies and their associations with the severity of COVID-19 with hypertension comorbid. A cross-sectional study in 2021 recruited 95 samples of COVID-19 patients from two regions representing the eastern and western parts of Indonesia. Detection of polymorphisms using rhAmp SNP showed the percentage of genotypes GG, AG, and AA at rs4331 according to genotype II, DI, and DD in polymorphism I/D (57%, 32%, and 11%). In contrast, rs4341 only showed one type of genotype (GG), and 37% of the samples were undetermined at rs4343. Based on the linkage disequilibrium, it is known that rs4331, rs1799752, and rs4343 are in strong LD (D'= 0.97 and 0.99), and rs4331 and rs1799752 can be markers of genes to replace one with another (R2= 0.957). The haplotype analysis showed a significant difference between the residents of western and eastern Indonesia (p = 0.005), whereas this was not the case with hypertension comorbidities and the severity of COVID-19. Seventeen percent of the G-I-G-G haplotypes showed moderate-severe severity, while 15% of the A-D-G-G haplotypes showed mild severity. Therefore, it can be concluded that the high I/D, rs4331, and rs4343 polymorphisms are likely co-inherited and that the G-I-G-G haplotype is associated with moderate-to-severe severity in COVID-19