Indonesian Journal of Pharmacy
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Synthesis, and Anti-Tumor Evaluation of Some New Flurbiprofen Derivatives Against MCF-7 and WRL-68 Cell Lines
Get PDFA new series of flurbiprofen derivatives containing thiosemicarbazide moiety (3-7) was synthesized from flurbiprofen as parent nucleus by esterification, hydrazide formation, and heating with different aryl isothiocyanate substituents, respectively. Flurbiprofen was also treated with thiosemicarbazide in the presence POCl3 as a catalyst, to produce 1,3,4 -thiadiazole -2-amine (8). Treatment of (8) with different aryl isothiocyanates produced thiourea derivatives (9-12). Also, the reaction of (8) with different benzoyl chloride substituents produced benzamide compounds (13-15). Eventually , treatment of (8) with ethyl acetoacetate(EAA) produced [1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one (16) .The new compounds were characterized by spectroscopic techniques :FTIR, 1HNMR, and CHNS analysis. A molecular docking study for the synthesized compounds (3-16), against the Vascular Endothelial Growth Factor receptor (VEGFR-2) was applied and it indicated that compounds 4,7,13, and 15,exhibited the optimum binding energy of -6.77, -6.12,-6.68, and -6.43 kcal/mol, respectively. Target compounds were also assessed for their in vitro anticancer effects in a cell-line study. All of the compounds tested showed the most plausible anticancer activity, compared to a positive control(Sorafenib), using in vitro MTT cytotoxic assay ,against human breast tumor (MCF-7), and normal WRL-68 cell line. The in vitro results revealed that compounds 4,5,10,11,13, and 15 exhibited the highest inhibitory activity at their IC50 concentrations, against MCF-7 cell lines, as follows (122.7,113.9,95,7. 109.1,40.32 and 112.29µg/mL, respectively. While their cytotoxic effect against normal WRL-68 cell line at their IC50 concentrations, as follow 210.2, 181.3 ,151.7,278.7,80.28, and 236 µg/mL, respectively, therefore, such compounds were considered more selective toward MCF-7 than normal WRL-68,and their selectivity index (SI): 1.71,1.59,1.59 ,2.55 ,1.99 , and 2.10,respectively . Among the synthesized compounds, the compound 15 was chosen to screen its effect in vitro through multi-parameter cytotoxic assay against MCF-7 breast cancer implemented in High Content Screening (ArrayScan XTI, Thermo Scientific),which could be taken in consideration as a starting point for the development of new anticancer drug
Optimization of Hydroxy Propyl Methyl Cellulose and Carbomer In Diltiazem Hydrochloride Mucoadhesive Buccal Film
Get PDFDiltiazem hydrochloride (HCl) is a category of calcium channel blocker used as an antihypertensive agent. Diltiazem HCl is a low bioavailable drug due to high first-pass metabolism and a short half-life (3-5 hours); hence mucoadhesive buccal film was made to overcome this weakness. Bioavailability of Diltiazem HCl increase if the buccal preparations can contact the mucosa for a sufficient time. Therefore, in this study, two polymers are combined to obtain good film characteristics, especially residence time and mucoadhesive strength. This study was aimed to optimize Hydroxy Propyl Methyl Cellulose (HPMC) and Carbomer's amount in Diltiazem HCl mucoadhesive buccal film. The formulas were prepared by the solvent casting method and optimized with design expert software. The release kinetics and mechanism were evaluated using DDSolver program. The optimum amount of polymer obtained from optimization was 40 mg of HPMC and 10 mg of Carbomer. The optimum formula's swelling index was 4.18. The mucoadhesive strength was 53.07 gF, and the mucoadhesive residence time was 529.33 min. The FTIR spectra showed there was no interaction between Diltiazem HCl and other excipients. Thus it did not disturb the therapeutic effect. Based on the DDSolver statistical parameters and curve-fitting, the dissolution model of Diltiazem HCl from buccal mucoadhesive film follows Korsmeyer-Peppas. The release exponent (n) is 0.55, which shows a non-fickian/anomalous diffusion release mechanism. These mechanisms represent drug release controlled by a combination of diffusion and erosion
Antibiotic Consumption and Resistance Pattern of 3 Coagulase-Negative Staphylococci Species: An Ecological Study
Get PDFA group of coagulase-negative staphylococci (CoNS) was historically classified as a nonpathogenic bacteria. Over the last few decades, nosocomial infections caused by CoNS as opportunistic pathogens have increased and become one of the major nosocomial pathogens. The aim of this study was to identify the relationship between the use of an antibiotic agent for CoNS in Bali’s regional public hospital and the development of antibiotic resistance during 3 years period. This study was a retrospective ecological study of antibiotic resistance and antibiotic consumption secondary data collected prospectively. It was conducted over a three years period of inpatient data. Susceptibility of CoNS to antibiotics was obtained from the hospital antibiogram of all isolates from 2017 to 2019. Sensitivity results in antibiogram were based on the standards provided by the Clinical and Laboratory Standards Institute (CLSI) with the disk diffusion method. Antibiotic consumption in DDDs/100 bed-days. The relationships between DDDs/100 bed-days of each antibiotic and rates of antibiotic resistance of each resistant strain of CoNS were tested using Spearman correlation and logistic regression. There was no significant correlation between antibiotic consumption (DDD) and the percentage of antibiotic resistance among the three CoNS species (p>0.05). However, this study found there was an inverse relationship between DDD and antibiotic resistance in Staphylococcus hominis species (OR = 0.063; CI [0.004-0.915]; p=0.043). We conclude that no significant correlation between antibiotic consumption and antibiotic resistance of the 3 CoNS species. There needs to be further research to identify antibiotic consumption, antibiotic resistance and other factors affecting antibiotic resistance
Immunostimulant Activity of Marchantia paleacea Bertol. Herb Liverwort Ethanol Extract in BALB/c Mice
Get PDFImmunostimulants are compounds that can stimulate an immune response by increasing the activity of non-specific and specific components of the immune system (humoral and cellular) against certain infections and diseases. The liverwort plant species Marchantia paleacea Bertol. has long been used as a source of nutrition and empirical medicine. However, scientifically there is still not much research data on immunomodulators in these plants. This study aims to determine the activity of immunomodulators in the ethanol extract of the herb Marchantia paleacea Bertol. in male mice of BALB/c strain. Bioactive compounds from this plant were extracted by maceration method using 96% ethanol. Extract characterization and phytochemical screening were determined according to WHO guidelines and standard procedures from previous studies. The immunomodulatory activity of the extract was tested by carbon clearance method and lymphoid organ index (non-specific responses), primary and secondary antibody titer tests (humoral specific responses), IL-2 cytokine levels and IFN-ɣ from serum secondary antibodies and delayed-type hypersensitivity reaction/DTH (cellular specific response). The results of qualitative phytochemical screening contained flavonoid compounds, saponins, phenolics, tannins and steroids/triterpenoids. The results of the non-specific immune response immunomodulator test showed that the dose of 52 mg/kg bw had the largest phagocytic index of 1.52 which included strong immunostimulation (K > 1.5) and the organ spleen index of 0.55 ± 0.11 which increased significantly compared to the control (p<0.05). The data on the acquisition of specific immune responses in the primary and secondary antibody titer test in the three test extracts resulted in increased titer levels compared to the control and at a dose of 52 mg/kg bw could significantly increase the levels of IL-2 cytokines in the control group (p<0,05). Meanwhile, in the DTH test, doses of 13 and 26 mg/kg bw could significantly increase the thickness of the soles of mice compared to controls (p<0.05)
Phytosomes of Naphthoquinone Enriched Extract of Root bark of Onosma echioides Exhibit Wound Healing Activity in Rats
No full textThe present study is aimed at evaluation of phytosomal gel of the petroleum ether extract of root bark of Onosma echiodes for wound healing activity in rats. Extract of root bark of O. echioides was standardized by isolated naphthoquinone dimer using HPTLC. Phytosomes (equivalent to 2% w/w of naphthoquinones) of the standardized extract were prepared by thin film hydration technique. The wound healing efficacy of the formulation was evaluated in rats by inflicting excision and incision wounds followed by treatment of the wounds topically. The parameters evaluated for healing included determination of breaking strength and tensile strength of healed skin for incision model and percentage wound contraction, hydroxyproline content, granulation tissue free radicals and catalase in excision wound model. The formulation treated group showed a significant healing (p<0.005) of both the excision and incision wounds with respect to wound contraction and tensile strength respectively, as compared to vehicle treated group. The oxidative stress of the granulation tissue was also found to be reduced as indicated by reduced lipid peroxidation and increase in catalase activity. The phytosomal gel of O. echioides effectively exhibited wound healing effect
Development of New Isolation and Quantification Method of Piperine from White Pepper Seeds (Piper Nigrum L) Using A Validated HPLC
Get PDFMost of the active pharmaceutical ingredients in the pharmaceutical world are obtained from natural ingredients, one of which is white pepper. White pepper seeds (Piper nigrum L.) contain the main alkaloid compound piperine, which has a broad spectrum pharmacological effect. This research aimed to isolate the piperine compound from white pepper seeds to make piperine more economical, simple, and effective so that it can be applied to large scale production in the pharmaceutical industry. The method of extracting and purifying piperine compounds was carried out using n-hexane and cyclohexane. The results of the isolated piperine were tested for their purity with a set of melting point apparatus, bidimensional TLC, and HPLC. The structure compound was then analyzed using FTIR and NMR. Furthermore, the isolated piperine was tested for its antioxidant activities using DPPH, ABTS, and FRAP. Cyclohexane was successfully used to remove the resinous matter from the n-hexane extract of white pepper to produce isolated piperine with 97.24% of purity. The results of the melting point, FTIR, 1H-NMR, and 12C-NMR of the isolated piperine were similar to that of the piperine reference substance and the literature review. The isolated piperine has weak antioxidant activities in the ABTS and FRAP test with the results of 15.25 ± 0.004 mM and 10.53 mol TE/g of the sample, respectively. 
Self Nano-Emulsifying Drug Delivery System (SNEDDS) of Curcuma Mangga Val. Essential Oil and The Stability Study
Get PDFoai:jurnal.ugm.ac.id:article/584Essential oil of Curcuma mangga Val. has been reported to have cytotoxic effect against cancer cell lines. But this oil is unstable in dispensing so that a self nano-emulsifying drug delivery system (SNEDDS) of the oil was conducted to solve the problem and improve its potency. In the study, optimization, verification, characterization, and stability test of the SNEDDS formula were carried out respectively by simplex lattice design (SLD) on Design Expert ver. 10 software, droplet size and Zeta potential determinations using particle size analyzer (PSA) instrument, as well as heating-cooling and freeze-thaw methods.
The best SNEDDS formula resulted was Miglyol : Tween 80 : PEG 400 = 16.034% : 68.380% : 15.586%; with transmittance of 84.47 + 1.05%, droplet size of 15.75 nm, zeta potential of -8.54 mV, polydispersity index (PDI) of 0.188, emulsifying time of 49.67 + 1.7 seconds in distilled water, 24.33 + 4.19 seconds in artificial gastric fluid and 21.33 + 2.87 seconds in artificial intestine fluid. After a freeze-thaw test there was no change on the emulsion’s clarity, color, smell, as well as no separation, which means that the formula was stable thermodynamically.
The optimum SNEDDS formula resulted has small particle size, better emulsifying time in artificial gastric and intestine fluids, as well as better thermodynamic stability, which in turn will improve the cytotoxic activity of the Curcuma mangga Val. rhizome oil toward cancer cells
New Approaches to Sample Preparation and Integrated Spectroscopic Methods for The Identification of Polioxyethylene Triolate Sorbitane for Pharmaceutical Examination of Drugs
Get PDFDue to the fast pace of development of spectroscopic research methods in the pharmaceutical expertise of drugs presented in the United States Pharmacopeia (USP) and European Pharmacopoeia (Ph. Eur.), in this paper, we examined complex methods for the identification and preparation for analysis of polyethylene sorbitan trioleate. Two new systems were identified for purification of 98% polyoxyethylene sorbitan trioleate from organic impurities in column chromatography: acetonitrile 100% and acetonitrile/acetone 7.5/2.5. It was also revealed that a chamber with metallic iodine was the most suitable for selecting an eluent and controlling the cleaning by the TLC method. Proton NMR did not detect organic impurities. Identification of polyoxyethylene sorbitan trioleate was carried out on H1, C13, COSY, and IR spectra. These research methods are characterized by simplicity in sample preparation, the availability of reagents, the effectiveness of identification and quantification analyzes, and the efficiency in labor and material cost
Phytochemical Profile And Antioxidant Activity Of Guazuma ulmifolia Leaves Extracts Using Different Solvent Extraction
Get PDFGuazuma ulmifolia is one of the common tropical plants that has long been used as a traditional medicine to reduce body weight as slimming herbs and to lower the cholesterol in the body. The leaves of G. ulmifolia contain phenolics compound such as flavonoids and tannin that contributes to its biological activities. In this research, we determined the content of total phenolics, flavonoids, tannins, antioxidant activity, and FTIR spectrum profile from four extracts of G. ulmifolia leaves. The extraction method used in this study was stepwise maceration with different solvents n-hexane, ethyl acetate, ethanol, and water. The content of total phenolics and flavonoids were found high in ethanol extract of G. ulmifolia leaves with 35.42 and 44.85 mg QE/g dry powder, respectively. The highest content of total tannins was obtained in ethyl acetate extract of G. ulmifolia leaves as 0.55%. Antioxidant activity from four extracts of G. ulmifolia leaves was measured using DPPH, CUPRAC, and reducing power method. The highest antioxidant activity for DPPH and CUPRAC method was obtained in ethyl acetate extract with the antioxidant capacity as 55.47 and 98.17 µmol trolox/g dry powder, respectively. While using reducing power assay gives the capacity 176.75 µmol trolox/g dry powder in the water extract. The pattern of FTIR spectra from four extracts of G. ulmifolia leaves gives the distinct characteristics of each spectrum profile. Principal component analysis using FTIR spectrum shows good clustering for each extract with 94% data variability (PC1= 77% and PC2 = 17%). It can be concluded that each extract of G. ulmifolia leaves gives a distinct phytochemical profile (phenolics content, flavonoids, tannins, and FTIR spectrum) that contributes to the antioxidant activity. This antioxidant activity mainly influenced by the concentration of phenolic compounds, which is known to have antioxidant properties
The influence of Propylene glycol/Water and Ethanol/Water Binary Solvents on the in vitro Permeation of Garcinia mangostana L. Pericarp Extract across Shed Snakeskin
Get PDFGarcinia mangostana pericarp (GMP) has antioxidant activity thus may be developed into a topical antioxidant formulation. This research aimed to study the topical delivery of GMP extract. Initially, some commonly used topical solvents, i.e., water and binary solvents of propylene glycol (PG)/water and ethanol/water (0; 10; 20 and 40%), were used to dissolve GMP extract and further tested on GMP extract in vitro skin permeation using shed snakeskin. The influence of solvents' effects was evaluated based on radical DPPH scavenging activity and expressed as radical scavenging activity equivalent GMP Extract (RSGMPE). The results showed that RSGMPE could be delivered into shed snakeskin. The extent of RSGMPE shed snakeskin retention was similar among water and all PG/water or ethanol/water binary solvents. RSGMPE was also found in the receptor phase from all PG/water binary solvents, whereas that from ethanol/water solvents only shown from 20% ethanol/water solvent even though all ethanol-water solvents produced significantly higher RSGMPE compared to water and PG/water binary solvent