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Antibacterial Compound from Aspergillus elegans SweF9 an Endophytic Fungus from Macroalgae Euchema sp.
The antibiotic resistance of bacterial pathogens has become a serious health concern and encouragement to search for novel and efficient antimicrobial metabolites. On the other hand, endophytic fungi have great potential as a natural source for antimicrobial agents. The objective of this study was to isolation antibacterial compound from endophytic fungi of A.elegans SweF9. The fungus was stationarily cultured at 30°C for 12 days in potato malt peptone (PMP) medium, then extracted with ethyl acetate. The antibacterial activities of the extract were evaluated by agar well diffusion method against Gram-poitive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli) bacterial strains. The broth extract was able to inhibit the growth of E. coli, S. aureus and B. subtilis with antibacterial activity index compared to streptomycin sulfate were 84.6%, 91.6%, and 90% respectively. The active compound (1) was purified to yield amorphous white and identified using FTIR, NMR, and EI-MS analyses, revealed identified as (+) - epi-Epoformin. The compound showed an antibacterial activity index of E. coli, S. aureus and B. subtilis bacterial were 38%, 45%, and 47%, respectively. Based on these results endophytic fungi A. elegans SweF9 can be used as a new source of potential antibacterial compound
Phytochemical analysis, antioxidant, antibacterial and antidiarrheal activities of Limnophila repens
The study was carried out to determine the phytochemical content, antioxidant, antibacterial and antidiarrheal activity of methanolic extract of whole plant of Limnophila repens. The total phenolic, flavonoids, flavonols, tannins, β-carotene, lycopene, chlorophyll-α, and chlorophyll-β contents were found to be 65.21 ± 0.004 mg GAE/g , 44.83 ± 0.003 mg QE/g , 17.21 ± 0.002 mg QE/g, 56.27 ± 0.002 mg GAE/g , 1.32 ± 0.01 µg/g, 0.93 ± 0.012 µg/g, 11.85 ± 0.04 mg/g and 9.69 ± 0.037 mg/g, respectively. In vitro antioxidant potential of L. repens was assessed using various methods like by 2,2-diphenyl-1 picrylhydrazyl (DPPH), hydroxyl radical scavenging assay, reducing power assay, FRAP assay and thiobarbituric acid assay. IC50 values of the aforesaid tests were found to be 2.33 mg/ml, 442.31 µg/ml, 374 µg/ml, 55.09 µg/ml, and 4.30 mg/ml, respectively. The total antioxidant capacity was observed 140.7 ± 0.004 mg/g AAE. Aantibacterial activity of the methanolic extracts of whole plant of L. repens was evaluated using the disk diffusion method. The plant extract didn’t show any activity against Gram-positive (except Staphylococcus aureus) and Gram-negative bacteria. Finally, castor oil induced method was conducted to investigate the antidiarrheal activity of L. repens. At the dose of 400 mg/kg, the plant extract (35.62% inhibition of diarrhea) exhibited stronger effect compared to standard drug, loperamide (27.4% inhibition of diarrhea)
Formulation and Evaluation of Glipizide Tablets Utilizing Hibiscus Rosasinensis Leaves Mucilage
This research work aims to develop glipizide tablets using Hibiscus rosasinensis leaves mucilage. The mucilage was extracted by using double distilled water and precipitated with ethanol. The precipitated mucilage was dried and grounded into powder. The tablet utilizing the mucilage as excipient was prepared by wet granulation method. The tablets were subjected to various tests. The evaluatory parameters of tablets were found to be within the limits as per United States Pharmacopoeia NF 24/19. FTIR spectrum reveals that there is no incompatibility between the ingredients used. Diabetes was induced in wistar albino rats using streptozotocin and effect of formulation on blood glucose level was determined. It was observed that the formulation could not sustain the release of glipizide. However, the glipizide release was retarded as the amount of mucilage was increased. It was observed that on the completion of antidiabetic study, the formulation could bring the blood glucose level to normal in group rats. However, the blood glucose level was still elevated in group administered with pure gliplizide. It can be concluded that HRM can be used to formulate glipizide tablets. The formulations with HRM shows better hypoglycemic activity and this may be attributed to antidiabetic activity of Hibiscus rosasinensis.
Formulation of Insulin Self Nanoemulsifying Drug Delivery System and Its In Vitro-In Vivo Study
Particulate delivery system can be used for improving the efficacy of protein and peptide drug. In addition to a polymer-based particulate delivery system, self-nanoemulsifying drug delivery system (SNEDDS), a lipid-based delivery system, is currently developed for either less water-soluble or soluble drugs. This study aims to design SNEDDS for oral insulin administration and its in vitro-in vivo study. The SNEDDS template was designed using D-optimal mixture design and was analyzed using software Design Expert 7.1.5. The obtained optimum template was loaded with insulin and evaluated for its transmittance percentage, emulsification time, particle size, zeta potential, stability, the amount of insulin in vitro diffused across rat intestine, and insulin serum concentration after oral administration. The study results revealed that the optimum template of SNEDDS formula consisted of 10% (w/w) Miglyol 812N, 65% (w/w) Tween 80, and 25% (w/w) propylene glycol. These optimum template then was loaded with insulin and characterized. SNEDDS insulin has particle size of 12.0±1.7 nm, zeta potential of +0.16mV, transmittance of >90%, and emulsification time of < 60 seconds. The stability study showed that SNEDDS insulin was stable from both precipitation and phase separation. The amount of insulin transported from SNEDDS formula in vitro was 32.45±2.03% and non-SNEDDS formula was 10.44±5.04%. In vivo study of SNEDDS insulin produced a significantly increased Cmax, AUC, and F value than insulin non SNEDDS (p < 0.05). In brief, SNEDDS formulation in this study is a promising approach to increase the effectiveness of oral insulin. Insulin is better given orally in SNEDDS formulation than in non SNEDDS formulation
Formulation of Ketorolac Tromethamine for Controlled Release in Gastrointestinal and Colonic Delivery System
A suitable matrix system of ketorolac tromethamine (KTR) formulation has been developed with the aim of increasing the contact time, achieving controlled release, reducing the frequency of administration, improving patient compliance. In this concern an enteric-coated KTR matrix tablet intended for specific delivery of drugs to the colon by combining the use of a time dependent core with a pH-sensitive film coating. Eudragit L100, with a threshold pH 7, was selected as coating material. New formulation is proved to be noble as to KTR delivery through both gastrointestinal and colonic system. New formulation is considered to reduce gastrointestinal side effects and achieve high local drug concentration at the afflicted site in the gastro-intestine and colon.
Hypoglycemic Activity and Pancreas Protection of Combination Juice of Mengkudu (Morinda citrifolia Linn.) Juice and Temulawak (Curcuma xanthorrhiza Roxb.) Juice on Streptozotocin-Induced Diabetic Rats
Mengkudu fruit contains scopoletin and temulawak rhizome contains curcumin have been observed because they have strong antioxidant activity and they were used traditionally as antidiabetic. This research aimed to evaluate effect of antihyperglycemic and pancreas protection of juice combination of mengkudu fruit juice (MFJ) and temulawak rhizome juice (TRJ) on diabetes rats which were inducted with streptozotocin (STZ). Rats were grouped into 7 groups, each of group consisting 5 rats. Each of group was treated accordingly for 28 days except for a normal group of rats. Rats taken blood from the plexus retroorbitalis for examination of blood glucose levels every week. On the last day, rats blood was examined for malondialdehyde (MDA) levels. After that the rats were turned off for examination of pancreatic morphological conditions. The results showed that diabetic rats given MFJ-TRJ combination juice experienced a significant decrease in blood glucose levels, a significant decrease in MDA levels and improvement pancreas morphology when compared with the negative control group. The conclusion of this research was giving combination juice of MFJ-TRJ juice can decreased blood glucose level, decreased MDA level and can improved pancreas morphology condition
Derivatives of 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines as increasing efficiency substances
In today's society, especially in eastern countries such as China, Japan etc., the problem of fatigue and even death at work is acute. One of the solution to this problem is complex therapy with increasing efficiency drugs. Derivatives of 1,2,4-triazole have already proven themselves as potential compounds for pharmacological correction of fatigue. Compounds were synthesized at the Department of toxicological and inorganic chemistry ZSMU. Using method of forced swimming on a group of white nonlinear rats activity of anti-fatigue of the compounds were analyzed. Having analyzed the data of pharmacological correction of fatigue for 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-4-amines, it should be noted that this series of compound do not show anti-fatigue effect. Introduction in molecule 3- (nonylthio)-5-(thiophen-2-ylmethyl)-4H- 1, 2, 4-triazol-4-amine 4-fluorbenzylidene, 4-(dimethylamino) benzylidene, 4- methoxybenzylidene, 2-chloro-6-fluorobenzylidene radicals lead to increase actoprotective effect. The most active compound is N-(2-chloro-6-fluorobenzylidene)-3-(nonylthio)-5-(thiophen- 2- ylmethyl)- 4H- 1, 2, 4- triazol- 4-amine which exceeds the standard (riboxin)
Protective Effect of Ethanolic Extract Tempuyung Leaf (Sonchus arvensis L.) in Gentamicin-induced Acute Tubular Necrosis on Wistar Rats
Acute tubular necrosis (ATN) is the most common histopathologic findings of acute kidney injury (AKI). AKI is marked by the decrement of glomerular filtration rate, causing waste metabolism retention (creatinine). Gentamicin is used as it is the most common nephrotoxic agent in inducing ATN. Tempuyung (Sonchus arvensis L.) has been used in folklore medicine to ameliorate kidney problems as it contains antioxidants, two of which are flavonoid and phenolic acid. Yet, these active substances’ benefit on gentamicin induced ATN has not been investigated in Indonesia. This research aims to analyze protective effect of ethanolic extract tempuyung leaf (EET) on gentamicin-induced ATN based on histopathological study and creatinine serum level. True experimental laboratoric study was done with simple random design on male wistar rats, randomly divided into 4 groups (n=4). Control group (CMC 0.5% aquadest); Induction group (Gentamicin 80 mg/kgBW); 1st treatment group (EET 100 mg/kgBW + Gentamicin 80 mg/kgBW) and 2nd treatment group (EET 200 mg/kgBW + Gentamicin 80 mg/kgBW) for ten days. On the 11th day, blood was taken for creatinine measurement and kidneys collection for histopathological study. Histopathological examination on gentamicin-treated rats revealed degenerative changes in kidney tubules. Aside from that, gentamicin-treated rats also showed increment in creatinine serum level. Conversely, simultaneous administration of EET with Gentamicin ameliorated the nephrotoxic effects of gentamicin as confirmed from the significant improvement on histopathological changes and normalization of creatinine serum level. Co-administration of EET and gentamicin provides protection on gentamicin-induced ATN, based on histopathological feature and creatinine serum level
Cytotoxicity of Tetrahydropentagamavunon-0 (THPGV)-0 and Tetrahydropentagamavunon-1 (THPGV-1) in Several Cancer Cell Lines
Tetrahydropentagamavunon-0 (THPGV-0) and Tetrahydro-pentagamavunon-1 (THPGV-1), are analogs of a curcumin metabolite, tetrahydrocurcumin, and a derivate of Pentagama-vunon-0 (PGV-0) and Pentagamavunon-1 (PGV-1), respectively. THPGV-0 and THPGV-1 have been successfully synthesized and are investigated for their anticancer potency. Cytotoxic assays were performed toward several cancer cell lines to determine values of the IC50 against those cell lines. Assessing cytotoxicity in Vero normal cell line showed the selectivity of those compound. THPGV-1 showed highest cytotoxic activity in lymphoma Raji cells, a suspension cell line, with an IC50 of 180mM. Both THPGV-0 and THPGV-1 showed similar potencies in T47D breast cancer cell line with IC50 values of 250-270mM. Regardless their high selectivity, however, cytotoxic activities of THPGV-0 and THPGV-1 were lower compared to PGV-0 and PGV-1 in HeLa cervical, T47D breast, and WiDr colon cancer cell lines. Further study using different types of cancer cell lines and confirmation of cell viability by another assays and apoptosis detection may give more benefit.
Screening of Antibacterial and Anticancer Activity of Soft Corals from Togean Islands, Indonesia
Soft corals (Octocorallia, Alcyonaceae) have been reported to possess diverse biological activities and unique structural chemistry. This study aims to screen the potential antibacterial and anticancer activity of some soft corals collected from Togean Islands, Central Sulawesi, Indonesia. They were Lobophytum sp, Sarcophyton sp, Sinularia sp 1, and Sinularia sp 2. All dried coral materials were extracted for 3 x 24 h by maceration method using methanol and then evaporated by rotary evaporator to obtain viscous extracts. The determination of antibacterial activity had been performed by well agar diffusion method against Staphylococcus aureus and Escherichia coli. Meanwhile, the cytotoxic activity was performed by MTT method, followed by apoptosis annexin V-FTIC assay agains. Identification for the presence of terpenoids was performed by vacuum p-anisaldehyde-sulphuric acid spraying reagent on thin layer chromatography (TLC). Sinularia sp2 extract have strongly inhibited S. aureus and E.coli with the diameter of inhibition range from 12.76mm and 17.86mm, respectively. Moreover, Sinularia sp2 extract possessed also cytotoxic activity against human breast adenocarcinoma (MCF-7) and colorectal carcinoma (HCT-116) with the IC50 of 46.807 and 47.186 μg/mL, respectively. Extract Sinularia sp 1 was found to have strongest cytotoxicity on human colon colorectal carcinoma (HCT-116) with the IC50 of < 1.505 μg/mL. Annexin V-FTIC assay clearly exhibited that the apoptosis mechanism is proposed by the extracts of Sinularia sp1 and Sinularia sp 2. Terpenoids were identified on both extracts suggesting for further purification and isolation for the bioactive terpenoid compounds.