Indonesian Journal of Pharmacy
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Natural Bioactive Cyclopeptides from Microbes as Promising Anticancer Drug Leads: A Mini-review
Get PDFNatural products from microbes are a rich source of bioactive molecules to serve as drug leads, predominantly in cancer therapy. Peptides are among the essential nature-derived biomolecules. Owing to their great diversity and favorable characteristics, cyclic peptides (cyclopeptides) from natural sources have become a propitious lead candidate for the development of therapeutics, including anticancer drugs. This present mini-review highlights cyclopeptides from microbial-derived natural products that have demonstrated significant cytotoxicity or anticancer activities. Moreover, this mini-review also provides a look into the mode of action of anticancer cyclopeptides. Selected examples are given for the potent anticancer cyclopeptides isolated in the recent decade from fungi and bacteria from both terrestrial and marine origins. Naturally occurring cyclopeptides with canonical and non-canonical amino acids isolated from fungi, myxobacteria, actinomycetes, marine cyanobacteria, and microbes associated with marine organisms and their anticancer activity are featured herein
LC-MS/MS and Cytotoxic Activity Analysis of Extract and Fraction of Calophyllum soulattri Stembark
No full textCalophyllum soulattri (Sulatri), a plant from Clusiaceae family, has been empirically used as traditional medicine. In the present study, C. soulattri stem bark extract and fractions were evaluated for their toxicity against MCF-7 breast cancer cell. The extract and fraction’s chemical content was analyzed using the combination of liquid chromatography with mass spectrometry (LC-MS/MS). The results showed that methanol extract and n-hexane fractions have strong cytotoxic activity with IC50 values 93.6 and 36 µg/mL, respectively. Meanwhile, as the positive control, ethyl acetate and cisplatin fractions have IC50 values 233 and 16.2 µg/mL, respectively. The LC-MS/MS analysis showed that the extract and fractions contained polyporusterone A, poricoic acid D, polyporusterone F, esulentagenin, and 1-acetyl-3-(methoxy-carbonyl)-β-carboline. Therefore, C. soulattri stem bark extract and fractions have potential activity as an anticancer agent that was able to inhibit MCF-7 breast cancer cell growth.
 
Formulation And Antioxidant Property Of Bitter Melon Seeds Oil Loaded Into SNEDDS Systems As A Nutraceutical
No full textBitter melon seeds oil is less soluble in the gastrointestinal tract and has low absorption. Therefore, a self-nanoemulsion dosage form needed to support its absorption and increase its stability. This study aimed to formulate bitter melon seeds oil into a self-nano emulsifying drug delivery system (SNEDDS) and evaluate its antioxidant activity using the Ferric Reducing Antioxidant Power (FRAP) method. The SNEDDS formulation uses bitter melon seed oil as the active ingredient and the oil phase, cremophor RH 40 as a surfactant, and glycerin as a co-surfactant. The results showed that the best SNEDDS formula obtains a ratio of oil: Smix (surfactant mixture) of 1:4. The best formula transmittance was 97.35 ± 0.04% with an emulsification time of 15.69 ± 0.06 seconds, a pH value of 6.87 ± 0.08, and a particle size of 31.8 ± 16.3 nm. Thermodynamic stability and robustness to dilution tests show the preparation is stable and resistant to various dilutions and pH. The antioxidant activity of bitter melon seed oil before and after being formulated into SNEDDS resulted in 62.73% and 50.31% reducing power. This result is not differences significantly. This study concluded that bitter melon seeds oil SNEDDS has good physical characteristics, stability, and no antioxidant activity changes
The Effects of Soyferment-Tempeh on Lipid Profile, Retinol-Binding Protein 4 (RBP4), and Phosphoenolpyruvate Carboxykinase (PEPCK) Gene Expression in Type 2 Diabetic Mice
No full textDiabetes Type 2 can cause oxidative stress leading to the accumulation of reactive oxygen species. Soyferment-Tempeh, a fermented soybean product with aerobic and anaerobic R. oligosporus incubation has a high antioxidant content of isoflavones that can regulate oxidative stress in diabetes. In this study, we evaluate the effects of Soyferment-Tempeh on lipid profile, Retinol-Binding Protein 4 (RBP4), and Phosphoenolpyruvate Carboxykinase (PEPCK) gene expression in type 2 diabetic mice. A total of 30 mice with the age of eight weeks were divided into six groups as follows: A) nondiabetic, B) diabetic mice, C) diabetic mice with metformin, D), E), and F) diabetic mice with Soyferment-Tempeh doses of 10, 20, or 40mg/100g body weight (BW), respectively, were administered treatments orally by gavages. Blood was collected for assessment of blood glucose level, and lipid profile before and after 3 weeks of the administration. After sacrificing the mice, livers were used for RBP4 and PEPCK gene expression assessment. Supplementation with three different doses of Soyferment-Tempeh in streptozotocin-induced diabetic mice for 21 days significantly (p<0.001) reduced blood glucose level, total cholesterol, triglycerides, low-density lipoprotein level, atherogenic index, and increased high-density lipoprotein level. There was a significant decrease in RBP4 gene expression in the Soyferment-Tempeh of dose 10mg/100g BW treatment groups (p<0.05), while the PEPCK gene expression did not significantly differ (p>0.05). These results demonstrate that supplementation with Soyferment-Tempeh decreases blood glucose level, atherogenic index, improves lipid profile, and decreases RBP4
Bioactive fractions from Streptococcus macedonicus MBF 10-2 produced in an optimized plant-based peptone medium fermentation
No full textPostbiotic fractions of several lactic acid bacteria have potential as microbial therapeutics for skin health and may also appeal to consumers who wish to avoid animal-based products. We aim to establish the optimum plant-peptone fermentation of Streptococcus macedonicus MBF10-2, which possess Bacteriocin Like-Inhibitory Substance activity in our previous study, to produce bacterial bioactive fractions. We evaluate their potential antibacterial and antioxidant actions, and as well assess the preliminary safety for human skin application. Fermentation was carried out by using plant peptone modified MRS, i.e., soy peptone and Vegitone, a non-animal-carbon sources that substitute proteose peptone in MRS medium. Fractions of MBF10-2 lysate and cell-free supernatant were collected and processed as follows, i.e. cell disruption, fraction separation and fractions freeze-drying. Fractions were confirm for antibacterial properties by the agar well diffusion method and assess for antioxidant activity using DPPH, while safety assessment was carried-out by skin patch assay. Maximum growth of MBF10-2 achieved by fermentation in soy peptone- and in Vegitone-modified media was 9.00 and 7.99 g total cell mass, respectively. The antibacterial property of fractions was most effective against Micrococcus luteus T18. The lysate fraction exhibited a mild antioxidant potency (IC50 840 µg/mL), and all bioactive fractions were proven safe and non-allergenic for human skins. Strep. macedonicus MBF10-2 postbiotics bioactive fractions were indicated as being safe for topical application. This is the first report on the production of a safe Strep. macedonicus bioactive postbiotic possessing mild antibacterial and mild-to-weak antioxidant. 
Bioactivity Screening of Endophytic Fungus Eutypa linearis isolated from Coleus amboinicus (Lour.)
Get PDFColeus amboinicus (Lour.) is a medicinal plant containing various bioactive compounds. Endophytes are microorganisms living inside intracellular tissue of plants and known as the source of bioactive compounds. In order to explore the potential of endophyte in producing novel bioactive compounds, this study focused on isolating endophytic fungi from the leaves of C.amboinicus, characterisation and screening their metabolite bioactivity during submerged culture fermentation. Isolation of endophytic fungi from the leaves segment of C.amboinicus was conducted on PDA media and fungus identification was carried out by analyzing its morphology and molecular examination. The production of metabolites was examined using thin layer chromatography and gas chromatography. Identification of the endophytic fungus showed 98.84% similarity with Eutypa linearis. This species was fermented submergedly in PDB medium for 14 days under dark and exposed to light and the fermentation broth was extracted using ethyl acetate. The results showed that exposure to the light did not significantly influence metabolite production. The ethyl acetate extract exhibited antioxidant and cytotoxic activities. Antioxidant activity of this extract as examined by DPPH assay showed IC50 of 105.31 ± 2.11 µg/mL. Cytotoxic activity against Hela cell line was known to be the best among other cell lines (IC50 301.53 ± 11.34 µg/mL) although it was found to be non selective (SI<1). The extract contained five major compounds namely Benzenemethanol, 4-nitro-(CAS) p-Nitrobenzyl alcohol; 2-Pentadecanone (CAS) Pentadecan-2-one; (1R*,6S*,10R*)-5,5-Dimethyl-11,12-dioxatricyclo[8.2.1.0(1,6)] tridecan-10-ol; 9,12-Octadecadienoic acid (Z,Z)-, methyl ester (CAS) Methyl linoleate; and 3-Furanacetic acid, 4-hexyl-2,5-dihydro-2,5-dioxo- (CAS) 2-carboxymethyl-3-N-hexyl-maleic anhydride
Beetroot Extracts as Haematopoietic Agents on Rats
Get PDFIntroduction: Beetroot (Beta vulgaris L.) contains flavonoid compounds that play a role in the haematopoietic process. It is known that methanol extract of beetroot has benefits in the process of haematopoiesis in normal white rats. Aims: To evaluate the beetroots extracts as hematopoietic agents on male rats. Methods: Beetroots dried powder was divided into two parts. One part was macerated separately with dichloromethane and 70% ethanol, while the other part is added with citric acid and washed with water to remove alkaloids and then extracted with 70% ethanol. The study used 24 rats which were divided into four groups. Each group consisted of 6 rats, namely the normal group, dichloromethane extract group, ethanolic extract group, and free alkaloids-ethanolic extract group. Each extract was given at a dose of 200 mg.Kg-1 for 21 days. Analyzed blood parameters are erythrocytes, haemoglobin, MCV, MCH, MCHC, leukocytes, and platelets. The data obtained consisted of the number of cells analyzed using one-way ANOVA then obtained by the Tukey test. Results: This study showed a significant increase in the number of erythrocytes, haemoglobin, MCV, MCH, MCHC, leukocytes, and platelets in rats that were given each extract compared to the normal group (p <0.05). The ethanolic extract of beetroot can increase erythrocytes, haemoglobin, MCV, MCH, MCHC, leukocytes, and platelets by 41.49%, 24.95%, 14.92%, 33.54%, 27.19%, 59.40%, and 35.37%, respectively. Conclusions: The ethanolic extract of beetroot has the potential as a good natural haematopoietic agent
Acute and Sub-Chronic Toxicity Study of 1-(2, 5-Dihidroxyphenil)-3- Pyridine-2-Il-Propenone In Adult Female Mice
Get PDFThis research aimed to evaluate the toxicity of 1-(2, 5-dihidroxyphenil)-3-pyridine-2-il-propenone (DPP) after 24 hours and 90-day administration in female mice. Acute toxicity test was performed using the OECD 423 method, and DPP was administered once a day at doses of 300, 2000, and 5000 mg/kg body weight (BW). Toxic symptoms were observed after 24 hours of administration, and this continued until the 14th day. The experimental animals were dissected and examined for histological organs on the 15th day. The sub-chronic toxicity test was performed using the OECD 408 method, and DPP at 14, 28, and 56 mg/kg/day was administered for 90 days. Toxic symptoms were observed every day, and the amount of food and water intakes were also measured. Furthermore, statistical analysis was performed, and changes in body weight as well as routine blood checks and biochemistry were observed. At the end of the study, experimental animals were killed and the vital organs' weights were examined before their histological analysis. The results showed that DPP at 300-5000 mg/kg/day and 14-56 mg/kg/day for 90 days did not show any toxic symptom respectively. In the sub-chronic toxicity test, no change was observed in blood and urine biochemical parameters (p≥0.05). However, lymphocytic infiltration in the liver and congested vessel in the kidney occurred after administration at 56 mg/kg / day. The results showed that the acute toxicity of DPP is at category 5 according to Globally Harmonized Classification System and sub-chronic toxicity is at a dose below 56 mg/kg/day
Mutation of Gyra Gene Found In Mycobacterium Leprae From Leprosy Patient In West Papua and Papua, Indonesia
No full textCases of leprosy in Indonesia are still high, especially in the provinces of West Papua, North Maluku and Papua. Drug resistance surveillance and typing strains of Mycobacterium leprae are useful molecular tools for leprosy control especially in the three Provinces. The purpose of this study was to identify mutations in the gyrA M. leprae gene obtained from leprosy patients in the provinces of West Papua and Papua on a molecular basis. M. leprae samples obtained from leprosy patients were extracted and continued with PCR and sequencing in the M. leprae gyrA gene. The sequencing results are aligned with M. leprae TN sequences to identify mutations. The phylogenetic tree was constructed using Mega 7 to get the M. leprae gyrA cluster. The RNAalifold server was employed to generate the conserved 2D structure for the gyrA MSAs. Six variants were found in the gyrA M. leprae obtained from the provinces of West Papua and Papua. The six variants are H71R, K73R, D95G, A101T, R107W, A127V. The existence of mutations in the gyrA M. leprae gene found in this study can be information in the treatment of leprosy in Papua if using Ofloxacin as an alternative treatment. Based on phylogenetic analysis found there are three distinct clusters of gyrA gene. The five variants are H71R, K73R, A101T, R107W, A127V are new variant of gyrA M. leprae. The D95G variant has been confirmed to cause resistance to Fluoroquinolone by in vitro methods, while the H71R, K73R, A101T, R107W, A127V variants are new variants whose effects on the fluoroquinolone are unknown. Thus, further analysis is needed to study the effects of the five variants on ofloxacin
Evaluation of a Hand Antiseptic with WHO-Recommended Formulation and Its Efficacy in Killing Methicillin-Resistant Staphylococcus Aureus (MRSA)
Get PDFThe present pandemic that is caused by COVID-19 and previously by the clone of the methicillin-resistant staphylococcus aureus (MRSA) has threatened human life. This condition requires materials that can break the chain of transmission from human to human and from the environment to human. This study aimed to evaluate the quality of alcohol-based hand antiseptic using WHO-recommended formulation based on the stability of the formulation, the risk of irritation, and the ability to kill bacteria. Assessments on the presence of rancidity, clarity, discoloration, final alcohol content, and skin irritation risk were done to know the quality of the product. Methicillin-resistant staphylococcus aureus (MRSA) was used to assess the percentage of bacterial killing power. The selected bacteria were bacteria that are commonly found in the hospital environment. The results showed that from four variants tested, MK.IV had good stability compared to other formulations. In terms of irritation risk, twenty-three selected subjects could well tolerate the formula. The results of the killing efficacy against MRSA showed that the antiseptic could kill 99.90% of the bacteria at the 1st, 2nd, and 5th minute. A selected manufacturer's product also showed the same killing efficacy at the 1st, 2nd, and 5th minute. The effective value of the antiseptic for each contact time was ≥ 90%