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Polyglactin surgical (PLGA) suture is a b biodegradable raidedsuture frequently used in clinical surgery. Due to its braided structure, polyglactin suture is easier contaminated by bacterial during surgery process. Thus, this study was coated by tannic acid (TA) to prevent Staphylococcus aureus binding. Suture surface modification was carried out by immersing PLGA in tannic acid- ferri chloride (TA-Fe) solution pH 8. The fabrication process was confirmed by FTIR analysis, and the antibacterial preventing activity was determined by bioinformatics analysis. Thus, this engineered suture increased the wettability in DI water, serum, and saline solutions, which could be promising to increase the biocompatibility in wound healing process. To sum up, our method would be applied in surgical suture to prevent bacterial infection and potentially elevate the biocompatibility by increasing wettability in biological solutions.

In the present work, we reported a successful synthesis and high antioxidant activity of C-alkylcalix[4]resorcinarene and C-alkylcalix[4]pyrogallolarene derivatives. The C-alkylcalix[4]resorcinarenes were prepared from a cyclization reaction of resorcinol and either pentanaldehyde or octanaldehyde in acidic condition. Meanwhile, the C-alkylcalix[4]pyrogallolarenes were prepared from a cyclization reaction of pyrogallol with pentanaldehyde or octanaldehyde. Four synthesized products, i.e. nBu-CR, nHep-CR, nBu-CP, and nHep-CP, were successfully prepared in 92.4-96.4% yield. The chemical structure of these products was elucidated by Fourier transform infrared (FTIR), liquid chromatography-mass spectrometry (LC-MS), and proton nuclear magnetic resonance (1H-NMR) analysis. The antioxidant activity assay of these compounds was evaluated through an in vitro assay employing 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. From the DPPH assay, it was found that the half-maximal inhibitory concentration (IC50) values of nBu-CR, nHep-CR, nBu-CP, and nHep-CP compounds were 25.1, 22.9, 11.5, and 21.9 µg mL-1, respectively. The IC50 value of the synthesized compounds was 2.0-4.3 times lower than the IC50 value of butylated hydroxytoluene (BHT) as the positive standard (49.9 µg mL-1), which is remarkable. This finding demonstrates that either C-alkylcalix[4]resorcinarenes or C-alkylcalix[4]pyrogallolarenes are better antioxidant agents than BHT. The nHep-CR compound was found as the best antioxidant agent from the other compounds due to weaker intramolecular and intermolecular hydrogen bonding as well as longer alkyl chain.

Dita Maria Virginia,1 Christine Patramurti,2 Fenty,1,3 Christianus Heru Setiawan,1 Jeffry Julianus,2 Phebe Hendra,1 Nicholas Adi Perdana Susanto3 1Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Sanata Dharma University, Yogyakarta, Indonesia; 2Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Sanata Dharma University, Yogyakarta, Indonesia; 3Bethesda Lempuyangwangi Hospital, Yogyakarta, IndonesiaCorrespondence: Dita Maria Virginia, Universitas Sanata Dharma, Mrican, Tromol Pos 29, Yogyakarta, 55281, Indonesia, Tel +62 274 513301, Fax +62 274 562383, Email virginia@usd.ac.idPurpose: This study aimed to explore the association of rs857148 A>C as 3ʹUTR variants with blood pressure, HbA1c profile, and lipid profiles as cardiometabolic parameters among patients with T2DM receiving metformin.Patients and Methods: This cross-sectional analytic research was conducted with 114 consecutively selected patients with T2DM. Polymerase chain reaction-restriction fragment length polymorphism was conducted to determine rs857148. A total of 108 patients fulfilled inclusion and exclusion criteria.Results: Genotype distribution agreed with the Hardy Weinberg Equation for Equilibrium (p> 0.05) but wildtype allele was found as the minor allele. Subjects with CC genotype and C allele had enhanced HbA1c levels (OR=7.12; 95% CI=1.05– 48.26; p=0.04; OR=1.66; 95% CI=1.06– 2.60; p=0.03, respectively). It was confirmed by dominant model whereas subjects with AA tended to have reduced HbA1c compared to AC+CC genotype (OR=0.15; 95% CI=0.02– 0.97; p=0.047). AC genotype had significant correlation to total cholesterol (OR=1.05; 95% CI=1.01– 1.10; p=0.03) compared to AA genotype.Conclusion: We conclude that polymorphism of rs87148, specifically CC genotype and C allele, has a significant association with HbA1c and total cholesterol after considering oral hypoglycemia agent dose, age, gender, and combination therapy, compared to AA genotype. Future studies that involve a larger sample population and more rigorous selection criteria are required.Keywords: PRKAA2, rs857148, 3ʹUTR, cardiometabolic, type 2 diabetes mellitus

The existence of a large number of mutant p53 in cancer cell nuclei gives a poor prognosis. However, mutant p53 existence creates a challenge to design a new anticancer compound targeted to mutant p53. The 3-carbethoxy-4-phenyl-but-3-en-2-one is a novel compound that was designed as an anticancer agent targeted to mutant p53. Further evaluation of this compound was done by in silico examination employing Auto Dock Vina as molecular docking software. Molecular docking results denoted that 3-carbethoxy-4-phenyl-but-3-en-2-one had lower binding energy than methylene quinuclidinone (MQ). Visual inspection of the docking results denoted that 3-carbethoxy-4-phenyl-but-3-en-2-one docked in the binding pocket crystal structures of mutant p53 (2BIM, 2J1Y, and 2J21), forming a hydrogen bonding or hydrophobic interaction with Cys-124, and the distance between double bonds of α, β-unsaturated of 3-carbethoxy-4-phenyl-but-3-en-2-one with –SH group of Cys-124 were shorter than MQ. These results demonstrated that 3-carbethoxy-4-phenyl-but-3-en-2-one is a promising ligand to mutant p53 in many types of mutations and predicted to have better activity than MQ as a mutant p53 reactivator especially in cancers with mutation type Arg-273-His and Arg-245-Trp.

Coronavirus disease 2019 (COVID-19) is still as global pandemic. No officially drugs to treat COVID-19 are available until now. Increasing number of patients and deaths trigger new antiCOVID-19 discovery efforts. In this study, we have conducted in silico screening employing molecular docking for Indonesian phytochemicals. Docking process was performed by employing AutoDock4 software on crystal structure 6VSB. Based on molecular docking results, several compounds had potential as antiCOVID-19 drugs, such as β-carotene, veramiline, ecliptalbine, betulinic acid, and lupeol. β-carotene was the most potential compound to treat COVID-19.

This study aimed to explore the association ofThis cross-sectional analytic research was conducted with 114 consecutively selected patients with T2DM. Polymerase chain reaction-restriction fragment length polymorphism was conducted to determineGenotype distribution agreed with the Hardy Weinberg Equation for Equilibrium (We conclude that polymorphism of

Carica papaya (papaya) leaf extract has been used for a long time in a traditional medicine to treat fever in some infectious diseases such as dengue, malaria, and chikungunya. The development of science and technology has subsequently made it possible to provide evidence that this plant is not only beneficial as an informal medication, but also that it has scientifically proven pharmacological and toxicological activities, which have led to its formal usage in professional health care systems. The development of formulations for use in nutraceuticals and cosmeceuticals has caused this product to be more valuable nowadays. The use of good manufacturing practice (GMP) standards, along with the ease of registering this product facilitated by policies of the national government, will absolutely increase the value of papaya leaf extract as a vital nutraceutical and cosmeceutical products in the near future. In this article, we review the potential of papaya leaf extract to be a high-value commodity in terms of its health effects as well as its industrial benefits.

Carica papaya (papaya) leaf extract has been used for a long time in a traditional medicine to treat fever in some infectious diseases such as dengue, malaria, and chikungunya. The development of science and technology has subsequently made it possible to provide evidence that this plant is not only beneficial as an informal medication, but also that it has scientifically proven pharmacological and toxicological activities, which have led to its formal usage in professional health care systems. The development of formulations for use in nutraceuticals and cosmeceuticals has caused this product to be more valuable nowadays. The use of good manufacturing practice (GMP) standards, along with the ease of registering this product facilitated by policies of the national government, will absolutely increase the value of papaya leaf extract as a vital nutraceutical and cosmeceutical products in the near future. In this article, we review the potential of papaya leaf extract to be a high-value commodity in terms of its health effects as well as its industrial benefits.

Overexpression of mutant p53 in cancer cell inactivates the p53 pathways to execute apoptosis and cell cycle arrest. This study aimed to synthesize new kardiena derivative compound, 3-carbethoxy-4(3’-chloro-4’-hydroxy)phenyl-but-3-en-2-one, to reactivate the p53 pathways to execute apoptosis and cell cycle arrest. Characterization of the synthetic compound employing melting point, IR, EI-MS, 1H-NMR, and 13C-NMR spectra revealed 3-carbethoxy-4(3’-chloro-4’-hydroxy)phenyl-but-3-en-2-one was successfully synthesized from 3-chloro-4-hydroxybenzaldehyde and ethyl acetoacetate using dimethylamine as a catalyst. This compound had antiproliferative activity against the WiDr cells which carried mutant p53. Its antiproliferative activity was better than 5’-FU as a reference standard to treat colon cancer. Increasing WiDr cell accumulation in the G2-M phase, the active form of caspase-3, and inducing apoptosis demonstrated the ability of 3-carbethoxy-4(3’-chloro-4’-hydroxy)phenyl-but-3-en-2-one to reactivate p53 pathways to execute apoptosis and cell cycle arrest in cancer cells carrying mutant p53.

Previous studies have reported that compounds bearing an arylamide linked to a heterocyclic planar ring have successfully inhibited the hemopexin-like domain (PEX9) of matrix metalloproteinase 9 (MMP9). PEX9 has been suggested to be more selectively targeted than MMP9's catalytic domain in a degrading extracellular matrix under some pathologic conditions, especially in cancer. In this study, we aim to synthesize and evaluate 10 arylamide compounds as MMP9 inhibitors through an enzymatic assay as well as a cellular assay. The mechanism of inhibition for the most active compounds was investigated via molecular dynamics simulation (MD). Molecular docking was performed using AutoDock4.0 with PEX9 as the protein model to predict the binding of the designed compounds. The synthesis was carried out by reacting aniline derivatives with 3-bromopropanoyl chloride using pyridine as the catalyst at room temperature. The MMP9 assay was conducted using the FRET-based MMP9 kits protocol and gelatin zymography assay. The cytotoxicity assay was done using the MTT method, and the MD simulation was performed using AMBER16. Assay on MMP9 demonstrated activities of three compounds (2, 7, and 9) with more than 50% inhibition. Further inhibition on MMP9 expressed by 4T1 showed that two compounds (7 and 9) inhibited its gelatinolytic activity more than 50%. The cytotoxicity assay against 4T1 cells results in the inhibition of the cell growth with an EC50 of 125 μM and 132 μM for 7 and 9, respectively. The MD simulation explained a stable interaction of 7 and 9 in PEX9 at 100 ns with a free energy of binding of -8.03 kcal/mol and -6.41 kcal/mol, respectively. Arylamides have potential effects as selective MMP9 inhibitors in inhibiting breast cancer cell progression.

The annual number of cancer deaths continues increasing every day; thus, it is urgent to search for and find active, selective, and efficient anticancer drugs as soon as possible. Among the available anticancer drugs, almost all of them contain heterocyclic moiety in their chemical structure. Xanthone is a heterocyclic compound with a dibenzo-γ-pyrone framework and well-known to have “privileged structures” for anticancer activities against several cancer cell lines. The wide anticancer activity of xanthones is produced by caspase activation, RNA binding, DNA cross-linking, as well as P-gp, kinase, aromatase, and topoisomerase inhibition. This anticancer activity depends on the type, number, and position of the attached functional groups in the xanthone skeleton. This review discusses the recent advances in the anticancer activity of xanthone derivatives, both from natural products isolation and synthesis methods, as the anticancer agent through in vitro, in vivo, and clinical assays.

Synthesis and physicochemistry properties prediction of a potential anti-inflammatory agent, diacetyl pentagamavunon-1 (diacetyl PGV-1), has been done. The synthesis was using pentagamavunon-1 (PGV-1) (2,87x10-3 mole) and anhydride acetic acid (26x10-3 mole; 37x10-3 mole; 49x10-3 mole) as starting materials and NaOH ethanolic as a catalyst. The AM1 semiempirical quantum-chemical calculations using the computational chemistry approach was used to predict and compare the physicochemisty properties of diacetyl PGV-1 to PGV-1. Odorless, light-yellow powder has been obtained. The powder was 0.8512-0.9602 g (2.02 x10-3 - 2.22x10-3 mole; 70.4-77.4%) and the purity of the powder was 92.4%. The purity of the product has been examined by high performance liquid chromatography (HPLC), while the structure elucidation has been done using IR (Infra Red), 1H-NMR (Nuclear Magnetic Resonance) and MS (Mass Spectroscopy). The physicochemisty properties prediction showed that diacetyl PGV-1 was more hydrophobic than PGV-1. Keywords: Anti-inflammatory, PGV-1, diacetyl PGV-1, AM1

Objective: To investigate the antihyperlipidemic, anti-inflammatory and analgesic properties of of E. longifolia root extract in animal models. Methods: In this study, glucose-fructose enriched diet-induced hyperlipidemia, carrageenan-induced paw edema and acetic acid-induced writhing were used to evaluate the anti-hypertriglyceridemia, anti-inflammatory and analgesic activities, respectively. At the end of the experiment of glucose-fructose enriched diet-induced hyperlipidemia, blood samples were collected and estimation of blood lipids were carried out. Edema thickness was measured using digital caliper at 0, 15, 30, 45, 60, 90, 120, 150, 180, 210, 240, 270, 300, 330, and 360 min after carrageenan injection. The number of abdominal writhing for each mouse was observed and counted during a period of 1 h post injection of acetic acid. Results: E. longifolia root extract demonstrated a significant reduction of triglyceride levels ( p

Objective: This study investigated the antihyperlipidemic and hepatoprotective effects of the hexane-ethanol fraction of methanol extract of Macaranga tanarius (HEM) in rats. Methods: The hexane-ethanol fraction was screened for toxicity by oral acute toxicity study. The antihyperlipidemic effect of the hexane-ethanol fraction and the unsolved of the hexane-ethanol fraction is measured against Wistar rats induced by glucose-fructose diets for 42 days through measuring serum cholesterol, triglyceride (TG), high-density lipoprotein cholesterol (HDL-c), low-density lipoprotein cholesterol (LDL-c), and fasting blood glucose. The hepatoprotective effect of the hexane-ethanol fraction is determined against Wistar rats with liver damage induced by carbon tetrachloride through measuring serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP), albumin, lactate dehydrogenase (LDH), and total bilirubin. R esults: There is no toxic effect that was observed on acute toxicity study. The TG, LDL-c, and fasting blood glucose levels were significantly (p