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The topical therapy with rifampicin (RF)-based formulations is beneficial for treating postoperative wound infections and to accelerate healing. Despite recent research highlighting the antibiotic's significant anti-inflammatory properties, limited topical wound healing products are currently available. The present study aimed to prove that the newly synthesized nanoparticles based on grafted alginate and poly(N-vinylcaprolactam) (pNVCL) and poly-lactic-co-glycolic acid (PLGA) contribute to the healing process of a wound. The methods used were at first the synthesis of the copolymer of alginate and pNVCL via grafting from technique and radical polymerization followed by water-in-oil-in water (W/O/W) emulsification; as oil phase PLGA dissolved in dichloromethane (DCM) was used. The formed nanoparticles were than characterized. The loaded RF was determined to be 160 µg/mL for a 20 mg formulation and within a four-hour time frame approximately 10% of the total loaded amount was released. The inhibitory concentrations (IC50) were 192.1 µg/mL for the nanoparticle, 208.8 µg/mL for pure rifampicin, and 718.1 µg/mL for the rifampicin-loaded nanoparticles. Considering the double role rifampicin was used for, the result was considered satisfactory in the way that these formulations could be used predominantly for postoperative wound irrigation in order to avoid infections and to improve healing. [ABSTRACT FROM AUTHOR]

Thallium (Tl) is a highly toxic heavy metal whose mechanism of toxicity is still not completely understood. The aim of this study was to test Tl cytotoxicity on several cell lines of different tissue origin in order to clarify specific Tl toxicity to a particular organ. In addition, possible interference of Tl with cell potassium (K) transport was examined. Human keratinocytes (HaCaT), human hepatocellular carcinoma (HepG2), porcine kidney epithelial cells (PK15), human neuroblastoma (SH-SY5Y) and Chinese hamster lung fibroblast cells (V79) were treated with thallium (I) acetate in a wide concentration range (3.9–500 µg/mL) for 24 h, 48 and 72 h. To assess competitive interaction between Tl and K, the cells were treated with four Tl concentrations close to IC50 (15.63, 31.25, 62.50, 125 µg/mL) in combination with/or without potassium (I) acetate (500 µg/mL). The cells' morphology was monitored, and cytotoxic effect was assessed by 3-(4, 5-dimethylthiazole-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) test. The most sensitive to Tl exposure were SH-SY5Y cells, while HepG2 were the most resistant. The combined exposure to thallium (I) acetate and potassium (I) acetate for every cell line, except V79 cells, resulted in higher cell viability compared to thallium (I) acetate alone. The results of our study indicate that cell sensitivity to Tl treatment is largely affected by tissue culture origin, its function, and Na+/K+-ATPase activity. [ABSTRACT FROM AUTHOR]

Background: The study investigates the antioxidant properties of Catharanthus roseus, focusing on identifying its antioxidant compounds and chemical constituents. We compare antioxidant activities across its root, stem, flower, and leaf and examine the inhibition of reactive oxygen species (ROS)–generating enzymes by the plant's phytocompounds. Methods: We conducted a comprehensive analysis that included proximate analysis, mineral content assessment, and in vitro antioxidant characterization of various plant parts—root, stem, flower, and leaf. The levels of bioactive phytochemicals in both ethanol and mixed‐solvent extracts of Catharanthus roseus were quantified using high‐performance liquid chromatography with a diode array detector (HPLC‐DAD). Additionally, we performed molecular docking studies to explore the interactions of quantified phytocompounds. Results: HPLC‐DAD analysis quantified catechin hydrate, catechol, (−) epicatechin, rutin hydrate, trans‐cinnamic acid, quercetin, vanillic acid, kaempferol, and trans‐ferulic acid in Catharanthus roseus. Despite the ethanol extract having higher total antioxidant properties and flavonoid content, the mixed‐solvent extract exhibited higher EC50 for reducing power and lower IC50 for ABTS, 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH), and metal chelating activities. Molecular docking studies indicated that compounds such as catechin, rutin, epicatechin, quercetin, and kaempferol significantly inhibit the ROS‐generating enzyme microsomal prostaglandin E synthase 1 (mPGES‐1). Conclusions: The mixed‐solvent extract had higher levels of catechin hydrate, rutin hydrate, trans‐ferulic acid, and vanillic acid, whereas the ethanol extract contained more (−) epicatechin, catechol, kaempferol, quercetin, and trans‐cinnamic acid. While the extracts displayed antioxidant activity, the phytoconstituents also inhibited ROS‐generating mPGES‐1. These results identify key compounds with potential for developing new chemotherapeutic agents against ROS. [ABSTRACT FROM AUTHOR]

Cytochrome P450 enzymes (CYPs) play a crucial role in phase I metabolic reactions. The activity of CYPs would affect therapeutic efficacy and may even induce toxicity. Given the complex components of traditional Chinese medicine, it is important to understand the effect of active ingredients on CYPs activity to guide their prescription. This study aimed to evaluate the effect of polyphyllin H on the activity of CYPs major isoforms providing a reference for the clinical prescription of polyphyllin H and its source herbs. The effects of polyphyllin H were evaluated in pooled human liver microsomes using probe substrates of CYP1A2, 2A6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 to determine their activities. The Lineweaver‐Burk was used to model the inhibition, and a time‐dependent inhibition experiment was performed to understand the characteristics of the inhibition. Polyphyllin H significantly suppressed the activity of CYP1A2, 2D6, and 3A4 with IC50 values of 6.44, 13.88, and 4.52 μM, respectively. The inhibition of CYP1A2 and 2D6 was best fitted with a competitive model, yielding the inhibition constant (Ki) values of 3.18 and 6.77 μM, respectively. The inhibition of CYP3A4 was fitted with the non‐competitive model with the Ki value of 2.38 μM. Moreover, the inhibition of CYP3A4 was revealed to be time‐dependent with the inhibition parameters inhibition constant (KI) and inactivation rate constant (Kinact) values of 2.26 μM−1 and 0.045 min−1. Polyphyllin H acted as a competitive inhibitor of CYP1A2 and 2D6 and a non‐competitive and time‐dependent inhibitor of CYP3A4. [ABSTRACT FROM AUTHOR]

Copyright of Indonesian Fisheries Processing Journal / Jurnal Pengolahan Hasil Perikanan Indonesia is the property of IPB University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Hyptis capitata Jacq. known as Sumambu plants in Sulawesi, has phytopharmaceutical importance. H. capitata extracts were evaluated for their phytochemical properties, antioxidant activity, and cytotoxicity. Using the maceration yielded five types of extracts: root chloroform (RC), root methanol (RM), leaf chloroform (LC), leaf methanol (LM), and leaf ethanol (LE). Phytochemical properties were identified by qualifying procedure and digital image analysis for quantifying Red-Green-Blue (RGB) percentage and hex colour code. 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay was used to determine the half-maximal inhibitory concentration (IC50). Cytotoxicity screening of each extract was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against HeLa and 4T1 cells. Gas Chromatography-Mass Spectrometry (GC-MS) assay was used to identify the phytochemical compounds of the extracts with the most promising potential. Alkaloids were the major constituents of the phytochemicals of RC, RM, LE, LC, and LM. RM and LM have potency and weak free radical scavenging activities, with IC50 value 31.08 and 58.03 µg/mL, respectively. The IC50 of RC and RM against HeLa cells were 84.21 ± 0.63 and 172.10 ± 02.90 µg/mL, respectively. Meanwhile, the cytotoxicity of RC and RM against 4T1 cells were 86.42 ± 0.80 and 182.82 ± 7.00 µg/mL, respectively. It means RC and RM exhibit a moderate level of cytotoxicity in both HeLa and 4T1 cells. LM shows moderate cytotoxicity, but it is limited to 4T1 cells with an IC50 value of 181.86 ± 12.68 µg/mL. The cytotoxicity level of extracts was lower than doxorubicin. Campesterol, ferruginol, stigmasterol, cis-13-octadecenoic acid methyl esters, and methyl palmitate were predicted to play a role in the antioxidant activity and cytotoxicity of RC, RM, and LM. RC, RM, and LM possess the potential for development as anticancer agents. Moreover, RM shows promise as an antioxidant due to its notable radical scavenging activity. Further research is required to explore the cytotoxic effects of RC, RM, and LM on normal cells and to assess their toxicity in experimental animals. [ABSTRACT FROM AUTHOR]

Introduction: The intergovernmental organizations Organisation for Economic Co-operation and Development (OECD) and Interagency Coordinating Committee on the Validation of Alternative Methods (ICCVAM) have developed guidelines for the use of in vitro models for toxicological evaluation of chemicals. However, the presence of manual steps and the requirement of multiple tools for data analysis, apart from being costly and time-consuming, can inadvertently introduce errors by researchers. Objectives: We have developed the SAEDC platform (Technological Solution for Exploratory Data Analysis and Statistics for Cytotoxicity, in Portuguese), which enables analysis of cytotoxicity data from assays following OECD Guideline No. 129. Methodology: In vitro experimental data were used to compare with the analysis methodology suggested in the Guideline. We analyzed 117 data sets covering chemicals from Category I to Unclassified according to GHS classification. Results: The four-parameters of non-linear regression (4PL) calculated by the SAEDC platform showed no significant differences compared to standard methodology in any of the data sets (p > 0.05). The coefficient of determination (R-squared) also demonstrated not only a good fit of the 4PL model to the data but also significant similarity to values obtained by the conventional methodology. Finally, the SAEDC platform predicted LD50 values for the chemicals from IC50, using the Registry of Cytotoxicity (RC) regression models. Conclusion: The comparison with the standard data analysis methodology revealed that SAEDC platform fulfills the requirements for cytotoxicity data analysis, generating reliable and accurate results with fewer steps performed by researchers. The use of SAEDC platform for obtaining toxicity values can reduce analysis time compared to the standard methodology proposed by regulatory agencies. Thus, automation of the analysis using the SAEDC platform has the potential to save time and resources for cytotoxicity researchers and laboratories while generating reliable results.

Copyright of Baghdad Science Journal is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Colorectal cancer is the second deadliest cancer worldwide. The side effects and resistance of existing chemotherapy drugs are the background for various studies looking for potential plant extracts as new anticancer agents. This study aims to determine the cytotoxic activity of simpor leaf extract from Belitung and its effect on apoptosis of WiDr colorectal cancer cells. The compound content in simpor leaf extract was analyzed using Gas Chromatography-Mass Spectrometry (GC-MS). The cytotoxic activity of simpor leaf extract at different concentrations (25, 50 and 100 ppm) was determined by the MTT test and apoptosis induction by Annexin V/PI flow cytometry analysis. Based on the GC-MS chromatogram results, 13 different compounds were detected. Analysis of the relationship between extract concentration and the percentage of WiDr cell inhibition showed that an extract concentration of 100 ppm was the concentration with the highest percentage of inhibition (20.12 % ± 4.99) compared to concentrations of 50 ppm (13.95 % ± 2.32) and 25 ppm (15.90 % ± 1.38) with an inhibitory concentration value (IC50) of simpor leaf extract of 10.45 ppm. Induction of WiDr cell apoptosis by the extract was influenced by the concentration of simpor leaf extract, which was increase in the percentage of apoptotic cells from 16 % at a concentration of 25 ppm to 70.5 % at a concentration of 100 ppm. The results of this study show that simpor leaf extract from Belitung is able to induce apoptosis in WiDr colorectal cancer cells. [ABSTRACT FROM AUTHOR]

Background: In 2018, an estimated 2 million people had breast cancer. Forest honey (Apis dorsata) can have antioxidant activity due to the presence of flavonoid saponin, alkaloid, and tannin compound, therefore can be used as anticancer through the induction of apoptosis. Objective: To determine the IC50 of forest honey (Apis dorsata) on T47D breast cancer cells and see the morphology of T47D cells after administration of forest honey. Methods: This study is an in vitro test of the cytotoxic activity of forest honey against T47D breast cancer cells using the MTT assay method. The concentration of forest honey was prepared by the two-fold microdilution method in the range of 1000 - 31.25 µg/mL. Doxorubicin was used as a control drug with a concentration of 20 - 0.675 µg/mL. The morphology of T47D cells after treatment was observed with an inverted microscope with 400x magnification. Results: Forest honey (Apis dorsata) from any concentration did not show any inhibition of growth of T47D breast cancer cells. Meanwhile, doxorubicin had an IC50 of 3.746 µg/mL. The morphology of T47D cells with honey administration showed many live cells with formazan crystals. Conclusion: Forest honey has no cytotoxic activity against T47D breast cancer cells.

Reactions with allyl-, acetyl-, and phenylisothiocyanate have been studied on the basis of 3-amino-4,6-dimethylpyridine-2(1H)-one, 3-amino-4-phenylpyridine-2-one, and 3-amino-4-(thiophene-2-yl)pyridine-2(1H)-one (benzoyl-)isothiocyanates, and the corresponding thioureide derivatives 8-11a-c were obtained. Twelve thiourea derivatives were obtained and studied for their anti-diabetic activity against the enzyme α-glucosidase in comparison with the standard drug acarbose. The comparison drug acarbose inhibits the activity of α-glucosidase at a concentration of 15 mM by 46.1% (IC50 for acarbose is 11.96 mM). According to the results of the conducted studies, it was shown that alkyl and phenyl thiourea derivatives 8,9a-c, in contrast to their acetyl–(benzoyl) derivatives and 10,11a-c, show high antidiabetic activity. Thus, 1-(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)-3-phenylthiourea 9a has the highest inhibitory activity against the enzyme α-glucosidase, exceeding the activity of the comparison drug acarbose, which inhibits the activity of α-glucosidase by 56.6% at a concentration of 15 mm (IC50 = 9,77 mM). 1-(6-methyl-2-oxo 4-(thiophen-2-yl)-1,2-dihydropyridin-3-yl)-3-phenylthiourea 9c has inhibitory activity against the enzyme α-glucosidase, comparable to the comparison drug acarbose, inhibiting the activity of α-glucosidase at a concentration of 15 mm per 41.2% (IC50 = 12,94 mM). Compounds 8a, 8b, and 9b showed inhibitory activity against the enzyme α-glucosidase, with a lower activity compared to acarbose, inhibiting the activity of α-glucosidase at a concentration of 15 mM by 23.3%, 26.9%, and 35.2%, respectively. The IC50 against α-glucosidase for compounds 8a, 8b, and 9b was found to be 16.64 mM, 19.79 mM, and 21.79 mM, respectively. The other compounds 8c, 10a, 10b, 10c, 11a, 11b, and 11c did not show inhibitory activity against α-glucosidase. Thus, the newly synthesized derivatives of thiourea based on 3-aminopyridine-2(1H)-ones are promising candidates for the further modification and study of their potential anti-diabetic activity. These positive bioanalytical results will stimulate further in-depth studies, including in vivo models. [ABSTRACT FROM AUTHOR]

Due to the various side effects of conventional cancer treatment therapy, efforts to find anticancer agents with minimal side effects are in great demand. One of them is the synthesis of organotin(IV) hydroxybenzoate derivatives. Three organotin(IV) compounds, namely diphenyltin(IV) 2-hydroxybenzoate, [Ph2Sn(2-HBz)2] (DPT2-DH) (2), diphenyltin(IV) 3-hydroxybenzoate, [Ph2Sn(3-HBz)2] (DPT3-DH) (3) and diphenyltin(IV) 4-hydroxybenzoate, [Ph2Sn(4-HBz)2] (DPT4-DH) (4), have been successfully synthesized. Compounds 2–4 were obtained by reacting diphenyltin(IV) oxide, [Ph2SnO] (DPTO) (1) with 2-hydroxybenzoic acid (2-HHBz), 3-hydroxybenzoic acid (3-HHBz) and 4-hydroxybenzoic acid (4-HHBz), respectively. The compounds synthesized were fully characterized by UV–Vis, FT-IR, and NMR spectroscopies and microelemental analysis to see the purity of the compounds. The antiproliferative activity of the compounds was tested against three cancer cell lines of lung cancer (A549), breast cancer (MCF-7) and cervical cancer (HeLa), and their activities were compared to normal cell cancer, Vero. The results of the antiproliferative test demonstrated that compound 2 was found to be most active against the A549 cell line. Compounds 2 and 3 are active against MCF-7 while compound 4 was found to be least active against all cancer lines tested. All compounds have also been found to have a good selectivity index (SI) toward the A549 cell line, although their SI values are not good enough against the HeLa cell line. [ABSTRACT FROM AUTHOR]

In this research, we examined the toxicity of Ag-graphene oxide (GO) nanocomposites against both the Gram-negative bacterium Escherichia coli and Glioblastoma cancer cells (U87MG). Our findings reveal that Ag-GO possesses bactericidal properties, with a minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of 160 µg/mL. The antibacterial efficacy of Ag-GO is contingent on contact time and concentration, making it a potential candidate for integration into materials designed to combat microbial infections. The bactericidal effect of Ag-GO can be attributed to the release of silver ions and the physical damage inflicted by the sharp edges of GO sheets. Furthermore, our study demonstrates that Ag-GO exhibits anticancer activity against U87MG cells, with an IC50 value of 270 µg/mL. The mechanism underlying the anticancer activity of Ag-GO likely involves cell membrane disruption and apoptosis induction. These findings signify the promising medical and biological applications of Ag-graphene oxide nanocomposites. [ABSTRACT FROM AUTHOR]

Three new metal complexes of ceftriaxone (cef), incorporating platinum(IV), gold(III), and ruthenium(III), were prepared. The complexes were prepared using a 1:2 molar ratio between ceftriaxone sodium salt (Na2cef) to AuCl3, PtCl4, and RuCl3 salts in methanol solvent. The as-synthesized complexes were characterized using microanalytical techniques for C, H, N, and S elements, magnetic and molar conductance measurements, as well as spectroscopic methods including FTIR, ¹ H NMR, and UV-Vis. The shape, morphology and size calculations have been examined using SEM, TEM, and X-ray diffraction data. The cef complexes were six-coordinate systems possessing a distorted octahedral geometry. Through the oxygen of both triazine and carboxylate moieties with the chemical formulae [Au(cef)2(Cl)(H2O)] (I), [Pt(cef)2(Cl)2] (II), and [Ru(cef)2(Cl)(H2O)] (III) the antibiotic cef acts as a bidentate ligand towards three metal ions. The newly created complexes demonstrated antibacterial activity showing efficacy in comparison to the cef sodium ligands. In vitro, antibacterial assays against specific microorganisms were evaluated to assess the antibacterial activities of the complexes. Cytotoxicity assays for cef complexes were conducted for HepG-2 and MCF-7 cell lines, representing human hepatocellular carcinoma and breast cancer, respectively. A value of 22.4 g and 26.2 g for 50% inhibitory concentration (IC50), respectively, for HepG-2 and MCF-7 were obtained for [Ru(cef)2(Cl)(H2O)] (III). [ABSTRACT FROM AUTHOR]

Background/Aim: Rapamycin inhibits the mTOR protein kinase. Methioninase (rMETase), by degrading methionine, targets the methionine addiction of cancer cells and has been shown to improve the efficacy of chemotherapy drugs, reducing their effective doses. Our previous study demonstrated that rapamycin and rMETase work synergistically against colorectal-cancer cells, but not on normal cells, when administered simultaneously in vitro. In the present study, we aimed to further our previous findings by exploring whether synergy exists between rapamycin and rMETase when used sequentially against HCT-116 colorectal-carcinoma cells, compared to simultaneous administration, in vitro. Materials and Methods: The half-maximal inhibitory concentrations (IC50) of rapamycin alone and rMETase alone against the HCT-116 human colorectal-cancer cell line were previously determined using the CCK-8 cell viability assay (11). We then examined the efficacy of rapamycin and rMETase, both at their IC50, administered simultaneously or sequentially on the HCT-116 cell line, with rapamycin administered before rMETase and vice versa. Results: The IC50 for rapamycin and rMETase, determined from previous experiments (11), was 1.38 nM and 0.39 U/ml, respectively, of HCT-116 cells. When rMETase was administered four days before rapamycin, both at the IC50, there was a 30.46% inhibition of HCT-116 cells. When rapamycin was administered four days before rMETase, both at the IC50, there was an inhibition of 41.13%. When both rapamycin and rMETase were simultaneously administered, both at the IC50, there was a 71.03% inhibition. Conclusion: Rapamycin and rMETase have synergistic efficacy against colorectal-cancer cells in vitro when administered simultaneously, but not sequentially. [ABSTRACT FROM AUTHOR]

Novel inhibitors of GlcNAc-Ts have been reported based on benzoxazolone appended amino acids/esters which showed a competitive inhibition of the enzyme with IC50 values in lower micromolar range. The compounds 1b–5b showed a better inhibition profile against GlcNAc-Ts as compared to 1a–5a as evidenced by the in vitro 96 well plate ELISA experiment and the in vitro cytotoxicity studies on the cancer cell lines PDAC, Caco-2, MDA-MB-231, HT-29, PC-3, and A549. The execution of ELISA and cytotoxicity experiments on the compounds 1a–5a in the presence of esterase enzyme along with the appraisal of the lipophilicity index, and calculation of Ki and Ka values for the enzyme-inhibitor complex further indicated that the compounds 1a–5a serve as prodrugs of the compounds 1b–5b owing to a better lipophilicity index of the former. Double reciprocal plots were constructed for 2 different concentrations of the test compounds 1b–5b and that of the natural substrate of OGT. A competitive mode of inhibition was observed for the test molecules which was further confirmed by molecular docking analysis of these molecules in the active site of OGT in the presence of its natural inhibitor. Mechanistic evaluation of the inhibition of OGT by test molecules was performed by NMR and HPLC experiments where hydrolysis of exocyclic urea linkage in the test molecules was observed on their incubation with the enzyme over a period. [ABSTRACT FROM AUTHOR]

Seasonal factors such as temperature, solar UV-light intensity, and daylight length can induce changes in the water quality properties and, hence, the nutritional compositions of plants. This comparative study was carried out for the consecutive four (4) seasons (winter, spring, summer, and autumn) to determine the influence of seasonal variations on the 50% inhibitory concentration (IC50), total antioxidant capacity (TAC), total phenolics content (TPC), and total flavonoids content (TPC) of the red chili fruit (RCF), red tomato fruit (RTF), green leafy spinach (GLS), and green leafy lettuce (GLL) collected from a coupled commercial aquaponics system. The IC50, TAC, TPC, and TFC concentration levels indicated a significant (P<0.05) difference in the summer compared with the winter, spring, and autumn. The RCF extract indicated the lowest IC50, thus greater scavenging power in comparison to RTF, GLS, and GLL extracts. Similarly, the RCF showed the highest TAC and TPC, while the GLL showed the highest TFC. In this study, variations in seasons have induced changes in the IC50, TAC, TPC, and TFC concentration levels of the RCF, RTF, GLS, and GLL extracts. [ABSTRACT FROM AUTHOR]

Butterfly pea flowers are plants that contain flavonoid compounds which produce a purple color, so they can be used as body butter. This research aims to determine the butterfly pea flower extract as body butter, which formula is the best in terms of the physical properties of the preparation and the antioxidant activity of the butterfly pea flower (Clitoria ternatea L.) using the DPPH (2,2-Diphenyl 1-1 Picrylhydrazyl) method. Samples were obtained from the Tegal area and used non-random/probability techniques with the simple random sampling method. The extraction method used is the reflux method with 70% ethanol solvent. This research used concentrations of butterfly pea flower extract (Clitoria ternatea L.) with concentrations of 1%, 3%, 6%. Then the physical properties of the body butter preparation were carried out including organoleptic tests carried out with the naked eye, pH testing using a pH stick, adhesion test, spreadability test, and antioxidant activity test of butterfly pea flower using DPPH which was classified as very, namely the value of butterfly pea flower in formulation 1:82,84 µg/ml, formulation 2: 77,98 µg/ml, formulation 3:77,39 µg/ml. [ABSTRACT FROM AUTHOR]

The affinity constant, also known as the equilibrium constant, binding constant, equilibrium association constant, or the reciprocal value, the equilibrium dissociation constant (Kd), can be considered as one of the most important characteristics for any antibody–antigen pair. Many methods based on different technologies have been proposed and used to determine this value. However, since a very large number of publications and commercial datasheets do not include this information, significant obstacles in performing such measurements seem to exist. In other cases where such data are reported, the results have often proved to be unreliable. This situation may indicate that most of the technologies available today require a high level of expertise and effort that does not seem to be available in many laboratories. In this paper, we present a simple approach based on standard immunoassay technology that is easy and quick to perform. It relies on the effect that the molar IC50 approaches the Kd value in the case of infinitely small concentrations of the reagent concentrations. A two-dimensional dilution of the reagents leads to an asymptotic convergence to Kd. The approach has some similarity to the well-known checkerboard titration used for the optimization of immunoassays. A well-known antibody against the FLAG peptide, clone M2, was used as a model system and the results were compared with other methods. This approach could be used in any case where a competitive assay is available or can be developed. The determination of an affinity constant should belong to the crucial parameters in any quality control of antibody-related products and assays and should be mandatory in papers using immunochemical protocols. [ABSTRACT FROM AUTHOR]

The present study provides the first information on the chemical composition and acetylcholinesterase inhibitory activity of the essential oil (EO) from the leaves of Mitrephora poilanei Weeras. & R.M.K.Saunders from Vietnam. Gas chromatography and gas chromatography-mass spectrometry analysis revealed that the main components of the M. poilanei EO were β-caryophyllene (13.2%), α-humulene (10.5%), germacrene D (8.1%), β-elemene (5.2%) and bicyclogermacrene (5.1%). The anti-acetylcholinesterase assay showed that the EO displayed moderate activity with IC50 value of 31.16 ± 3.06 μg/mL. These findings proposed that the plant can be exploited for its anti-acetylcholinestrate potential. [ABSTRACT FROM AUTHOR]

Abstract Cytochrome P450 enzymes (CYPs) play a crucial role in phase I metabolic reactions. The activity of CYPs would affect therapeutic efficacy and may even induce toxicity. Given the complex components of traditional Chinese medicine, it is important to understand the effect of active ingredients on CYPs activity to guide their prescription. This study aimed to evaluate the effect of polyphyllin H on the activity of CYPs major isoforms providing a reference for the clinical prescription of polyphyllin H and its source herbs. The effects of polyphyllin H were evaluated in pooled human liver microsomes using probe substrates of CYP1A2, 2A6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 to determine their activities. The Lineweaver‐Burk was used to model the inhibition, and a time‐dependent inhibition experiment was performed to understand the characteristics of the inhibition. Polyphyllin H significantly suppressed the activity of CYP1A2, 2D6, and 3A4 with IC50 values of 6.44, 13.88, and 4.52 μM, respectively. The inhibition of CYP1A2 and 2D6 was best fitted with a competitive model, yielding the inhibition constant (Ki) values of 3.18 and 6.77 μM, respectively. The inhibition of CYP3A4 was fitted with the non‐competitive model with the Ki value of 2.38 μM. Moreover, the inhibition of CYP3A4 was revealed to be time‐dependent with the inhibition parameters inhibition constant (KI) and inactivation rate constant (Kinact) values of 2.26 μM−1 and 0.045 min−1. Polyphyllin H acted as a competitive inhibitor of CYP1A2 and 2D6 and a non‐competitive and time‐dependent inhibitor of CYP3A4.

Free radicals are one of many forms of reactive oxygen sorts known for having unpaired electrons. The presence of free radicals in the body can cause damage such as premature aging, characterized by the appearance of wrinkles. This damage can be countered with antioxidant compounds. Beetroot is one of the fruits with antioxidant properties due to the presence of betacyanin compounds from the flavonoid group. This research aims to identify the antioxidant activity and IC50 value of beetroot (Beta vulgaris L.) extract nanoemulsion formulations using the DPPH method. Nanoemulsion formulations were prepared with varying concentrations of beetroot extract at 1% (X1), 3% (X2), and 5% (X3) to determine which concentration has the best antioxidant activity. Quality evaluation of the nanoemulsion formulations was also conducted, including organoleptic tests, pH tests, and homogeneity tests. The results showed that the beetroot extract nanoemulsion formulations have antioxidant activity and meet the requirements for physical properties and formulation stability. Nanoemulsion formulations with 5% (X3) beetroot extract content exhibited the best antioxidant activity with an IC50 value of 136.475 ppm.

Antioxidant compounds play an essential role in health because they can reduce the risk of chronic diseases such as cancer and coronary heart disease. This study analyzed the antioxidant activity of red fruit oil and juice. This study used an experimental method with oil and juice obtained through boiling for 4-5 hours. The stages of the study include flavonoid qualitative tests and antioxidant activity tests using the DPPH method using UV-Vis Spectrophotometers. Based on the research results, oil and red fruit juice contain flavonoids that have the potential to be antioxidants. Antioxidant activity test with the DPPH method showed IC50 in red fruit oil products on the market at 30.11 ppm and red fruit juice at 31.80 ppm, showing vigorous antioxidant activity compared to homemade red fruit oil with an IC50 of 85.98 ppm.

The leaves extract of Rourea coccinea was fractionated, following the bioguided method, to give one phenolic compound named 1-caffeoylquinic acid lactone (1-CQL) (1), isolated from this plant for the first time, and the 3-O-β-D-glucopyranoside of stigmasterol (2). The structure of these compounds was determined. The Minimum Inhibitory Concentrations (MIC) for antisalmonella activity was up to 2000 µg·mL-1 for extract and fractions, and up to 500 µg·mL-1 for compound 1. The half-inhibitory Concentration (IC50) values against Plasmodium falciparum PfDd2 was 92.56 µg·mL-1 for extract and 31.24 to 77.21 µg·mL-1 for fractions. Compound 1 exhibited on the same strain an antiplasmodial activity with an IC50 value of 8.58 µg·mL-1. These results justify the use of this plant in Beninese pharmacopeia for the treatment of several diseases such as malaria.

Abstract Motivation The prediction of cancer drug response is a challenging subject in modern personalized cancer therapy due to the uncertainty of drug efficacy and the heterogeneity of patients. It has been shown that the characteristics of the drug itself and the genomic characteristics of the patient can greatly influence the results of cancer drug response. Therefore, accurate, efficient, and comprehensive methods for drug feature extraction and genomics integration are crucial to improve the prediction accuracy. Results Accurate prediction of cancer drug response is vital for guiding the design of anticancer drugs. In this study, we propose an end-to-end deep learning model named DeepAEG which is based on a complete-graph update mode to predict IC50. Specifically, we integrate an edge update mechanism on the basis of a hybrid graph convolutional network to comprehensively learn the potential high-dimensional representation of topological structures in drugs, including atomic characteristics and chemical bond information. Additionally, we present a novel approach for enhancing simplified molecular input line entry specification data by employing sequence recombination to eliminate the defect of single sequence representation of drug molecules. Our extensive experiments show that DeepAEG outperforms other existing methods across multiple evaluation parameters in multiple test sets. Furthermore, we identify several potential anticancer agents, including bortezomib, which has proven to be an effective clinical treatment option. Our results highlight the potential value of DeepAEG in guiding the design of specific cancer treatment regimens.

Severe acute respiratory syndrome coronavirus 2 (SARS‑CoV‑2) induced cytokine storm is the major cause of COVID-19 related deaths. Patients have been treated with drugs that work by inhibiting a specific protein partly responsible for the cytokines production. This approach provided very limited success, since there are multiple proteins involved in the complex cell signaling disease mechanisms. We targeted five proteins: Angiotensin II receptor type 1 (AT1R), A disintegrin and metalloprotease 17 (ADAM17), Nuclear Factor‑Kappa B (NF‑κB), Janus kinase 1 (JAK1) and Signal Transducer and Activator of Transcription 3 (STAT3), which are involved in the SARS‑CoV‑2 induced cytokine storm pathway. We developed machine-learning (ML) models for these five proteins, using known active inhibitors. After developing the model for each of these proteins, FDA-approved drugs were screened to find novel therapeutics for COVID‑19. We identified twenty drugs that are active for four proteins with predicted scores greater than 0.8 and eight drugs active for all five proteins with predicted scores over 0.85. Mitomycin C is the most active drug across all five proteins with an average prediction score of 0.886. For further validation of these results, we used the PyRx software to conduct protein-ligand docking experiments and calculated the binding affinity. The docking results support findings by the ML model. This research study predicted that several drugs can target multiple proteins simultaneously in cytokine storm-related pathway. These may be useful drugs to treat patients because these therapies can fight cytokine storm caused by the virus at multiple points of inhibition, leading to synergistically effective treatments.

AbstractDifferent microalgal species possess the proficiency of tolerating heavy metals and enhance certain metabolic processes under metal stress. This is a novel study on C. minutissima under Chromium (III) stress to determine the IC50 value for optimization, to evaluate its phycoremediation potential and biofuel prospects. Varied range of Chromium Sulfate (20-120 mg/L) exposure on C. minutissima presented an IC50 value of 83.78 mg/L and ICPMS data stated that C. minutissima was able to eliminate 96.5% of Cr (III) from the medium with a BCF value of 0.96 and a high TI value of 1.035, reflecting on the high Cr (III) resistance ability and remediation potential of the selected microalgal species. A higher biomass productivity was observed for stressed cells (17.92 mg/L/day) than control (15.42 mg/L/day). The lipid content and productivity in the metal treated cells was elevated (21.21% and 0.77 mg/L in control, 30.12% and 1.26 mg/L under stress, respectively) with simultaneous maintenance of growth and photosynthetic functions. GC-MS study indicated a rise in MUFA under Cr (III) stress. This study presents significant insights for further investigation in utilization of C. minutissima for integrated approaches toward Cr (III) bioremediation and biodiesel production. [ABSTRACT FROM AUTHOR]

Breast cancer represents a major global health issue with multidrug resistance (MDR) posing a significant challenge. MDR leads to cancer cells becoming resistant to various drugs, severely compromising the effectiveness of breast cancer treatments. Doxorubicin (DOX) is a fundamental drug in the treatment of breast cancer but contributes to the development of MDR. DOX is commonly used in the study of MDR with the overexpression of ATP binding cassette transporter superfamily B member 1 (ABCB1) gene being one of the main mechanisms through which tumor cells exhibit MDR. Current research, including more than 150 clinical trials on ABCB1 inhibitors, aims to overcome this obstacle. However, due to severe side effects and poor solubility, none of these inhibitors have been approved by the U.S. Food and Drug Administration (FDA), which highlights the urgent need for safer and more effective solutions. Danshensu (DSS) shows potential in reversing MDR without the severe side effects associated with other treatments, underscoring its importance in advancing breast cancer therapy. This study investigated the reversing effects and mechanisms of DSS on MDR in human breast cancer cell lines MCF-7/DOX and MCF-7. The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was employed to evaluate the impact of DSS on cell drug sensitivity and resistance. Further, fluorescence spectrophotometry was applied to measure the intracellular concentration of DOX, and flow cytometry was used to analyze the expression of P-glycoprotein (ABCB1), a protein associated with drug resistance. The results showed that DSS significantly reduced the IC50 value of DOX for MCF-7/DOX cells without notable effects on MCF-7 cells, indicating a specific action against resistant cells. Furthermore, DSS increased the intracellular concentration of DOX in MCF-7/DOX cells and decreased the expression of ABCB1 in these cells. The results confirmed that DSS could reverse MDR in MCF-7/DOX cells by reducing the expression of ABCB1. This discovery offered new insights into the mechanisms through which DSS impacted drug resistance and provided a potential therapeutic strategy for overcoming resistance in breast cancer treatments. [ABSTRACT FROM AUTHOR]

Integrative oncology comprises a range of therapies that can complement standard cancer treatments, such as chemotherapy, surgery, and radiotherapy. One commonly used approach to complementary medicine involves using naturally occurring antioxidants, such as Ayurvedic herbal extracts, to assist in reducing the adverse effects of cancer treatment on healthy cells. Swastharakshak Plus® (SR plus®) is a polyherbal formulation consisting of Tinospora cordifolia, Curcuma longa, and Camellia sinensis, known for their phytochemical content. This research paper hypothesized that SR plus® has anti-oxidant properties and a cytotoxic effect on HeLa cancer cells. The study found significantly lower IC50 values for SR plus® ethanol extract after both 24 hours (22 µg/ml) and 48 hours (8.65 µg/ml) of exposure, compared to methanol and water extracts of SR plus®. Also, fluorescence staining using Hoechst dye, DAPI, and dual staining (acridine orange and propidium Iodide) revealed the occurrence of apoptosis in HeLa cells treated with the IC50 concentration of SR plus® ethanol extract for 48 hr. HeLa cells showed 43% cell death SR plus® ethanol extract. In conclusion, the SR plus® formulation exhibited cytotoxicity activity against the HeLa cell line, possibly due to apoptosis. By investigating complementary therapies like SR plus®, we may find valuable additions to existing cancer treatments that can enhance their efficacy and reduce side effects. [ABSTRACT FROM AUTHOR]

Copyright of Indonesian Fisheries Processing Journal / Jurnal Pengolahan Hasil Perikanan Indonesia is the property of IPB University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The taste of green tea is different and unique; factors that contribute to this include the type of picking method, leaf age, variety, and clones. The researchers used the disc method for antimicrobial testing, the DPPH method for antioxidant testing with a visible spectrophotometer set to 515 nm wavelength, the HPLC method for catechin content analysis, and phytochemical screening as a qualitative test. The results of this study's phytochemical screening tests revealed that green tea was positive for terpenoids with Liebermann Bouchard reagent, flavonoids, and tannins with FeCl3 reagent, and good inhibition zones for pathogenic bacteria of Staphylococcus aureus, Streptococcus mutans, and Salmonella typhi. The outcomes of the negative control, 5%, 10%, and 15% green tea ethanol extract against the following microorganisms were: 0; 4,3; 6,35; 8,05 mm for Staphylococcus aureus, 0; 5,9; 6,95; 8,55 mm for Streptococcus mutans, and 0; 3,45; 4,4; 6,45 mm for Salmonella typhi. Results indicated that Salmonella typhi and Staphylococcus aureus were more effectively inhibited by green tea ethanol extract than Streptococcus mutans. Antioxidants demonstrated IC50 of 33.33 indicating a very significant antioxidant activity in the test. determined using a visible spectrophotometer. The HPLC test yielded a catechin content of 16.9%. [ABSTRACT FROM AUTHOR]

Copyright of Indonesian Fisheries Processing Journal / Jurnal Pengolahan Hasil Perikanan Indonesia is the property of IPB University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Motivation: The prediction of cancer drug response is a challenging subject in modern personalized cancer therapy due to the uncertainty of drug efficacy and the heterogeneity of patients. It has been shown that the characteristics of the drug itself and the genomic characteristics of the patient can greatly influence the results of cancer drug response. Therefore, accurate, efficient, and comprehensive methods for drug feature extraction and genomics integration are crucial to improve the prediction accuracy. Results: Accurate prediction of cancer drug response is vital for guiding the design of anticancer drugs. In this study, we propose an end-to-end deep learning model named DeepAEG which is based on a complete-graph update mode to predict IC50. Specifically, we integrate an edge update mechanism on the basis of a hybrid graph convolutional network to comprehensively learn the potential high-dimensional representation of topological structures in drugs, including atomic characteristics and chemical bond information. Additionally, we present a novel approach for enhancing simplified molecular input line entry specification data by employing sequence recombination to eliminate the defect of single sequence representation of drug molecules. Our extensive experiments show that DeepAEG outperforms other existing methods across multiple evaluation parameters in multiple test sets. Furthermore, we identify several potential anticancer agents, including bortezomib, which has proven to be an effective clinical treatment option. Our results highlight the potential value of DeepAEG in guiding the design of specific cancer treatment regimens. [ABSTRACT FROM AUTHOR]

This article reports on the synthesis of nine promising new 1,3,4-thiadiazole derivatives based on 3-aminopyridones, containing various acidic linkers. The synthesis was carried out by cyclizing the corresponding thiohydrazides 4a–c and anhydrides of glutaric, maleic, and phthalic acids upon heating in acetic acid solution. The conducted bio-screening of the synthesized new 1,3,4-thiadiazole derivatives containing different acidic linkers (butanoic, acrylic, and benzoic acids) showed that they have significant inhibitory activity against α-glucosidase (up to 95.0%), which is 1.9 times higher than the value for the reference drug acarbose (49.5%). Moreover, one of the 1,3,4-thiadiazole derivatives with a benzoic acid linker—2-(5-((6-Methyl-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridin-3-yl)carbamoyl)-1,3,4-thiadiazol-2-yl)benzoic acid (9′b)—showed an IC50 value of 3.66 mM, nearly 3.7 times lower than that of acarbose (IC50 = 13.88 mM). High inhibitory activity was also shown by 1,3,4-thiadiazole derivatives with a butanoic acid linker (compounds 7b, 7c)—with IC50 values of 6.70 and 8.42 mM, respectively. A correlation between the structure of the compounds and their activity was also established. The results of molecular docking correlated well with the bioanalytical data. In particular, the presence of a butanoic acid linker and a benzoic fragment in compounds 7b, 7c, and 9b increased their binding affinity with selected target proteins compared to other derivatives 3–6 (a–c). Calculations according to Lipinski's rule of five also showed that the synthesized compounds 7b, 7c, and 9b fully comply with Ro5 and meet all criteria for good permeability and acceptable oral bioavailability of potential drugs. These positive bioanalytical results will stimulate further in-depth studies, including in vivo models. [ABSTRACT FROM AUTHOR]

The solubilization of butylated hydroxyanisole (BHA) in aqueous surfactant solutions of different architectures (anionic, cationic, and nonionic) has been investigated to improve its aqueous solubility and assess the effect of surfactant‐based multiphase environments on its antiradical activity against 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH). Herein, we report that the micellar encapsulation and DDPH antiradical activity of BHA are highly dependent on the structure and amount of surfactant used. Radical scavenging activity (RSA) and solubilization were efficient in nonionics compared to ionics. DPPH reduction kinetics in micellar media is essential to uncover the behavior of BHA in multiphase environments commonly encountered in different food systems simulated by aqueous micelles. The study is important to identify the optimal medium for improving the solubility and antioxidant capacity of compounds like BHA, and to anticipate the effect of different micro‐heterogeneous/multiphase environments on BHA's antioxidant capability. [ABSTRACT FROM AUTHOR]

Copyright of Indonesian Fisheries Processing Journal / Jurnal Pengolahan Hasil Perikanan Indonesia is the property of IPB University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Objectives: The objective of this study was to investigate the essential oil (EO) extracted from the leaves of Vernonia volkameriifolia DC., a Vietnamese plant belonging to the Asteraceae family. The focus was on determining the chemical composition of the EO and assessing its antimicrobial and antioxidant activities. Methods: The EO obtained from V. volkameriifolia underwent comprehensive analysis using gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) to identify its chemical constituents. Antimicrobial activity was determined against eight microorganisms using the broth microdilution susceptibility method, with minimum inhibitory concentration (MIC) values calculated. Additionally, antioxidant activity was assessed through DPPH and ABTS assays, with half maximal inhibitory concentration (IC50) values indicating the potency of the EO. Results: The main components of the V. volkameriifolia EO were identified as ß-bisabolene (25.2%), ß-pinene (19.1%), germacrene D (13.1%), and cis-ß-elemene (11.4%). The EO exhibited significant antimicrobial activity, with a MIC value of 200 µg/mL against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Aspergillus niger, and Saccharomyces cerevisiae. Additionally, it displayed activity against Candida albicans with a MIC value of 100 µg/mL. In antioxidant tests, the EO demonstrated notable potential, with IC50 values of 144.1 µg/mL and 179.8 µg/mL for DPPH and ABTS, respectively. Conclusion: This study represents the inaugural investigation into the EO extracted from the leaves of V. volkameriifolia. The identified chemical components, along with the demonstrated antimicrobial and antioxidant activities, contribute valuable insights into the potential applications of V. volkameriifolia EO in pharmaceutical and therapeutic contexts. Further research can build upon these findings to uncover additional properties and applications of this EO. [ABSTRACT FROM AUTHOR]

Hyptis capitata Jacq. known as Sumambu plants in Sulawesi, has phytopharmaceutical importance. H. capitata extracts were evaluated for their phytochemical properties, antioxidant activity, and cytotoxicity. Using the maceration yielded five types of extracts: root chloroform (RC), root methanol (RM), leaf chloroform (LC), leaf methanol (LM), and leaf ethanol (LE). Phytochemical properties were identified by qualifying procedure and digital image analysis for quantifying Red-Green-Blue (RGB) percentage and hex colour code. 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay was used to determine the half-maximal inhibitory concentration (IC50). Cytotoxicity screening of each extract was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay against HeLa and 4T1 cells. Gas Chromatography-Mass Spectrometry (GC-MS) assay was used to identify the phytochemical compounds of the extracts with the most promising potential. Alkaloids were the major constituents of the phytochemicals of RC, RM, LE, LC, and LM. RM and LM have potency and weak free radical scavenging activities, with IC50 value 31.08 and 58.03 µg/mL, respectively. The IC50 of RC and RM against HeLa cells were 84.21 ± 0.63 and 172.10 ± 02.90 µg/mL, respectively. Meanwhile, the cytotoxicity of RC and RM against 4T1 cells were 86.42 ± 0.80 and 182.82 ± 7.00 µg/mL, respectively. It means RC and RM exhibit a moderate level of cytotoxicity in both HeLa and 4T1 cells. LM shows moderate cytotoxicity, but it is limited to 4T1 cells with an IC50 value of 181.86 ± 12.68 µg/mL. The cytotoxicity level of extracts was lower than doxorubicin. Campesterol, ferruginol, stigmasterol, cis-13-octadecenoic acid methyl esters, and methyl palmitate were predicted to play a role in the antioxidant activity and cytotoxicity of RC, RM, and LM. RC, RM, and LM possess the potential for development as anticancer agents. Moreover, RM shows promise as an antioxidant due to its notable radical scavenging activity. Further research is required to explore the cytotoxic effects of RC, RM, and LM on normal cells and to assess their toxicity in experimental animals.

Medicinal plants contain various secondary metabolites, such as alkaloids, polyphenols, terpenes, tannins, terpenoids, and flavonoids. These compounds are important sources for treating numerous diseases. Datura stramonium, a plant from the Solonaceae family, is rich in alkaloids, glycosides, terpenoids, steroids, flavonoids, tannins, and saponins. Over time, this plant has demonstrated significant therapeutic effects. The objective of this study was to extract atropine and scopolamine compounds, which are alkaloids found in D. stramonium leaves, and investigate their antibacterial and cytotoxic effects. Atropine and scopolamine were isolated from D. stramonium and analyzed using high-performance chromatography (HPLC) and carbon and proton NMR (NMR H1, C13). The antibacterial activity of atropine and scopolamine against Shigella dysenteriae (PTCC 1188), Streptococcus pyogenes (ATCC 19615), and Staphylococcus epidermidis (CIP 81.55) was investigated using the disc diffusion and microdilution methods. The cytotoxic activity on AsPC-1 (pancreatic adenocarcinoma), MCF-7 (breast cancer), and ACHN (renal carcinoma) cell lines was studied using the MTT reagent assay method. Both compounds exhibited the highest antibacterial activity against S. dysenteriae, while the lowest antibacterial activity was observed against S. pyogenes. All three cancer cell lines were treated with different concentrations of atropine and scopolamine for 24 and 48 h. The results of both extracts showed that increasing the concentration of the extracts decreased the viability of all three cell lines. The IC50 values of both extracts were measured at 24 and 48 h. Preliminary results confirm the therapeutic potential of these two compounds, but further studies are required to investigate there in vivo effects.

Background: Piper longum L. is a tropical and subtropical medicinal plant that has been used as antidiabetic, diarrhea, stomachache, cough, asthma, and bronchitis since ancient times. The in vitro-grown callus from the leaf, however, has not been tested and utilized for any of these conditions. Thus, this research pursues to assess the comparative study of antioxidant, antibacterial, and antidiabetic activities of in vitro-grown callus and various parts of Piper longum-grown in the wild. Methods: The antioxidant activity of crude extracts and the fractions were determined by DPPH (1,1-diphenyl-2-picrylhydrazyl) free-radical scavenging assay, the antibacterial activity by agar-well diffusion method, and antidiabetic activity by α-amylase and α-glucosidase inhibition assay. In addition, the total phenol content (TPC) and total flavonoid contents (TFC) were calculated using Folin-Ciocalteau reagent and aluminum chloride complex-forming assay respectively. Results: The highest antioxidant activity (IC50=134.81±1.16 µg/mL), TPC (41.22±0.50 mg of GAE/g dry weight), and TFC (73.41±0.53 mg of QE/g dry weight) were obtained in the dichloromethane (DCM) fraction of root than other crude extracts and fractions. The DCM fractions of root exhibited the minimum inhibitory concentration (MIC) at 5.0 mg/mL and minimum bactericidal concentration (MBC) of 8.35 mg/mL to the Staphylococcus aureus. Moreover, the DCM fraction of root showed the highest α-amylase and α-glucosidase inhibition (IC50=365.21±31.02 and 489.07±27.96 µg/mL) than other crude extracts and fractions. To the best of our information, comparative antioxidant (IC50=206.61±0.64 µg/mL), antibacterial (suppressed 80 % of tested bacteria), and antidiabetic (IC50=1165.15±15.63 and 1304.76±12.43 µg/mL) properties of the in vitro-grown callus were recorded for the first time in P. longum, and were found to be comparative to those of the wild-grown parts. Conclusions: These results showed that wild-grown P. longum roots, particularly the DCM fraction, could be an important source of natural antioxidants, antimicrobials, and antidiabetics for better curative uses than other wild-grown parts and in vitro-grown callus. In vitro-grown callus, however, could be used as a natural drug source and used to conserve P. longum in its natural habitats in the future.

The topical therapy with rifampicin (RF)-based formulations is beneficial for treating postoperative wound infections and to accelerate healing. Despite recent research highlighting the antibiotic’s significant anti-inflammatory properties, limited topical wound healing products are currently available. The present study aimed to prove that the newly synthesized nanoparticles based on grafted alginate and poly(N-vinylcaprolactam) (pNVCL) and poly-lactic-co-glycolic acid (PLGA) contribute to the healing process of a wound. The methods used were at first the synthesis of the copolymer of alginate and pNVCL via grafting from technique and radical polymerization followed by water-in-oil-in water (W/O/W) emulsification; as oil phase PLGA dissolved in dichloromethane (DCM) was used. The formed nanoparticles were than characterized. The loaded RF was determined to be 160 µg/mL for a 20 mg formulation and within a four-hour time frame approximately 10% of the total loaded amount was released. The inhibitory concentrations (IC50) were 192.1 µg/mL for the nanoparticle, 208.8 µg/mL for pure rifampicin, and 718.1 µg/mL for the rifampicin-loaded nanoparticles. Considering the double role rifampicin was used for, the result was considered satisfactory in the way that these formulations could be used predominantly for postoperative wound irrigation in order to avoid infections and to improve healing.

Phyllanthus niruri grows easily in Indonesia and is widely used in traditional medicine. Differences in growing conditions, methods of preparation, and harvest time greatly affect the phytochemical contents, affecting the efficacy and toxicity of medicinal plants. This study aims to identify the phytochemical contents and toxicity and determine the antioxidant and antimicrobial activities of Phyllanthus niruri extract (PNE) commonly used by people in Aceh. Phytochemical analysis was carried out qualitatively and semi-quantitatively with GC-MS. A toxicity test was carried out with the brine shrimp lethality test (BSLT). The antioxidant activity was assessed by measuring IC50 against the DPPH system. Antimicrobial assays against Staphylococcus aureus, Escherichia coli, and Candida albicans were determined based on the disc diffusion test. The results of this study indicate that PNE contains phenolics, flavonoids, tannins, steroids, saponins, and alkaloids. Based on the semiquantitative phytochemical analysis using GC-MS, the major phytochemical component of PNE is 2,3 dihydro-3-5-dihydroxy-6-methyl-4H-pyran-4-one, hexadecanoic acid, triazole derivates, linolenic acid, benzaldehyde 3,4-dimethoxy, hexahydroanthracene derivatives, and phytol. The LC50 PNE is 532.96 ppm. The IC50 value for PNE in inhibiting DPPH is 56.72 ppm. PNE has antimicrobial activity against S. aureus, directly proportional to the increase in concentration. PNE obtained in community yards in Aceh has a low level of toxicity with potent antioxidant and antimicrobial activity against S. aureus. [ABSTRACT FROM AUTHOR]

Copyright of Indonesian Fisheries Processing Journal / Jurnal Pengolahan Hasil Perikanan Indonesia is the property of IPB University and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Chemotherapy and radiotherapy resistance are major obstacles in the long-term efficacy of head and neck squamous cell carcinoma (HNSCC) treatment. Secondhand smoke (SHS) exposure is common and has been proposed as an independent predictor of HNSCC recurrence and disease-free survival. However, the underlying mechanisms responsible for these negative patient outcomes are unknown. To assess the effects of SHS exposure on cisplatin efficacy in cancer cells, three distinct HNSCC cell lines were exposed to sidestream (SS) smoke, the main component of SHS, at concentrations mimicking the nicotine level seen in passive smokers' saliva and treated with cisplatin (0.01–100 µM) for 48 h. Compared to cisplatin treatment alone, cancer cells exposed to both cisplatin and SS smoke extract showed significantly lower cisplatin-induced cell death and higher cell viability, IC50, and indefinite survival capacity. However, SS smoke extract exposure alone did not change cancer cell viability, cell death, or cell proliferation compared to unexposed control cancer cells. Mechanistically, exposure to SS smoke extract significantly reduced the expression of cisplatin influx transporter CTR1, and increased the expression of multidrug-resistant proteins ABCG2 and ATP7A. Our study is the first to document that exposure to SHS can increase cisplatin resistance by altering the expression of several proteins involved in multidrug resistance, thus increasing the cells' capability to evade cisplatin-induced cell death. These findings emphasize the urgent need for clinicians to consider the potential role of SHS on treatment outcomes and to advise cancer patients and caregivers on the potential benefits of avoiding SHS exposure. [ABSTRACT FROM AUTHOR]

In the present study, CV dye, known as a recalcitrant dye, was tested for bioremediation via Trichoderma harzianum in a dual-chambered MFC for the first time. Two types of carbon clothes, KIP and CSV from the Dacarb company (France), were tested as electrodes and supported for fungi growth. We first observed that 52% and 55% of the CV were removed by the MFC using KIP and CSV anodes, respectively. The incomplete removal of VC was explained by the relative toxicity of VC to T. harzianum and correlated with IC50 determined as 0.97 ± 0.28 mg L−1 at 25 °C. Furthermore, the MFC working with the KIP electrode was more efficient with a higher maximum power density of 1096 mW m−3 and was only 14.1 mW m−3 for CSV. The MFC experiments conducted on KIP without the T. harzianum biofilm exhibited significantly lower potential and power density values, which proves the electrocatalytic effect of this fungus. These results provide new insight into the development of an effective MFC system capable of direct energy generation and, at the same time, promoting the bioremediation of the persistent CV pollutant. [ABSTRACT FROM AUTHOR]