In vitro and in silico studies of the potential cytotoxic, antioxidant, and HMG CoA reductase inhibitory effects of chitin from Indonesia mangrove crab (Scylla serrata) shells.

This study aimed to characterize chitin extracted from Indonesia mangrove crab (Scylla serrata) shells, as well as to assess its in vitro cytotoxic, antioxidant, and HMG CoA reductase inhibitory potentials. In silico molecular docking, molecular dynamic, and ADMET prediction analyses were also carried out. Chitin was extracted from mangrove crab shells using deproteination and demineralization processes, Scanning Electron Microscopy (SEM) and Fourier Transform Infrared (FTIR) characterization are then performed. The MTT method was further tested in a study of cell viability, while in vitro method was used to assess HMG CoA reductase inhibitory and antioxidant activities. The extracted chitin was found to have a moderate level of cytotoxic and antioxidant activities. In vitro studies showed that it has an IC50 of 36,65 ± 0,082 µg/mL as an HMG CoA reductase inhibitor, and decreased enzyme activity by 68.733 % at 100 µg/mL as a concentration. Furthermore, in the in silico study, chitin showed a strong affinity to several targets, including HMG CoA reductase, HMG synthase, LDL receptor, PPAR-alfa, and HCAR-2 with binding energies of -5.7; -5.8; -3.6; -5.6; -4.6 kcal/mol, respectively. Based on the ADMET properties, it had non-toxic molecules, which were absorbed and distributed across the blood-brain barrier. The molecular dynamics (MD) simulation also showed that it remained stable in the active sites of HMG CoA reductase receptor for 100 ns. These results indicated that chitin from Indonesian mangrove crab shells can be used to develop more potent HMG CoA reductase inhibitor with antioxidant and cytotoxic activities for effective dyslipidemia therapy.

Antioxidant Activities of Stem, Leaves and Fruits Extracts of Pepino (Solanum muricatum Aiton).

<b>Background and Objective:</b> Pepino (<i>Solanum muricatum</i> Aiton), rich with vitamin C and flavonoids, constitutes an abundant source of potent antioxidants. This research was conducted to determine antioxidant activity from three different parts of pepino based on equivalence with ascorbic acid, to analyze the relationship between total phenolic content (TPC) and total flavonoid content (TFC) on antioxidant activities and to determine flavonoid compounds. <b>Materials and Methods:</b> Antioxidant activities were determined using 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) and Cupric Ion Reducing Antioxidant Capacity (CUPRAC) methods. The TPC and TFC were determined by UV-visible spectrophotometry. The correlation between TPC, TFC and antioxidant activity was analyzed using Pearson's method. Flavonoid compound content was performed by HPLC. <b>Results:</b> The ethyl acetate pepino fruit extract expressed the highest antioxidant activity by DPPH and CUPRAC assays. The highest TPC was obtained from the ethyl acetate extract of pepino stem (18.493 g GAE/(100 g)), while the highest TFC was obtained from the hexane extract of pepino leaves (9.541 g QE/(100 g)). <b>Conclusion:</b> The DPPH and CUPRAC assays demonstrated that pepino exhibits potential as a source of natural antioxidants, especially in its fruit part.

Antibacterial and antioxidant activities in various parts of Artocarpus lacucha Buch. Ham. ethanolic extract.

Artocarpus lacucha is an endemic plant to North Sumatera, Indonesia. This plant has pharmacological activities, including acting as an antioxidant and antibacterial. The aim of the present study was to analyze the antibacterial and antioxidant activities, and determine the flavonoid compounds from four parts of A. lachuca, namely leaves, barks, twigs and fruits. Antioxidant activity was investigated using the 2,2-diphenyl 1-picrylhydrazyl (DPPH) and cupric reducing antioxidant capacity (CUPRAC) methods. Antibacterial activity was analyzed using disk diffusion and microdilution methods. Several flavonoids, such as luteolin-7-O-glucoside, rutin, quercetin, kaempferol and apigenin, were determined using high performance liquid chromatography. Based on the antioxidant activity test results using the DPPH method, the bark ethanolic extract provided the highest antioxidant capacity, while the CUPRAC method indicated that the twig ethanolic extract had the highest antioxidant capacity. The antibacterial activity test results demonstrated that at a low concentration of 750 µg/disk the bark ethanolic extract obtained the highest inhibition zone and minimum inhibitory concentration level against six of nine pathogenic bacteria. Therefore, A. lachuca bark ethanolic extract could be potentially developed as antioxidant and antibacterial agents.

In Vivo Pharmacodynamics of Calophyllum soulattri as Antiobesity with In Silico Molecular Docking and ADME/Pharmacokinetic Prediction Studies.

This study aims to determine the antiobesity activity of Calophyllum soulattri leaves extract (CSLE) on high fat diet-fed rats (HFD) and to predict the molecular docking and pharmacokinetics of selected compounds of Calophyllum soulattri to fat mass and obesity-associated protein (FTO). Daily body weight, organ, carcass fat (renal and anal), body mass index, total cholesterol, and total triglyceride levels were observed after CSLE was given orally for 50 days. Furthermore, body mass index of a CSLE dose of 50 mg/kgbw, 100 mg/kgbw and orlistat (120 mg/kgbw) group are 0.68, 0.57 and 0.52, respectively. The total body weight of the CLSE dose of 100 mg/kgbw group showed the lowest percentage change, followed by a CLSE dose of 50 mg/kgbw compared to the normal and positive control group. The carcass fat index of CSLE dose of 100 mg/kgbw was not significantly different from orlistat, which was in line with its total cholesterol level and triglyceride (p < 0.05). The binding affinity of selected compounds from Calophyllum soulattri (friedelin, caloxanthone B, macluraxanthone, stigmasterol, trapezifolixanthone, dombakinaxanthone, and brasixanthone B) to FTO are -8.27, -9.74, -8.48, -9.34, -8.85, -8.68 and -9.39 kcal/mol, which are better than that of orlistat at -4.80 kcal/mol. The molecular dynamics simulation showed that the interaction between Caloxanthone B compounds and obesity receptors was relatively stable. Lipinski's rule determined the absorption percentage of all compounds above 90% with good drug-likeness. The results showed the potential of CSLE as an antiobesity drug candidate.

Novel Insight into Pickering Emulsion and Colloidal Particle Network Construction of Basil Extract for Enhancing Antioxidant and UV-B-Induced Antiaging Activities.

We developed a facile preparation method of oil-in-water (O/W) Pickering emulsion in an emollient formulation using basil extract (Ocimum americanum L.) as a solid particle stabilizer by fine-tuning the concentration and mixing steps of common cosmetic formulas, such as humectants (hexylene glycol and glycerol), surfactant (Tween 20), and moisturizer (urea). The hydrophobicity of the main phenolic compounds of basil extract (BE), namely, salvigenin, eupatorin, rosmarinic acid, and lariciresinol, supported high interfacial coverage to prevent coalescence of globules. Meanwhile, the presence of carboxyl and hydroxyl groups of these compounds provides active sites for stabilizing the emulsion using urea through the formation of hydrogen bonds. Addition of humectants directed the in situ synthesis of colloidal particles during emulsification. In addition, the presence of Tween 20 can simultaneously reduce the surface tension of the oil but tends to inhibit the adsorption of solid particles at high concentrations, which otherwise formed colloidal particles in water. The level of urea and Tween 20 determined the stabilization system of the O/W emulsion, whether interfacial solid adsorption (Pickering emulsion, PE) or colloidal network (CN). Variation of the partition coefficient of the phenolic compounds present in basil extract facilitated the formation of a mixed PE and CN system with better stability. The addition of excess urea induced interfacial solid particle detachment, which caused the oil droplet enlargement. The choice of stabilization system determined the control of antioxidant activity, diffusion through lipid membranes, and cellular antiaging effects in UV-B-irradiated fibroblasts. Particle sizes of less than 200 nm were found in both stabilization systems, which is beneficial for maximizing their effects. In conclusion, this study provides a technological platform to realize the demand for natural dermal cosmetic and pharmaceutical products with strong antiaging effects.

Potential Antioxidative Activity of Waste Product of Purple Sweet Potato (Ipomoea batatas Lam.).

<b>Background and Objective:</b> Antioxidants are substances that can deactivate free radicals. Phenol and flavonoid are antioxidant compounds widely found in plants, including purple sweet potato (<i>Ipomoea batatas</i> L.). This research aimed to investigate three purple sweet potato-based organs' antioxidative activity and flavonoid contents. <b>Materials and Methods:</b> Antioxidative activities, total phenolic content and total flavonoid content were performed by UV-visible spectrophotometry. Pearson's method analyzed the correlation of TPC and TFC with antioxidative activities and the correlation between two antioxidative testing methods. <b>Results:</b> Antioxidative activity of three organs purple sweet potato using DPPH method showed values varied from 6.572-290.894 mg AAE g¹ and using CUPRAC method varied from 25.169-621.254 mg AAE g¹. The highest TPC was found in ethanolic leaves extract (20.885 g GAE 100 g¹), while the highest TFC was found in ethyl acetate leaves extract (10.048 g QE 100 g¹). <b>Conclusion:</b> DPPH and CUPRAC tests revealed that purple sweet potato leaves, stem and tuber extracts were potent antioxidants. The potential antioxidative activity was found in the waste product of purple sweet potatoes (leaves and stem). Phenol and flavonoid compounds had contributors to antioxidative activity. DPPH and CUPRAC methods gave linear results for most of the antioxidative activity in three organs of purple sweet potato. Ethanol stem extract contained luteolin 7-O-glucoside, rutin, quercetin, kaempferol and apigenin. Rutin had the highest content, which was 0.399%.

Effect of Banana (Musa sp.) Peels Extract in Nanoemulsion Dosage Forms for the Improvement of Memory: In Vitro & In Vivo Studies.

BACKGROUND: Banana (Musa sp.) is a plant rich in phytochemical compounds, especially antioxidants, which are hypothesized to inhibit the activity of acetylcholinesterase, an enzyme associated with Alzheimer's Disease. OBJECTIVE: This research aimed to study nanoemulsion preparations of Kepok banana (KEP-NE) and Tanduk banana (TAN-NE) peel extracts for their activities as antioxidants, acetylcholinesterase as well as tyrosinase inhibitors, and as agents to improve short-term memory. METHODS: Nanoemulsion was prepared using a combination of high shear homogenization and ultrasonication. The antioxidant activity test was carried out using DPPH and ABTS methods. Meanwhile, memory improvement was studied in a mouse model with memory impairment induced by alloxan (120 mg/kg b.w) using the Y-maze apparatus. ELISA performed determination of acetylcholinesterase and tyrosinase inhibition. RESULTS: Characterization of the nanoemulsion was performed to include particle size, antioxidant activity, acetylcholinesterase, and tyrosinase inhibition. The particle size and polydispersity index (PI) of KEP-NE and TAN-NE were 84.2 nm (PI: 0.280) and 94.1 nm (PI: 0.282), respectively. The antioxidant activity of DPPH showed that the respective IC50 values of KEP-NE and TAN-NE were 0.64 µg/mL and 1.97 µg/mL. At the same time, the values with the ABTS method were 1.10 µg/mL and 1.72 µg/mL, respectively. The IC50 of KEP-NE on acetylcholinesterase inhibition was 108.80 µg/mL, and that on tyrosinase inhibition was 251.47 µg/mL. The study of short-term memory in the Y-maze revealed that the groups Kepok peel extracts 100 and 300 mg/kg b.w and KEP-NE 100 and 300 mg/kg b.w significantly (P < 0.05) improved short-term memory. CONCLUSION: This study suggests that the nanoemulsion dosage form of Kepok banana peel extract has antioxidant and acetylcholinesterase inhibition and tyrosinase inhibition activities and could potentially be an adjunct alternative treatment for memory disorders. Modifying the smaller drug particle size contributes to the delivery system. The nanoemulsion can increase pharmacological activity.

Crystal Guava (Psidium guajava L. "Crystal"): Evaluation of In Vitro Antioxidant Capacities and Phytochemical Content.

Free radicals can cause many diseases, such as cancer. Antioxidant is a compound that could scavenge free radicals. One of the natural antioxidants is guava. The goals of this research were to investigate the antioxidant activity of leaves and fruit of crystal guava by determining the value of the Antioxidant Activity Index (AAI) using DPPH, CUPRAC, and FRAP; evaluate the total phenolic content (TPC) and total flavonoid content (TFC); analyse the correlation between the TPC and TFC with AAI DPPH, CUPRAC, and FRAP, and analyse the correlation between the 3 methods. Extraction was performed by the reflux method using n-hexane, ethyl acetate, and ethanol. Determination of AAI DPPH, CUPRAC, FRAP, the TPC, and the TFC was performed by UV-visible spectrophotometry. The correlation of the TPC and TFC with AAI DPPH, CUPRAC, and FRAP and, also, the correlation of the 3 methods were investigated by Pearson's method. The antioxidant activity of leaves and fruit extracts of crystal guava showed AAI DPPH in the range of 0.33-56.46, CUPRAC 0.20-7.31, and FRAP 1.65-59.89. The highest TPC was given by ethanol leaf extracts (49.55 ± 1.45 g GAE/100 g), while the highest TFC was for n-hexane leaf extracts (9.68 ± 0.210 g QE/100 g). The TPC of leaves extract had a significantly positive correlation with AAI DPPH, CUPRAC, and FRAP. AAI DPPH, AAI CUPRAC, and AAI FRAP of leaves and fruit extract of crystal guava showed a significantly positive correlation. In general, leaves extract had strong antioxidant activity by the three methods. For the highest antioxidant activity, ethanol was the best solvent for extraction leaves and ethyl acetate for extraction fruit of crystal guava. The TPC in leaves extract contributed to the antioxidant activity by DPPH, CUPRAC, and FRAP methods. The Antioxidant activity of leaves and fruit extracts of crystal guava was linear by the three methods.

Antioxidant and antibacterial activities of multiflora honey extracts from the Indonesian Apis cerana bee.

OBJECTIVES: Honey is an apiary product with various medicinal properties resulting from its bioactive compounds. Here, we aimed to determine the antioxidant and antibacterial properties of the Indonesian Apis cerana honey extracts and their correlation with total phenolic content (TPC) and total flavonoid content (TFC). METHODS: We extracted ethyl acetate-n-hexane and two types of ethanolic extracts from crude honey. Phenols and flavonoid content were calculated using spectroscopy. The antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric ion reducing antioxidant power (FRAP) assays, and it was reflected via the antioxidant activity index (AAI). An agar diffusion test was used to test the antimicrobial activity. RESULTS: The ethyl acetate extract of the Karangasem honey provided the highest amount of phenolic and flavonoid content, and the strongest antioxidant activity using DPPH and FRAP assays. The ethanolic honey extracts were active against Bacillus subtilis and Escherichia coli; in this regard, the strongest effect was noticed from the Singaraja honey extract. The positive significant correlations between TPC and AAI were observed in all samples. Similar results also appeared between phenolic and flavonoid compounds and their antibacterial activity in most of the tested samples. CONCLUSIONS: In our study, honey extracts possessed antioxidant and antibacterial activities that were mostly related to the qualitative and quantitative properties of phenols and flavonoids. Geographical origin brought variations in the phytochemical profiles and bioactivities of honey.

Antioxidant potential of two varieties of Sesamum indicum L. collected from Indonesia.

OBJECTIVES: In this study, we aimed to determine the antioxidant activities of two varieties of sesame (Sesamum indicum L.) seeds using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) method, and to investigate the correlation between total phenolic as well as flavonoid contents and antioxidant activities of the extracts. METHODS: The antioxidant activities were determined using DPPH, ABTS, and FRAP assays, and the total phenolic content (TPC) and total flavonoid content (TFC) were measured by ultraviolet (UV)-Vis spectrophotometry. The correlation between total phenolic and flavonoid contents and DPPH IC50, ABTS IC50, and FRAP EC50 values was analyzed by Pearson's method. RESULTS: The IC50 DPPH values of all sesame seed extracts were in the range of 8.88-44.21 µg/mL and IC50 ABTS values were in the range of 24.91-141.19 µg/mL. EC50 FRAP value ranged from 222.40 to 872.57 µg/mL. The highest TPC of 1.57 g gallic acid equivalent (GAE)/100 g was observed in ethanolic extract of black sesame seed, while the highest TFC of 4.29 g quercetin equivalent (QE)/100 g was observed in ethyl acetate extract of white sesame seeds. The TPC in black sesame seed extract was significantly negative correlated with IC50 ABTS value (r = -0.828, p < 0.01) and EC50 FRAP value (r = -0.976, p < 0.01). CONCLUSIONS: All sesame seed extracts were categorized as very strong antioxidants by DPPH assay. Phenolic compounds in black sesame seeds were found to be the major contributors to antioxidant activities by using ABTS and FRAP methods. White and black sesame seeds have the potential to be developed as sources of natural antioxidants.

Correlation of phytochemical content with antioxidant potential of various sweet potato (Ipomoea batatas) in West Java, Indonesia

Objective:To determine antioxidant activity and phytochemical content from various tubers extracts of sweet potato (Ipomoea batatas) and to explore the correlation of phytochemical content with their antioxidant activities.Methods:Antioxidant activities were tested using DPPH and FRAP assays.Total phenolic was calculated by Folin-Cioealteu reagent,flavonoid content by Chang's method and correlation with their antioxidant activities were analyzed by Pearson's method.Results:PO2 showed highest antioxidant activity,which had the lowest IC50 DPPH (10.54 μg/mL) and the lowest EC5o FRAP (11.14 μg/mL).PO2 showed the highest total phenolic (11.91 g GAE/100 g) and total flavonoid content (17.83 g QE/100 g).There were significantly negative correlation between total phenolic content and flavonoid content in sample PO with their IC5o DPPH and EC5o FRAP.IC50 DPPH of sample PP and PO showed significantly positive correlation with their EC5o FRAP.Conclusions:Result of DPPH method shows that all different ethyl acetate and ethanolic tubers extracts of four varieties of sweet potato are classified as strong and very strong antioxidant.Result of DPPH and FRAP methods indicates that phenolic and flavonoid compounds in sample PO contributes together to antioxidant activities.Antioxidant activities of sample PP and PO by DPPH method are linear to FRAP method.

Antibacterial Activity of Ethanolic Extract of Cinnamon Bark, Honey, and Their Combination Effects against Acne-Causing Bacteria.

Propionibacterium acnes and Staphylococcus epidermidis are the major skin bacteria that cause the formation of acne. The present study was conducted to investigate antibacterial activity of ethanolic extract of cinnamon bark, honey, and their combination against acne bacteria. The antibacterial activity of extract of cinnamon bark and honey were investigated against P. acnes and S. epidermidis using disc diffusion. Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were attained using Clinical and Laboratory Standard Institute (CLSI) methods. The interaction between cinnamon bark extract and honey was determined using a checkerboards method. The results showed that the MICs of cinnamon bark extract and honey against P. acne were 256 µg/mL and 50% v/v, respectively, while those against S. epidermidis were 1024 µg/mL and 50% v/v, respectively. The MBC of cinnamon bark extract against P. acnes and S. epidermidis were more than 2048 µg/mL, whereas the MBC for honey against P. acnes and S. epidermidis were 100%. The combination of cinnamon bark extract and honey against P. acnes and S. epidermidis showed additive activity with a fractional inhibitory concentration index (FICI) value of 0.625. Therefore, the combination of cinnamon bark extract and honey has potential activity against acne-causing bacteria.

Activity of Kaempferia pandurata (Roxb.) rhizome ethanol extract against MRSA, MRCNS, MSSA, Bacillus subtilis and Salmonella typhi.

Temu kunci (Kaempferia pandurata (Roxb.)) has a number of benefits and one of these is antibacterial. The rhizome is said to have antibacterial activity against Streptococcus mutans, Lactocillus sp. and Candida albicans. The aim of the study is to test the antibacterial activity of Kaempferia pandurata (Roxb.) rhizome ethanol extract on methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant coagulase negative Staphylococci (MRCNS), methicillin-sensitive Staphylococcus aureus (MSSA), Bacillus subtilis and Salmonella typhi. Antimicrobial activity of the extract was assayed by the microdilution method using Mueller Hinton Broth with sterilized 96 round-bottomed microwells to determine the Minimum Inhibitory Concentration (MIC) as well as to determine the time-kill activity. The MIC of the extract was 16 ppm for both Bacillus subtilis and MRSA; 8 ppm for both MSSA and Salmonella typhi and 4 ppm for MRCNS. Ethanol extract of Kaempferia pandurata (Roxb.) showed antibacterial activity against all the tested bacteria and was the most potent against MRCNS, with MIC 4 ppm. The killing profile test of the extract displayed bactericidal activity at 8-16 ppm against MRSA, MSSA, Bacillus subtilis and Salmonella typhi and bacteriostatic activity at 4 ppm towards MRCNS.