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This study investigates the potential of flavonoid compounds from Sandoricum koetjape leaf extracts as tyrosinase inhibitors, using in vitro and in silico methodologies. Tyrosinase is crucial for melanin synthesis, and its excessive activity leads to hyperpigmentation disorders. The extracts underwent maceration, partitioning, and concentration, followed by tyrosinase inhibition assays and LC-MS/MS analysis. The ethyl acetate fraction showed the highest inhibitory activity, revealing key flavonoids like Kaempferol-3-O-β-Dglucopyranoside and Quercimeritrin. Molecular docking and dynamic simulations provided insights into their binding mechanisms. Kaempferol-3-Oβ-D-glucopyranoside exhibited a binding affinity of -8.4 kcal/mol, while Quercimeritrin had -7.7 kcal/mol. PreADME profiles indicated Quercimeritrin’s higher solubility, better skin permeability, and lower environmental toxicity. This comprehensive evaluation underscores the viability of S. koetjape as a natural source for tyrosinase inhibitors, highlighting the need for further optimization and in vivo studies to confirm efficacy and safety for dermatological applications.

Foodborne pathogens may cause foodborne illness, which is among the major health problems worldwide. Since the therapeutic options for the treatment of the disease are becoming limited as a result of antibacterial resistance, there is an increasing interest to search for new alternatives of antibacterial. Bioactive essential oils from Curcuma sp become potential sources of novel antibacterial substances. The antibacterial activity of Curcuma heyneana essential oil (CHEO) was evaluated against Escherichia coli, Salmonella typhi, Shigella sonnei, and Bacillus cereus. The principal constituents of CHEO are ar-turmerone, β-turmerone, α-zingiberene, α-terpinolene, 1,8-cineole, and camphor. CHEO exhibited the strongest antibacterial activity against E. coli with a MIC of 3.9 µg/mL, which is comparable to that of tetracycline. The combination of CHEO (0.97 µg/mL) and tetracycline (0.48 µg/mL) produced a synergistic effect with a FICI of 0.37. Time-kill assay confirmed that CHEO enhanced the activity of tetracycline. The mixture disrupted membrane permeability of E. coli and induced cell death. CHEO at MIC of 3.9 and 6.8 µg/mL significantly reduced the formation of biofilm in E. coli. The findings suggest that CHEO has the potential to be an alternative source of antibacterial agents against foodborne pathogens, particularly E. coli. [ABSTRACT FROM AUTHOR]

Currenty, Citrus reticulata has been found to modulate RAW 264.7 macrophage cell line. In the present study, the immunomodulatory effects of Citrus species peel extracts, including Citrus microcarpa, C. limon L., C. sinensis L. and C. hystrix were investigated on cellular immune responses in Wistar rats and mice. Mice were treated with ethanol extracts of Citrus species orally at dosages of 25, 50 and 100 mg/kg bw for 7 days. The phagocytosis activity of the extracts was examined using the carbon clearance method. Meanwhile, oral administration of Citrus species ethanol extracts at dosages of 17.5, 35 and 70 mg/kg bw was administered to Wistar rats to assess the effect of extracts on the delayed-type hypersensitivity (DTH) response using paw edema-method. Thin Layer Chromatography (TLC)-densitometry analysis was also performed. In both animal models, all extracts enhanced the cellular immune responses. Amongst the samples, C. sinensis, at the dose of 100 mg/kg bw in mice and 70 mg/kb bw in rats, demonstrated the highest stimulation on phagocytosis activity and DTH response, respectively. Except C. microcarpa, rutin was found in all Citrus species. The results indicate that Citrus species, particularly C. sinensis, have the potential to be developed into a potent immunostimulatory agent. [ABSTRACT FROM AUTHOR]

Adenostemma lavenia (L.) is one of the medicinal plants on Nias Island that is used to treat many symptoms including cough, fever and diarrhea. Empirical data of this plant suggests that these medicinal benefits can be attributed to its antibacterial and antioxidant properties, as well as the total flavonoids contained within it, but research on this is still limited. Adenostemma lavenia (L.) was extracted with ethanol, while the antibacterial properties were measured using the disc method. Antioxidant testing was conducted with the DPPH (1,1-diphenyl-2-2picrihydrazyl) inhibition method. Total flavonoids were assessed using a modified AlCl3 method with a quercetin standard. Antibacterial test results of Staphylococcus aureus, Klebsiela pneumoniae, Propionibacterium acnes, Escherichia coli, Salmonella typhi, Bacillus cereus and Shigella sonnei with mean inhibition were 8.76 ± 0.44, 8.13 ± 0.72, 8.77 ± 0.45, 6.47 ± 0.54, 7.77 ± 0.60, 7.33 ± 0.44, 12.06 ± 0.60 respectively. IC50 was 59.844 ± 3.36 ppm. Total flavonoids were 13.566 ± 0.021 mcg/g. The results of the antibacterial test of the ethanolic extract of Adenostemma lavenia (L.) were classified as moderate. The antioxidant activity and total flavonoids were in the high category, which can be attributed to the capture of free radicals to overcome disease. [ABSTRACT FROM AUTHOR]

The anti‐inflammatory and immunosuppressive activities of plant secondary metabolites are due to their diverse mechanisms of action against multifarious molecular targets such as modulation of the complex immune system associated with rheumatoid arthritis (RA). This review discussed and critically analyzed the potent anti‐inflammatory and immunosuppressive effects of several phytochemicals and their underlying mechanisms in association with RA in experimental studies, including preliminary clinical studies of some of them. A wide range of phytochemicals including phenols, flavonoids, chalcones, xanthones, terpenoids, alkaloids, and glycosides have shown significant immunosuppressive and anti‐inflammatory activities in experimental RA models and a few have undergone clinical trials for their efficacy and safety in reducing RA symptoms and improve patient outcomes. These phytochemicals have potential as safer alternatives to the existing drugs in the management of RA, which possess a wide range of serious side effects. Sufficient preclinical studies on safety and efficacy of these phytochemicals must be performed prior to proper clinical studies. Further studies are needed to address the barriers that have so far limited their human use before the therapeutic potential of these plant‐based chemicals as anti‐arthritic agents in the treatment of RA is fully realized. [ABSTRACT FROM AUTHOR]

The presence of cancer stem cells (CSCs) in lung cancer could contribute to cancer development and unsuccessful treatment. β-Catenin protein has been found to play a crucial role in cell survival. As artocarpin has been postulated to exert important antitumor properties, this research was conducted to elucidate the effect of artocarpin in the suppression of CSCs through modulating the β-Catenin signalling pathway. Using isolated CSCs from lung adenocarcinoma cell lines (H460), the potential of artocarpin in suppressing CSC was assessed using MTT assay. The stemness gene expression was analysed using real-time quantitative polymerase chain reaction; meanwhile, the assessment of artocarpin binding affinity against the β-Catenin active site was performed using docking analysis and validated with RT-qPCR. A 62.5% of lung CD166+CD44+ CSCs cells and 37.5% of lung CD166-CD44-non-CSCs cells were identified in the H460 cell line. The results revealed that artocarpin exerted the highest cytotoxic value against lung CD166+CD44+ CSCs with an IC50 value of 5.07 μg/mL compared to CD166-CD44-non-CSCs and H460 cells which were 8.67 μg/mL and 9.07 μg/mL, respectively. Additionally, the expression of stemness genes such as KLF4, SOX2, and NANOG was found to be significantly reduced (P< 0.05) in the treated lung CSCs with fold change (FC) values of 0.025, 0.104, 0.074, respectively in 10 μM artocarpin. The molecular docking analysis showed that artocarpin possessed the best-docked complexes with β-Catenin and WNT protein with high binding energy values (-7.04 kcal/mol and -14.91 kcal/mol), respectively compared to other WNT/β-Catenin inhibitors including isorhamnetin, fisetin, genistein, silibinin, catechin, luteolin, coumestrol and β-naphthoflavone. These findings support the inhibitory activity of artocarpin on lung C SCs w ith l ow W NT a nd β -Catenin gene expression levels and FC values (0.155, P<0.01 and 0.129, P<0.05) in 10 μM artocarpin compared to untreated cells, respectively. Therefore, based on this study, it is suggested that artocarpin has the potential to be developed as a therapeutic agent to inhibit stem cell regeneration in lung cancer via the WNT/β-Catenin signalling pathway through inhibition of TCF-4/β-Catenin complex formation. [ABSTRACT FROM AUTHOR]

According to Basic Health Research data in Indonesia in 2020 shows that the diarrhea morbidity rate in Indonesia is still high. In Indonesia, the unripe fruit of the Kayu banana (Musa paradisiaca L. var. Kayu) is a drug that is often used empirically by the people of Senduro village, Lumajang, East Java, Indonesia, to treat diarrhea. This study was conducted to investigate the antibacterial activity of unripe fruit peel, unripe fruit flesh and unripe fruit. A disc diffusion test was selected to assess the sensitivity of each sample to Escherichia coli. The disc dilution was used to determine the value of MIC and MBC in Escherichia coli. Total phenolic content to determine phenolic levels in samples that are suspected of providing antibacterial activity. Analysis of secondary metabolite profiles using the UPLC-Q-TOF/MS instrument. Unripe fruit peel extract shows more optimal antibacterial activity compared to other extracts. The diameter value of the inhibitory zone of the unripe fruit peel extract is 17 mm and the yield of a large ΔOD is -1.3620 at a concentration of 10 % w/v. Based on the calculation results from the regression equation, TPC fruit extract was obtained by 8.6 %, TPC flesh extracts by 6.1 % and TPC from bark extract by 10.8 %. Based on the data from the interpretation of compound content analysis using UPLC-QToFMS, it can be seen that there are 25 mayor compounds. These results suggest that the unripe fruit peel extract of banana Kayu has the potential to be antibacterial against Escherichia coli. The application of this research is as a reference for the development of antidiarrheal standardized herbal medicines and the implication of this research is to support the independence of national medicinal raw materials in Indonesia. [ABSTRACT FROM AUTHOR]

The emergence and spread of antimalarial drug resistance have become a significant problem worldwide. The search for natural products to develop novel antimalarial drugs is challenging. Therefore, this study aimed to assess the antimalarial and toxicological effects of Chan-Ta-Lee-La (CTLL) and Pra-Sa-Chan-Dang (PSCD) formulations and their plant ingredients. The crude extracts of CTLL and PSCD formulations and their plant ingredients were evaluated for in vitro antimalarial activity using Plasmodium lactate dehydrogenase enzyme and toxicity to Vero and HepG2 cells using the tetrazolium salt method. An extract from the CTLL and PSCD formulations exhibiting the highest selectivity index value was selected for further investigation using Peter's 4-day suppressive test, curative test, prophylactic test, and acute oral toxicity in mice. The phytochemical constituents were characterized using gas chromatography-mass spectrometry (GC-MS). Results showed that ethanolic extracts of CTLL and PSCD formulations possessed high antimalarial activity (half maximal inhibitory concentration = 4.88, and 4.19 g/mL, respectively) with low cytotoxicity. Ethanolic extracts of the CTLL and PSCD formulations demonstrated a significant dose-dependent decrease in parasitemia in mice. The ethanolic CTLL extract showed the greatest suppressive effect after 4 days of suppressive (89.80%) and curative (35.94%) testing at a dose of 600 mg/kg. Moreover, ethanolic PSCD extract showed the highest suppressive effect in the prophylactic test (65.82%) at a dose of 600 mg/kg. There was no acute toxicity in mice treated with ethanolic CTLL and PSCD extracts at 2,000 mg/kg bodyweight. GC-MS analysis revealed that the most abundant compounds in the ethanolic CTLL extract were linderol, isoborneol, eudesmol, linoleic acid, and oleic acid, whereas ethyl 4-methoxycinnamate was the most commonly found compound in the ethanolic PSCD extract, followed by 3-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-4H-chromen-4-one, flamenol, oleic acid amide, linoleic acid, and oleic acid. In conclusions, ethanolic CTLL and PSCD extracts exhibited high antimalarial efficacy in vitro. The ethanolic CTLL extract at a dose of 600 mg/kg exhibited the highest antimalarial activity in the 4-day suppressive and curative tests, whereas the ethanolic PSCD extract at a dose of 600 mg/kg showed the highest antimalarial activity in the prophylactic test. [ABSTRACT FROM AUTHOR]