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Endometriosis is a gynecological disease in the form of chronic inflammation characterized by the presence of tissue outside the uterine cavity that affects around 176 million women around the world. The pathogenesis of this disease is still unknown, resulting in a lack of standard treatment. People in East Nusa Tenggara, Indonesia, use boiled water from the cortex of Sterculia quadrifida R.Br. as a menstrual laxative and to treat menstrual pain, believed to be associated with endometriosis. The aim of this study was to investigate how a water extract of the S. quadrifida cortex prevents endometriosis lesions from growing in mice (Mus musculus) endometriosis models. This study was conducted as a true experimental research, dividing the mice into a control group and three SWE groups at doses of 200, 400, and 800 mg/kgBW. The findings showed that all SWE doses can significantly reduce endometriosis lesions and NF-κB expression compared to the negative control, with the optimal dose being 800 mg/kgBW. This activity was predicted due to its flavonoid compounds. These findings demonstrate the significant potential of S. quadrifida cortex as a developed herbal medicine for endometriosis treatment. [ABSTRACT FROM AUTHOR]

Luvunga scandens is traditionally used for malaria, antibacterial, antifungal, antidote to snake bites, and against scorpion stings. Based on the ethnomedicine approach, we focus to explored the antimalarial effect of L. scandens. The stem and leaves of L. scandens were gradually extracted with n-hexane, dichloromethane, and methanol. All samples were examined antimalarial against Plasmodium falciparum 3D7 and cytotoxicities against HepG2 cell lines. The active extract was fractionated by Vacuum Liquid Chromatography (VLC) and the fractions obtained were further tested for antimalarial and cytotoxicity. The most potent extracts against P. falciparum were the dichloromethane extracts of L. scandens leaves (LS-L-D) and stem (LS-S-D), with IC50 values of (6.61±0.04 µg/mL) and (5.38±0.01 µg/mL), respectively. Both extracts were found to be safe and effective because their selectivity indices (SI) values were greater than 2. Based on the antimalarial activity, toxicity, and percentage of yield, we fractionated LS-L-D using VLC, and obtained 26 fractions (F1-F26). Fraction 23 (F23) was identified as the most active fraction with an IC50 value of 2.44±0.09 µg/mL and CC50 value of 46.35±0.03. The HPLC profile of F23 shows several peaks. The major peak has a UV spectrum with maximum absorption at wavelengths of 247, 257, and 322 nm, respectively, indicating the characteristics of the flavonoid compound group, especially isoflavones. This data suggested that isoflavones possibly take a role in the antimalarial activity of fraction 23. Further study needs to be conducted to isolate and identify the active compounds from this fraction. [ABSTRACT FROM AUTHOR]

Malaria is one of the tropical diseases that become a health problem worldwide. The elimination of this disease faced various burdens, leading to the need for new antimalarial drugs. Based on the previously reported antimalarial activity of Artocarpus genus, Artocarpus sericicarpus has been selected as one of the candidates which are potential to be explored as a source of antimalarial substances. This study aimed to obtain active antimalarial fractions from A. sericicarpus leaves. Extraction of A. sericicarpus leaves was conducted by ultrasonic-assisted extraction using nhexane, dichloromethane, and methanol as solvents. All extracts were tested for their antimalarial activity by Lactate Dehydrogenase (LDH) assay. The most active extract was fractionated by Vacuum Liquid Chromatography (VLC) and fractions were further tested by LDH assay as well. Cytotoxicity test conducted by resazurin assay on several cell lines to determine the active and nontoxic fractions which have the potential to be further purified and identified the active substances. The n-hexane, dichloromethane, and methanol extract showed antimalarial activity with IC50 values of 23.96±0.06 μg/mL, 2.72±0.08 μg/mL, and 23.39±0.05 μg/mL, respectively. Dichloromethane extract was chosen for further separation due to its highest antimalarial activity. The separation was obtained in nine fractions. Fractions 2-9 had an IC50 value of less than 10 μg/mL, indicating an active antimalarial substance. Meanwhile, fraction 1 has moderate antimalarial activity. Cytotoxicity test results considered all fractions to be non-toxic. The TLC profile of dichloromethane extract identified polyphenolic compounds, suggesting the active polyphenolic compounds can be further isolated from the active fractions (F2-F9). [ABSTRACT FROM AUTHOR]

This research aims to discover active compounds from the leaf extract from Cratoxylum glaucum using the bioassay-guided isolation method. The multistage extraction of C. glaucum leaves was conducted using n-hexane, dichloromethane, and methanol. The LDH assay was employed to analyze antimalarial activity, and the Resazurin assay was used to measure cytotoxicity values. The structure of the active isolates was determined using spectroscopic techniques. The compound 1 was successfully isolated from the dichloromethane extract of C. glaucum leaves (Cg.FD) and confirmed as a prenylated xanthone namely cratoxyarborenone E. The in vitro antimalarial activity showed an IC50 value of 5.82 ± 0.04 μM, the cytotoxicity assay exhibited a CC50 value of 20.74 ± 0.04 µM, and the SI value was determined to be 3.56. Our research demonstrates that cratoxyarborenone E was first reported from Cg.FD and shows promise as a prospective candidate for new antimalarial drugs. [ABSTRACT FROM AUTHOR]

Andrographis paniculata tablets (AS201-01) have previously been shown to have potent bioactivity as an antimalarial and to produce no unwanted side effects in animal models. Here, we present the phase 1 clinical trial conducted to evaluate the safety of AS201-01 tablets in healthy volunteers. The study was a randomized, double-blind controlled cross-over, a placebo-controlled design consisting of a 4-day treatment of AS201-01 tablets. A total of 30 healthy human volunteers (16 males and 14 females) were divided into two groups, and each group was given 4 tablets, twice daily for 4 days. Group 1 received AS201-01, while group 2 received placebo tablets. Volunteers were given a physical examination before the treatment. The effects of AS201-01 on random blood glucose, biochemical, and hematological as well as urine profiles were investigated. There were no changes in observed parameters as a result of AS201-01 being administered. Statistical analysis showed no significant difference (p>0.05) between the test and control group regarding hematology profile, biochemical profile, and random blood glucose. Increased appetite and better sleep, which categorized as grade 1 adverse event was reported after treatment with AS201-01 tablet The outcome supports our previous observation that the AS201-01 tablet, given twice a day for 4 days, is safe and nontoxic. [ABSTRACT FROM AUTHOR]

Centella asiatica (L.) is a medicinal plant with anti-inflammatory, anti-asthmatic, antihemorrhoidal, wound healing, and antioxidant effects. Currently, the dry extract of Centella asiatica is widely produced by various industries. It is necessary to determine the quality of the extracts on the market. The aims of this study are to develop the asiaticoside assay method using TLC-densitometry, identification of the compound groups, and determination of the antioxidant activity of Centella asiatica dry extracts and Centella asiatica extract on-market products. The phytochemical content of Centella asiatica extracts was evaluated using the TLC-densitometry method. The validation of the analysis method for asiaticoside assay was subsequently carried out, as well as the determination of antioxidant activity using the DPPH method. The method validation results showed that the TLC-densitometry method met the validation parameter criteria. Asiaticoside assay of the dry extract, simplicia, and on-market extract products were 9.07, 0.10, 0.60, and 10.53%, respectively. Furthermore, the results of the antioxidant activity of the dry extract and on-market extract products showed an IC50 value of 0.1166, 0.5783, and 1.9513 mg/mL, respectively. This study obtained a valid method for analyzing asiaticoside assay using the TLC-densitometry method. Asiaticoside content of dry extract was 9,07%, and extract products on-market were 0,60% and 10,53%, respectively. The IC50 value of the dry extract of Centella asiatica was in the moderate antioxidant category, while the on-market extract products were in the very weak antioxidant category. [ABSTRACT FROM AUTHOR]

Background: Artocarpus altilis leaf extract (AAL.E) was separated by VLC, and six fractions were obtained. Fraction 5 (AAL.E.5) showed antimalarial activity with an IC50 value of 3.71 µg/mL. Objective: This study aimed to determine the antimalarial activity of AAL.E.5 subfractions against P. falciparum, the mechanism of action against Plasmodium Falciparum Malate quinone oxidoreductase (PfMQO), and the active substances. Methods: The AAL.E.5 was separated by open-column chromatography and eluted with chloroform-methanol gradient elution in order of increasing polarity. The antimalarial activity of all subfractions was assessed using a lactate dehydrogenase (LDH) assay against P. falciparum and the mechanism of action of the PfMQO enzyme. The profiles of the most active subfractions were analyzed using High-Performance Liquid Chromatography (HPLC). Results: The separation of fraction 5 (AAL.E.5) yielded 11 subfractions (AAL.E.5.1–AAL.E.5.11). Screening antimalarial activity at 10 μg/mL in this subfraction showed that only five subfractions (AAL.E.5.6-AAL. E.5.10) inhibited P. falciparum and two subfractions (AAL.E.5.6 and AAL.E.5.10) inhibited the PfMQO enzyme. Only subfraction 6 (AAL.E.5.6) inhibited both, with IC50 values of 6.609 µg/mL and 20.34 µg/mL. The thin layer chromatography profile of AAL.E.5.6 revealed reddish-orange spots, indicating the presence of flavonoid compounds, and was also presumed from the UV-visible to HPLC chromatogram for band I in the 300 – 400 nm range and band II in the 240–285 nm range. Conclusion: Subfraction 6 has antimalarial activity against P. falciparum and is thought to have a mechanism of action in PfMQO. Based on the TLC, HPLC, and UV-Vis spectra, subfraction 6 was assumed to be a flavonoid. [ABSTRACT FROM AUTHOR]

Treatments of hepatitis C virus have been developed and increased the sustained virology response (SVR), however, there are several reports of drug resistance, high-cost issue, and limited access to current hepatitis C virus (HCV) treatment that remain become a problem. This necessitates to search for complementary and alternative drugs against HCV, therefore the investigation of active compounds from plant extracts such as Melicope latifolia, a plant that has been reported as anti-HCV, will be provided in this study. The anti-HCV activities were tested using in vitro cultured cells of hepatocyte cell line Huh 7.5 and HCV genotype 2a (J6/JFH1). Ethanol extract of M. latifolia leaves was separated by chromatographic methods and the chemical structures of the isolated compounds were established based on mass spectrometry, 1D, and 2D nuclear magnetic resonance spectral data, as well as comparison with reported data. The interaction of the compound with the protein, which involves to HCV activity, was determined by docking analysis. Three known methoxyflavone compounds identified as 5,4'-dihydroxy-7-prenyloxy-3,8,5'-trimethoxyflavone (1); 5,3'-dihydroxy-3,7,8,4'-tetramethoxyflavone (2); and 5-hydroxy-3,7,8,3',4'-pentamethoxyflavone (3) were isolated from the ethanolic extract of M. latifolia leaves. Anti-HCV activities revealed that compound (1) strongly inhibited HCV J6/JFH1 with a 50% inhibitory concentration (IC50) value of 6.7±0.4 µg/mL and 50% cytotoxic concentration (CC50) of 19.3 µg/mL. The docking analysis revealed an interaction with the 4GAG, a protein that involves in the entry step of HCV, and the 4EAW protein which plays an important role during HCV replication. [ABSTRACT FROM AUTHOR]