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Preliminary research showed that Cratoxylum sumatranum extract and fractions exhibited antimalarial activity. Two caged xanthone compounds identified as cochinchinone D and cochinchinoxanthone were disengaged from an active portion of the stem bark of C. sumatranum. The purpose of this study is to determine the antimalarial activity of both compounds against Plasmodium falciparum and their in silico prediction on several food vacuole enzymes. Lactate dehydrogenase assay was used to regulate the antimalarial activity, and in silico molecular docking was carried out with a number of receptors, including plasmepsin-II, M1-alanyl aminopeptidase, and falcipain-3. Absorption, distribution, metabolism, excretion, and toxicity (ADME-T) prediction was also conducted for both compounds. The inhibitory concentration (IC50) value for antimalarial activity determination was conducted by probit analysis using GraphPad Prism Version 6.0. Cochinchinone D and cochinchinoxanthone were found to have antimalarial activity, with respective IC50 values of 4.79 µM and 4.41 µM, respectively. Cochinchinone D has a higher affinity for binding to plasmepsin-II, according to in vitro findings. Meanwhile, cochinchinoxanthone and chloroquine as standard have a better affinity to alanyl aminopeptidase. Both compounds have similar ADME-T profiles. Cochinchinone D and cochinchinoxanthone have a high antimalarial activity possibly through the mechanism of inhibition on plasmepsin-II, falcipain-3, and M1-alanyl aminopeptidase enzymes in food vacuole. Both caged compounds have the potential for further development as antimalarial. [ABSTRACT FROM AUTHOR]

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]

Hepatitis C virus (HCV) is an RNA virus with a high mutation rate, making it prone to developing resistance. There is currently no vaccine for this disease, and the existing treatments are often costly. Therefore, this study aimed to provide alternative and complementary antiviral options from plant by evaluating the activity of Piper betle (P. betle) against HCV and its combination with existing antiviral drugs, Ribavirin and Simeprevir. The antiviral inhibition was identified by in vitro culture using Huh7it-1 cells and JFH1a HCV. The phytochemistry profile was also determined by Thin Layer Chromatography (TLC) and High-Performance Liquid Chromatography (HPLC). The result showed that the ethanol extract of P. betle had strong activity with an IC50 value of 0.08 ± 0.028 µg/mL. The mechanism of action showed that the extract dominantly inhibited the post-entry steps. Furthermore, the combination of P. betle extract with simeprevir showed higher anti-HCV activity compared to the single use of the drug, but no effect was observed in the combination with ribavirin. The Western blotting analysis showed that the inhibition of NS3 protein levels was in a dosedependent manner. Based on the phytochemistry evaluation, the extract was found to contain flavonoids, polyphenols, and alkaloids. These results suggested that the ethanolic extract of P. betle could be a good candidate for the development of alternative anti-HCV drugs. [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]

Abstract The study aimed to investigate the antioxidant and cholinesterase inhibitory activities of the leaves and stems of Artocarpus sericicarpus and to analyse the phenolic compounds in the extracts. The modified Ellman's method was used to determine the cholinesterase inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The antioxidant properties were evaluated using DPPH and ABTS methods. The total phenolic content (TPC) was measured by spectrometric assay, and compound identification was carried out by LC-MS/MS analysis. The results showed that the leaf and stem extracts of A. sericicarpus exerted significant inhibitory effects against AChE and BChE, as well as antioxidant activities. The stem ethanolic extract exhibited the highest potency against AChE and BChE with IC50 values of 5.81 and 11.46 µg/mL, respectively. The leaf and stem ethanolic extracts gave higher antioxidant activities and TPC compared to the water-based extracts. The LC-MS/MS analysis indicated the presence of phenolic compounds, such as flavones, flavonols, flavanones, prenylated chalcones, and xanthones in the extracts. [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]

The combination of Luvunga sarmentosa and Eurycoma longifolia is widely prescribed in traditional medicine by the local Dayak tribe in Central Kalimantan, Indonesia. The study aimed to evaluate the effect of antioxidants and analgesics from the combination of hydro-alcoholic extract of L. sarmentosa and E. longifolia stem. The phytochemical investigation was performed using an established method described in the literature. The total phenolic content was determined by the Folin Ciocalteu, whereas the flavonoid was determined by aluminum chloride. The in vitro antioxidant activity was determined using DPPH free radical scavenging assay. The analgesic effect was determined by acetic acid-induced writhing and hot plate tests in male mice. The result shows that combination extract (CE, IC50 162.5±0.21 μg/mL) had higher antioxidant activity than L. sarmentosa extract (LSE, IC50 200.20±0.23 μg/mL) and E. longifolia extract (ELE, IC50 293.45±0.32 μg/mL). All extracts showed significant dose-dependent analgesic activity against acetic acid-induced writhing and hot plate pain models. A higher dose of CE, LSE, and ELE (550 mg/kg) produced significant inhibition of writhing by 67.60±2.76, 56.45±2.34, and 68.64±1.65%, respectively. The maximum possible analgesia of CE, LSE, and ELE in the hot plate test at 550 mg/kg BW dose was 25.32%, 16.04%, and 26.72%. CE has higher analgesic activity than LSE and ELE. The extracts are more effective for peripheral than central analgesia. Its mechanism may be related to inhibiting the inflammatory mediator's release. The high antioxidant and analgesic activity at CE is relevant to the higher total flavones and phenols compared to LSE and ELE. [ABSTRACT FROM AUTHOR]

Background: There are thousands of species of known medicinal plants in the world. Ruta angustifolia L. has been widely used in traditional medication for jaundice and liver disease. Previous studies have shown that R. angustifolia leaves can inhibit the hepatitis C virus in Huhit culture cells, reduce the value of NS3 protein, and possess a synergistic effect in combination with antiviral drugs. Therefore, this plant is potential to be developed as a drug candidate. Characteristics of plants including microscopic, physicochemical properties, and phytochemical profiles are necessary information to ensure the quality of raw material in drug development. Objective: This study was carried out to examine the microscopic and physicochemical including the standardized parameter of R. angustifolia leaves to fulfil the quality raw materials as traditional medicine. Methods: Simplicia of R. angustifolia leaves obtained from Jombang, East Java, were observed under a microscope and determined its physicochemical properties referred to the Materia Medica Indonesia V. The TLC and HPLC profiles of extract were determined as well. Results: Microscopic analysis were conducted by transfection sections and the presence of epidermis cells, palisade, mesophyll with stomata, and Ca-oxalate crystal were found. The standard parameter obtained value of loss of drying, extractive value in water and ethanol, and ash value. The TLC and HPLC profiles of leaves extract demonstrated to contain with flavonoid, terpenoids, and alkaloids. Conclusion: Ruta angustifolia obtained from Jombang, east Java, has a specific character in microscopic analysis. The physicochemical properties analysis of R. angustifolia leaves as a raw material met the requirements according to Materia Medica Indonesia V. [ABSTRACT FROM AUTHOR]

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Background: Hepatitis c virus infection is a global health problem which chronically infected 71 million people in the world. This infection has a risk of becoming liver cirrhosis and hepatocellular carcinoma. Since the current HCV therapy has been developed by direct-acting antivirals (DAA), however, most patients get limited access due to the high cost. Therefore, further development anti-HCV agent still greatly needed. Ruta angustifolia is a natural resource which was reported to possess anti-HCV activity. Ribavirin is an antiviral agent used to treat several virus infections, either DNA or RNA. Ribavirin was known to inhibit HCV infection by regulated immune system in host cells and interfering the replication of HCV by inhibit HCV RdRp. Objective: The current study evaluated the combination treatment of R. angustifolia extracts and ribavirin by in vitro culture cells of Huh 7it. Method: The study was conducted under an invitro cell culture of Huh 7it and infected with JFH1a. Result: The result demonstrated an enhancement effect of the extract by increasing the anti-HCV activity 3.5-fold higher compared to ribavirin alone. The 50% inhibitory concentration of ribavirin by single treatment was 10.43 ± 0.18 µg/mL, while in combination with Ruta angustifolia extract was 2.80 ± 0.03 µg/mL. Further analysis of the combination by CompuSyn software mediated a synergistic effect among the combination with a combination index value of 0.691. Conclusion: These results suggested that combination of Ribavirin and Ruta angustifolia should be considered in developing anti-hepatitis C virus agents. [ABSTRACT FROM AUTHOR]

Alzheimer's disease (AD) is a progressive neurodegenerative disorder that mainly occurs in elderly people. The increasing number of people suffering from AD causes health, social and economic problems. Therapeutic strategies implemented to slow down the progress of AD are by using cholinesterase inhibitors and antioxidants. The current study aimed to investigate the antioxidant and cholinesterase inhibitory properties of the leaves and stems of Cassia spectabilis as well as to determine the total phenolic contents in the samples. The leaves and stems of C. spectabilis were extracted with 96% ethanol by the maceration method. The cholinesterase inhibitory assay was performed by using the modified Ellman's method against two cholinesterase enzymes, namely acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The antioxidant properties of the samples were evaluated using 2,2-diphenyl-1-picryl hydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods. The total phenolic contents (TPC) were determined by a colorimetric assay using gallic acid as a reference. The results showed that the leaves and stems of C. spectabilis exerted significant inhibitory effects against both AChE and BChE enzymes with IC50 values of 24.3 and 9.8 µg/mL for the leaves and 58.6 and 47.8 µg/mL for the stems, respectively. The extracts showed moderate antioxidant activity in both DPPH and ABTS assays with IC50 ranging from 117 - 313 µg/mL. The presence of phenolic content in the samples may contribute to the antioxidant potency of the samples. The presence of non-phenolic compounds, such as alkaloids may be responsible for the cholinesterase inhibitory properties of the extracts. [ABSTRACT FROM AUTHOR]

Background: Hepatitis C Virus infection is a serious health problem that leads to chronic liver disease, liver cirrhosis, hepatocellular carcinoma, which causes high morbidity. Direct-Acting Antiviral Agents have been used as anti-hepatitis C Virus therapy. However, it was covered only in limited patients due to the high cost. Moreover, serious side effects and resistance cases were also reported in some HCV genotypes. Objective: This research aimed to find new anti-HCV from some Indonesia plants collected from Balikpapan Botanical Garden, East Borneo. Methods: Twenty-one leaf and stem barks extracts were successively extracted in n-hexane, dichloromethane, and methanol. Extracts were screened for their anti-HCV activity under in vitro culture cells in the concentration of 30 µg/mL. Plant extracts were inoculated in the Human Hepatocellular 7it and infected with HCV Japanese Fulminant Hepatitis strain 1a. Determination of 50% Inhibitory Concentration (IC50) value was further conducted at concentration of 100; 30; 10; 1; 0.1; 0.01 µg/ml of extracts. Results: In vitro anti-HCV activity revealed that among 21 plants extract, 11 extracts, namely, n-hexane extract from Luvunga scandens leaves, DCM extract from the leaf of L. scandens, Artocarpus sericicarpus, Artocarpus dadah, Eusideroxylon zwageri, Neolitsea cassiaefolia, methanol extract from A. sericicarpus and A. anisophyllus leaves, DCM extract from A. anisophyllus and A. elmeri stem bark, methanol extract from A. dadah stem bark, having potential inhibition with IC50 range 0.08 ± 0.05 to 12.01 ± 0.95 µg/mL. Conclusions: These results indicate that the eleven extracts could be good candidates as sources of anti-HCV agents. [ABSTRACT FROM AUTHOR]

The use of standard antimalarial drugs, such as dihydroartemisinin-piperaquine (DHP) for the treatment of malaria during pregnancy is limited due to the risk of teratogenicity. The alternative is therefore required although few exist. Here we show a phytopharmaceutical drug derived from Andrographis paniculata (AS201-01), which is effective as herbal antimalarial both in vitro and in vivo and may be a suitable alternative when used in complementary treatment with DHP. Plasmodium berghei infected pregnant BALB/c mice were divided into four groups: G1 (negative control), G2 (AS201-01), G3 (DHP), and G4 (combination of DHP and AS201-01). Pheripheral blood was collected during therapy for counting parasitemia. Placental samples were analyzed for the expression of IFN-γ, TNF- α, IL-10, placental parasite counts and foetal morphology. Groups G4 and G3 both showed a 100% inhibition of peripheral parasitemia. However, the treatment in G4 was found to be less effective than that in G2 and G3 in preventing placental parasitemia. The G4 treatment was able to reduce the expression of IFN-γ and IL-10, whereas TNF-α was not significantly different from the control group. Foetal morphologic abnormalities were observed in all groups except G2; G4 showed lower percentage of abnormalities compared to G3 and G1. A combination of A. paniculata tablet (AS201-01) with DHP has the potential to reduce the toxicity of DHP in malaria treatment. [ABSTRACT FROM AUTHOR]

The marine sponges with their unique and wide range of biodiversity, producing unusual metabolites emerge as a good candidate for new therapeutic agents, including as acetylcholinesterase (AChE) inhibitor. The aims of this study are to evaluate the potency of fractions and isolated compound from Agelas nakamurai as AChE inhibitor, as well as to determine the structure of the isolated compound. The bioassay-guided isolation protocol was carried out in this study. The AChE inhibitory assay was carried out based on the modified Ellman's method. The structure of the isolated compound was determined by NMR spectroscopy and mass spectrometry. A diterpene alkaloid was isolated from the active fraction of A. nakamurai. This compound exhibited a molecular ion at m/z 422.3280 [M]+ in mass spectrometry. The UV profile of the isolated compound showed a strong peak at 269 nm, and the specific rotation value is [α]20D +28,0 (MeOH, c 0.25). These data together with the ¹H and 13C NMR spectroscopy data are similar to that reported for iso-agelasine C. The isolated iso-agelasine C gave moderate inhibition against AChE enzyme with an IC50 value of 30.68 ± 0.92 μg/mL, which was lower compared to the extract and fractions. The stronger AChE inhibitory activity in the extract and fractions is possibly due to the synergistic activity of compounds present in the extract and fractions of A. nakamurai. Iso-agelasine C could serve as a lead for the development of diterpene alkaloid as an AChE inhibitor. [ABSTRACT FROM AUTHOR]

Objectives: The rapid spread of antimalarial drug resistance is becoming a problem in the treatment of malaria. The fact was indicated the importance of finding new antimalarial drugs. The genus Garcinia is well known to be a rich source of bioactive prenylated xanthones and triterpenes reported for their antimalarial activity. Garcinia parvifolia is one of the Garcinia genera that can be explored for the search of new antimalarial drugs. This study was aimed to determine the antimalarial activities of G. parvifolia extracts and fractions. Methods: Garcinia parvifolia Miq. stem was collected from Balikpapan Botanical Garden in East Kalimantan, Indonesia, was extracted gradually with n-hexane, dichloromethane, and methanol by ultrasonic assisted method. The most active extract was further separated using the open column chromatography method. All extracts and fractions were tested against Plasmodium falciparum 3D7 using lactate dehydrogenase (LDH) assay and followed by IC50 determination. Results: The results showed that all extracts inhibit P. falciparum growth by LDH assay. The highest inhibition was showed by dichloromethane stem extract (BP12-S-D) with the IC50 value of 6.61 ± 0.09 μg/mL. Further fractionation of BP12-S-D has obtained 10 fractions. All of them were identified by TLC, and a brownish-yellow spot (fraction-1) appears after spraying with 10% H2SO4. Fraction-1 (F1) performed the highest parasite growth inhibition with the IC50 value of 6.00 ± 0.03 μg/mL compared with other fractions. This fraction was classified as having a promising activity of antimalarial. The fraction-1 was identified using HPLC, and two major peaks were observed (A and B). The UV–Vis spectra showed the absorption at wavelengths 250 and 278 (A), 243, 281, and 317 nm (B). Based on the profile of TLC, HPLC, and UV–Vis spectra of F1, it was expected that the active compounds are flavonoid (A) and xanthone (B). Conclusions: The fraction-1 of dichloromethane extract of G. parvifolia Miq. stem has the highest antimalarial activity. It might be a potential candidate for the new antimalarial drug. [ABSTRACT FROM AUTHOR]

Phyllanthus niruri has been known as an immunomodulator and also reported to possess an antiviral activity against several RNA viruses, such as hepatitis B virus and hepatitis C virus by inhibiting viral entry and replication. Since the current situation of Coronavirus Disease 2019 (COVID-19) which infected among the world and caused severe disease and high morbidity, it urgently needed to find new agents against COVID-19. Therefore, in silico screening against COVID-19 receptors is carried out as an initial stage of drug discovery by evaluating the activity of phyllanthin and hypophyllanthin, an isolated from Phyllanthus niruri, in inhibiting spike glycoprotein (6LZG) and main protease (5R7Y) which play as target receptors of COVID-19. Molegro Virtual Docker 6.0 used to determine the best binding energy through the rerank score which shows the total energy bonds calculation. Phyllanthin and hypophyllanthin demonstrated to possess greater binding affinity toward the COVID-19 inhibition sites than their native ligand. The rerank score of phyllanthin and hypophyllanthin are lower than the native ligands 6LZG and 5R7Y. This result indicated that phyllanthin and hypophyllanthin have a stronger interaction than the native ligands both in spike glycoprotein (entry inhibitor) and main protease (translation and replication inhibitor). In conclusion, phyllanthin and hypophyllanthin are predicted to have strong activity against COVID-19 through inhibiting spike glycoprotein and main protease under in silico study. Further research is needed to support the development of P. niruri as inhibitor agents of COVID-19 through bioassay studies. [ABSTRACT FROM AUTHOR]

Human immunodeficiency virus (HIV) infection is considered as a major immunosuppressive disease linked to malignancies and other opportunistic infections. Recently, the high prevalence of HIV drug-resistant strains required a high demand for novel antiviral drug development, especially in herbal medicine approaches. The objective of this study was to evaluate the possibility of Ficus fistulosa leaves can inhibit HIV replication in ethanol extract form as well as its fractions using chloroform, ethyl acetate, and butanol solvents. F. fistulosa leaves were extracted using ethanol as a solvent and further gradually fractionated in chloroform, ethyl acetate, and butanol solvents. The targeted persistently infected virus (MT4/HIV) cell lines were cocultured with ethanol extract and fractions at different time points. The syncytium formation and cytotoxicity assays were performed to evaluate the potential antiviral activity of F. fistulosa leaves. One of the four tested extract/fractions showed antiviral activity against HIV. The ethanol extract showed weak inhibition with a high level of toxicity (IC50 = 8.96 μg/mL, CC50 ≥50 μg/mL, and SI = 5.58). Meanwhile, chloroform fraction effectively inhibited the MT4/HIV cell proliferation while keeping the toxicity to a minimal level (IC50 = 3.27 μg/mL, CC50 = 29.30 μg/mL, and SI = 8.96). In contrast of ethyl acetate fraction and butanol fraction showed no anti HIV activity with a high level of toxicity (CC50 ≥50 μg/mL) and low SI value (>2.17 μg/mL and >0.97 μg/mL). Chloroform fraction of F. fistulosa leaves showed effectively as anti-viral activity against MT4/HIV cells. [ABSTRACT FROM AUTHOR]

Alzheimer's disease (AD) is a degenerative brain disease characterized by confusion, behavior changes, decline in memory and cognitive skills. One of the strategies in the treatment of AD is to use acetylcholinesterase (AChE) inhibitors. The current study aims to determine the AChE inhibitory activities of the extract and fractions of the root of Rauvolfia serpentina. Extraction was carried out by maceration method using ethanol, followed by liquid–liquid partition using n-hexane, ethyl acetate and n-butanol. Further fractionation was conducted by using vacuum liquid chromatography (VLC). The AChE inhibitory assays were performed by using Ellmann's method. Phytochemical screening was carried out by TLC method. The ethanolic extract of R. serpentina showed inhibition against AChE enzyme with an IC50 value of 7.46 μg/mL. The extract and fractions showed higher inhibition against butyrylcholinesterase (BChE) compared to AChE. Amongst three fractions obtained, the n-butanol fraction showed the strongest inhibition with an IC50 value of 5.99 μg/mL against AChE. VLC fractionation of the n-butanol fraction yielded 13 subfractions (VLC 1–VLC 13). Four out of 13 subfractions gave more than 80% inhibition against AChE, namely subfractions 4–7, with IC50 values ranging from 4.87 to 47.22 μg/mL. The phytochemical screening of these subfractions suggested the presence of alkaloids. The ethanolic extract, as well as fractions of R. serpentina root, are potential for AChE inhibitor. The alkaloid compound may be responsible for this activity. [ABSTRACT FROM AUTHOR]

The antimalarial drug resistance is an obstacle in the effort to overcome malaria. The new alternative antimalarial drug became in great attention of urgent need. Current antimalarial drugs were derived from plants. Therefore, the plant is considering a potential source of new drugs. Cratoxylum sumatranum belongs to the Hypericaceae family contain xanthones and phenolic compounds, which was reported for their antimalarial activities. This study aims to determine the antimalarial activities of C. sumatranum extracts and fractions. Cratoxylum sumatranum stem bark (BP14-SB) collected from Balikpapan Botanical Garden in East Kalimantan, Indonesia, was extracted gradually with n-hexane, dichloromethane, and methanol by ultrasonic-assisted extraction method. All extracts were tested against Plasmodium falciparum 3D7 by lactate dehydrogenase (LDH) assay and followed by IC50 determination. The most active extract was further separated and tested for their antimalarial activities. The results showed that dichloromethane stem bark extract (BP14-SB-D) had the strongest inhibition of parasite growth with the IC50 value of 0.44 ± 0.05 μg/mL and moderately toxic with the CC50 value of 29.09 ± 0.05 μg/mL. Further fractionation of BP14-SB-D by open column chromatography using silica gel and gradient hexane–ethyl acetate obtained 12 fractions. LDH assay for these 12 fractions of BP14-SB-D showed that Fraction-6 (IC50 value of 0.19 ± 0.03 μg/mL) was performed the strongest inhibition of parasite growth, compared to other fractions. TLC identification showed that BP14-SB-D contains xanthone. The dichloromethane extract of C. sumatranum stem bark (BP14-SB-D) and Fraction-6 from this extract exhibited antimalarial activity and the potential to be developed an antimalarial substance. [ABSTRACT FROM AUTHOR]

Background: Medicinal plants are potential sources for drug candidates. It possesses with various metabolites which have many pharmacology effects. Ruta angustifolia is one of medicinal plants that has been used traditionally for liver disease. Previous study it has been demonstrated to inhibit hepatitis C virus under in vitro cell culture. It decreased protein NS3 level and gave synergistic effect in combination with simeprevir and telaprevir. This plant provides a prospective candidate to develop as anti-HCV Objective: This study evaluates the phytochemistry screening for qualitative assay and determine the concentration of rutin as marker compound for developing R. angustifolia extract as anti-HCV agent. Materials and Methods: R. angustifolia leaves were extracted with 70% of ethanol. Extract and rutin were analysis their anti-HCV activity by in vitro culture cells of Huh7it. The concentration of rutin was determine by TLC densitometry. Results: The 70% ethanol extract of R. angustifolia dan rutin exhibit anti-HCV activities with IC50 value of 2.9 ± 0.8 µg/ml and 28.1 ± 5.6 µg/ml, respectively. Screening phytochemistry demonstrated to contain flavonoid, terpenoid, alkaloid and polyphenols. TLC densitometry analysis yield the concentration of rutin in extract 0.06 %. Conclusion: Extract of 70% ethanol of R. angustifolia has a potential anti-HCV activity. Extract of R. angustifolia may provide a good candidate for developing anti-HCV agents. [ABSTRACT FROM AUTHOR]