The formulation of three phytopharmaceutical products of Andrographispaniculata fractions (AP fraction A and B) containing diterpene lactones as an active substance were developed and their antimalarial activities against Plasmodium bergheihas been examined. In vivo antimalarial assay on P. berghei infected mice was carried out by oral administration,twice a dayfor four consecutive days of the AP fractions product, which were Tablet I : wet granulated formula of AP fraction A; Tablet II : wet granulated formula of AP fraction B; Tablet III : solid dispersion formula of AP fraction B.. The results revealed that three phytopharmaceutical products of A.paniculata were inhibited parasite's growth with inhibition range of 70.15% to 80.35%. There was no significant difference of antimalarial activities between Tablet II and III, meanwhile there was significant difference among Tablet I with Tablet II and Tablet III.It was concluded that antimalarial activity depending on raw material form of A. paniculata active substance.

Background New agents for developing alternative or complementary medicine to treat the hepatitis C virus (HCV) are still needed due to high rates of HCV infection globally and the current limitations of available treatments. Treatment of HCV with a combination of direct acting antivirals have been shown to be approximately 90% effective but will be limited in the future due to the emergence of drug resistance and high cost. The leaves of Melicope latifolia have previously been reported to have anti-HCV activity and are a potential source of bioactive compounds for future novel drug development. This study aimed to evaluate the efficacy of the extract of M. latifolia fruit to treat HCV and to isolate its active compounds. Method M. latifolia fruit was extracted using methanol and purified using vacuum liquid chromatography (VLC) and Radial Chromatography. The anti-HCV activity was analyzed using cell culture lines Huh7it-1 and JFH1 (genotype 2a). Time-of-addition and immunoblotting studies were performed to identify the mode of action of the isolated active compounds. The structures of the active compounds were determined using nuclear magnetic resonance (NMR) spectra, UV, IR, and Mass Spectra. Results Six known compounds were isolated from M. latifolia fruit: O-methyloktadrenolon, alloevodionol, isopimpinellin, alloxanthoxyletin, methylevodionol, and N-methylflindersine. N-methylflidersine was the most active compound with IC50 value of 3.8 μg/ml while methylevodionol, isopimpinellin, and alloevodionol were less active. O-methyloktadrenolon and alloxanthoxyletin were moderately active with IC50 values of 10.9 and 21.72 μg/ml, respectively. N-methylflidersine decreased level of HCV NS3 protein expression in the cells. Conclusion The alkaloid compound, N-methylflindersine which was isolated from M. latifolia possesses anti-HCV activity through post-entry inhibition and suppressed NS3 protein expression.

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Background Current therapy of chronic hepatitis C virus (HCV) with direct-acting antivirals (DAAs) has dramatically improved the sustained virologic response (SVR) of affected patients; however, treatment with DAAs remains expensive, and drug-resistant HCV variants remain a threat. As a result, there is still a need to continue to develop affordable and effective drugs for the treatment of HCV. Previously, we have demonstrated that a crude extract from Artocarpus heterophyllus leaves is a potential anti-HCV candidate. In this study, we have further purified this crude extract, examined which sub-fraction possesses the highest antiviral activity, and then explored its efficacy at different HCV life cycle stages. We also assessed synergistic antiviral effects between the A. heterophyllus extract and commercially available anti-HCV drugs. Methods We used vacuum liquid chromatography (VLC) and high-performance liquid chromatography (HPLC) to fractionate a dichloromethane extract of A. heterophyllus leaves. We then examined the anti-HCV activity of the fractions using HCV genotype 2a, JFH1a; the antiviral mode of action was determined by exploring adding the treatments at different times. We examined the antiviral effects on the viral entry stage through a virucidal activity test, viral adsorption examination, and pretreatment of cells with the drug. The effects on the post-viral entry stage were determined by the levels of HCV protein expression and HCV RNA expression in infected cells. Results Through activity guided purification, we identified the sub-fraction FR3T3 as possessing the most robust anti-HCV activity with an IC50 value of 4.7 ± 1.0 μg/mL. Mode-of-action analysis revealed that FR3T3 inhibited post-viral entry stages such as HCV NS3 protein expression and HCV RNA replication with marginal effects on the viral entry stage. Thin-layer Chromatography (TLC) indicated that FR3T3 contained terpenoids and chlorophyll-related compounds. We also found a synergistic antiviral activity when the DCM extract of A. heterohyllus was used in combination therapy with commercial anti-HCV drugs; Ribavirin, Simeprevir, Cyclosporin A. Conclusions The extract of A. heterophyllus and its sub-fraction, FR3T3, presented here have anti-HCV activities and could be candidate drugs for add-on-therapy for treatment of chronic HCV infections.

Objectives. To determine the analgesic and antipyretic activities of a tablet derived from Andrographis paniculata ethyl acetate fraction (AS201-01) in animal models. Methods. The tablet derived from AS201-01 contains an equivalent of 35 mg andrographolide per tablet. Analgesic activity was determined using an acetic acid-induced writhing test on adult male mice. A writhe was recorded by a stopwatch and was defined as the stretching of the abdomen and/or stretching of at least one hind limb. For the determination of antipyretic activity, pyrexia was induced by subcutaneous injection of 15% w/v Brewer’s yeast into adult male rats. Rectal temperature was monitored at 1, 2, 3, and 4 hours after treatment. Results. The results showed that the AS201-01 tablet had analgesic and antipyretic activity. In the acetic acid-induced writhing model, AS201-01 tablet exhibited significant analgesic effect with a 66.73% reduction in writhing response at a dose of 50 mg andrographolide/kg body weight compared to the negative control group. The tablet also showed a significant antipyretic effect. The maximum antipyretic effect was observed after the third hour of administration of the AS201-01 tablet at a dose of 100 mg andrographolide/kg body weight. Conclusion. Tablet of Andrographis paniculata ethyl acetate fraction (AS201-01) exhibited analgesic and antipyretic activities.

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the treatment need to be considered as important problems. 4,5 In order to circumvent those problems, the development of new antiviral drugs is very much required. Some plants have been reported to have hepatitis C antiviral activity. Plant extracts from Toona sureni, 6 Artocarpus heterophyllus, 7 Ficus fistulosa, 8 Alectron serratus, 9 and Melicope latifolia 4 significantly inhibited HCV activity in vitro. A variety of active phytochemicals such as flavonoids, terpenoids, lignins, sulphides, polyphenolics, coumarins, saponins, furyl, alkaloids, polylines, thiophenes, protein, and peptides have been identified to inhibit various viruses. 10 Melicope latifolia belongs to the Rutaceae family, commonly known in Indonesia as Ki Sampang and is traditionally used to cure fever and abdominal cramps. The tree typically has a height of about 20 m and is commonly found in primary and secondary open forests. M. latifolia plants are distributed in Malaysia, Philippines, Java-Indonesia, Kalimantan-Indonesia and Papua New Guinea. 11 The chemical compounds which were contained in the M. latifolia plant, are flavonoids, alkaloid, coumarins and terpenoids. 10,12 In general, plant species in the Rutaceae family contain the chemical constituent of alkaloid group, including the Melicope genus.