ANTIMALARIAL ACTIVITY AND CYTOTOXICITY STUDY OF ETHANOL EXTRACT AND FRACTION FROM ALECTRYON SERRATUS LEAVES

Objective: The resistance of Plasmodium falciparum to standard antimalarial drugs has led the scientist to investigate medicinal plants as new potentials in the treatment or prevention of malaria. Previous study showed that the ethanol extract from Alectryon serratus leaves inhibited P. falciparum in vitro. The purpose of this study was to determine the in vitro and in vivo antimalarial activity and toxicity of ethanol extract and fractions of A. serratus leaves.Methods: Ethanol extract of A. serratus leaves was partitioned with dichloromethane, ethyl acetate and n-butanol successively. Antimalarial activities were determined in vitro against P. falciparum 3D7 based on HRP2 measurement in a simple enzyme-linked immunosorbent assay (ELISA) and in vivo against Plasmodium berghei ANKA based on the 4-days suppressive test by Peters. The toxicity study was determined by MTT assay using Huh7it cells.Results: Ethanol extract and fractions of A. serratus exhibited antimalarial activity and was proved to be nontoxic. Ethyl acetate (EA) and butanol (BuOH) fractions performed a higher antimalarial activity (IC50<10 µg/ml) and lower toxicity (SI>10) compared with ethanol extract and dichloromethane (DCM) fraction. EA fraction had IC50value of 9.45 µg/ml and SI of 10.58, while BuOH fraction had IC50value of 7.69 µg/ml and SI of 130.04. In vivo antimalarial activity was conducted for ethanol extract and EA fraction. The result showed that EA fraction and ethanol extract had ED50 5.92 mg/kg BW and 13.82 mg/kg BW, respectively.Conclusion: Ethanol extract and EA fraction of A. serratus leaves showed in vivo and in vitro antimalarial activities and proved to be nontoxic. Both of them are a good candidate of new source in the development of new antimalarial drugs.Â

The Development of tablet formulation of Artocarpus champeden Stembark extract as antimalarial drug

Parasite resistance to antimalarial drug, chloroquine and sulfadoxin-pirimetamin, still e major problem in malaria control worldwide, thereforc, the cffort in developing a new targct of antimalarial drug become a high priority. Our preliminary test revealed that fuom A. chanpeden exhibiedt potent antimalarial activities againts P. lalciparum in vitro brghci in vivo. Several isolaEd compounds from this plant exhibited antimalarial activity drc isotated compound identified as hetcroflavon C, a prenylated flavooe, have a higher activity than chloroquine. Therefore, it is potential to be developed as antimalarial rcscarch was conducted to develop tablet formulation of ethanol extract of A. stcmbark (EEAC). The formula that composed: EEAC 150 mg, lactose 140 mg, cabarnilum 46 mg, avicel PH l0l 79o, primogcl 57o, and Mg stcarat 1% was the selected Th€ tablet hardness o[ the formula has span betwccn 9.0-12.27 kP and the averagc is , thc disintegration time of formula 12 minutcs 4? seconds. A standard fiays test oll P. infected mice was used to evaluated in vrv, antimalarial activity of the tablet. This rlvcalcd that EEAC tablet has antimalarial activity against parasite P. berghei in vivo. ration ofEEAC tablet at a dose of 10 mg/kg body weight multiple dose (twice a day) thc parasite growth better than 100 mg/kg body weight single dose (once a day) activity of tablet in multiple dose pcr oral shqwed inhibition of parasite growth of while at single dose per oral showed inhibition of parasite growth of 83.32

Screening of anti-HIV activities in ethanol extract and fractions from Ficus fistulosa leaves

Objectives: 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. Methods: 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. Results: 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). Conclusions: Chloroform fraction of F. fistulosa leaves showed effectively as anti-viral activity againstMT4/HIV cells

In vivo antimalarial activity of Andrographis paniculata Tablets

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

Free-Radical Scavenging Activity Screening of Some Indonesian Plants

Objective: Indonesia is well known for its biodiversities and very rich of plants species which only a small portion of the species have been investigated in detail. This study aimed to investigate free radical scavenging activity of some Indonesian plants. Methods: Ethanol extract of leaves and stems of plants were tested for their free radical scavenging activity using 2,2-Diphenyl-1-picrylhydrazyl (DPPH) by TLC-autography and spectrophotometry method. Results: The TLC-autography result showed that all samples have free-radical scavenging activities. Spectrophotometry analysis results showed that the lowest IC50 value was ethanol extract of Alectryon serratus stem with IC50 value of 2.04 ppm, lower than vitamin C with IC50 value of 3.11ppm. The highest IC50 value was ethanol extract of Ochrosia akkeringae leaves with IC50 value of 214.64 ppm. Conclusion: Ethanol extract of Alectryon serratus stem may be potential to be developed as a medicinal drug

Effect of Andrographis paniculata tablet (AS201-01) on Transforming Growth Factor Beta (TGF-β) expression and parasite inhibition in mice placenta infected with Plasmodium berghei

Background: Transforming Growth Factor β (TGF-β) is a cytokine regulator of inflammation that important in inhibited parasite growth and preventing inflammation. Andrographis paniculata was empirically used as traditional medicine in Indonesia to cure malaria by activating TGF-β. Preliminary studies showed that AS201-01 tablets containing the ethyl acetate fraction of A. paniculata had been shown to inhibit the growth of Plasmodium berghei.Aims: This study aims to determine the effect of the AS201-01 tablet on parasite inhibition and TGF-β expression in P.berghei infected mice placenta.Methods: About 24 pregnant mice were divided into 4 groups: healthy pregnant mice (normal) (G1), untreated infected pregnant mice (negative control) (G2), infected pregnant mice treated by AS201-01 tablets (G3), and infected pregnant mice treated with Dihydroartemisinine-piperaquine (positive control) (G4). About 1x106 parasitemia were infected on the 9th day of pregnancy, while therapy was administered on the 11th day of pregnancy. The placenta was collected at the 15th day of pregnancy. The parasite inhibition and TGF-β expression were evaluated using Hematoxylin-Eosin (HE)  and immunohistochemistry assay.Results: The results showed that the parasite still found in the placenta of G2, G3, and G4 still, but parasite of placental in G2 was higher than G3 and G4. There was a significant difference in the parasite inhibition between G2 with G3 and G4 (p&lt;0.05). In addition, the immunohistochemistry assay found that there was a significant difference in TGF-β expression between G2 with G3, G4, and G1 (p&lt;0.05).Conclusion: Administration of the AS201-01 tablets inhibit parasite P. berghei and increase TGF-β expression on the placenta of infected mice.</p

Treated Plasmodium berghei infected pregnant mice by Andrographis paniculata tablet (AS201-01) decreasing the TLR-4 expression and apoptosis index of placental tissue

Objective: This study aimed to evaluate the effect of Andrographis paniculata tablet (AS201-01) in decreasing expression of Toll-Like Receptor-4 (TLR-4) and apoptosis index of placental tissue of Plasmodium berghei infected pregnant mice. Material and Methods: A total of 24 pregnant mice were divided into 4 groups, G1 was uninfected pregnant mice group, G2 was untreated Plasmodium berghei infected pregnant mice, G3 was P. berghei infected pregnant mice treated with AS201-01 tablet and G4 was P. berghei infected pregnant mice treated with dihydropiperaquine-phosphate (DHP) tablets. All mice were sacrifice at day 15th of pregnancy and the placenta was collected. The TLR-4 expression and apoptosis index were evaluated using immunohistochemistry assay. Results: The TLR-4 expression and apoptosis index on G3 was lower than G2 and showed a statistically significant difference (P = 0.00). The TLR-4 expression and apoptosis index of placental tissue in P. berghei infected pregnant mice which treated with AS201-01 tablet were decreased compared to untreated group and DHP tablet treated group as well. Conclusion: AS201-01 tablet containing ethyl acetate fraction of A. paniculata could decrease TLR-4 expression and apoptosis index of placental tissue in P. berghei infected pregnant mice

Free Radical Scavenging and Analgesic Activities of 70% Ethanol Extract of Luvunga sarmentosa (BI.) Kurz from Central Kalimantan

Luvunga sarmentosa, commonly known as saluang belum, is widely used in Kalimantan to relieve pains, rheumatism, boost the immune system, and fever. The research on the free radical scavenging and analgesic effect of the L. sarmentosa stem extract has not been reported. This study aimed to evaluate the free radical scavenging and analgesic activity of the ethanol extract of L. sarmentosa. The L. sarmentosa stem was extracted using 70% ethanol and tested for free radical scavenging using the 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and analgesic activity, acetic acid-induced writhing test, and hot plate test in an animal model. The results showed that the 70% ethanol extract of the L. sarmentosa had an anti-free radical scavenging and analgesic activity. The extract has weak free radical scavenging with an IC50 value of 293.45 µg/mL. Analgesic activity using the writhing test indicated that the extract significantly reduced the writhes count after oral administration in a dose-dependent manner compared to the negative control. Extract at a dose of 550 mg/kg BW can reduce the writhing test by 67.60% compared to others. In contrast, the diclofenac sodium reduced the number of writhes by 74.74%. While in a hot plate, the extract at a dose of 550 mg/kg BW produced a maximum possible analgesia (MPA) of 17.64%, lower than the MPA of diclofenac sodium (51.01%). Analgesic activity of the extract has higher inhibition on the writhing test than on the hot plate. The extract could be responsible for the peripheral mechanism by inhibiting the prostaglandin biosynthesis

In vivo antimalarial activity of Andrographis paniculata Tablets

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

In Vivo Antimalarial Activity of Ethanol Extract and Ethyl Acetate Fraction of Alectryon serratus Leaves on Plasmodium berghei Infected Mice

Malaria was a major global public health concern due to the development of resistance by the most lethal causative species, Plasmodium falciparum. Natural products were potential sources of new antimalarial drugs (Bero, 2011; Nogueira, 2011). In vitro antimalarial activity screening of several Indonesian plants using HRP2 method showed that ethanol extract and ethyl acetate (EA) fraction of Alectryon serratus were active as an antimalarial (Widyawaruyanti, 2014). The aim of this study is to identify Thin Layer Chromatography (TLC) profile and investigate in vivo antimalarial activity of extract and fraction of Alectryon serratus leaves