Antimalarial Activity of Andrographis Paniculata Ness‘s N-hexane Extract and Its Major Compounds (original) (raw)
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Pharmaceutical …, 1992
Andrographis paniculata Ness is one of the plants that is under explored and could contain potentially active substances to serve as an antimalarial. Structure investigation of major compounds that have responsibility for the antimalarial activity of Andrographis paniculata Ness's n-hexane extract is very important so that it is known whether the antimalarial activity is synergistic or from the major compounds. Menthol and dioctyladipate as major component from n-hexane extract of Andrographis paniculata Ness have been succesfully isolated using simple and inexpensive methods. The solvent system used are n-hexane : ethyl acetate (10:1) and n-hexane: chloroform (10:3) consecutively either for column or preparative thin layer chromatography. FT-IR, 1 H-NMR and GC-MS were used to determine the structure of compounds. The activity of n-hexane extract, menthol and dioctyladipate related to the inhibition of heme polymerization have been done comprehensively. The inhibition of heme polymerization activity of isolate compounds and n-hexane extract are classified to a good level (dioctyl adipate IC 50 = 1.15 ± 0.41 mg/mL, menthol IC 50 = 0.31 ± 0,01 mg/mL, and n-hexane extract IC 50 = 0.07 ± 0.03 mg/mL) and potentially as antimalarial. From the IC 50 , the antimalarial activity of Andrographis paniculata Ness's n-hexane extract is working synergistically, not by the major compounds.
In vivo Antimalarial Activity of Andrographis Paniculata Tablets
Procedia Chemistry, 2014
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.
Since the emergence of drug resistant strains of malaria parasites, the rate of resistance has been increasing and limiting adequate treatment of malaria. Consequently, there is an urgent global need to isolate new classes of antimalarial compounds from natural sources. The aim of this study was to test Andrographis paniculata extract for the ability to treat malaria. The Andrographis paniculata powder from commercial capsule was freshly dissolved in DMSO and diluted with normal saline. The four-day suppressive, curative effects against established infection and prophylactic models of the extract were carried out in P. berghei ANKA infected ICR mice, using pyrimethamine as a positive control. Parasitemia was then monitored at day 4 after treatment with the extracts (suppressive and curative tests) or after infection (prophylactic test), and percent inhibition was subsequently calculated and compared with pyrimethamine treated group. It was found that the extract (2, 20, and 100 mg.k...
Research Journal of Pharmaceutical, Biological and Chemical Sciences , 2017
The rapid spread of resistance encourages the search for new active compounds. Andrographis paniculata commonly known as sambiloto was empirically used as traditional medicine in Indonesia to cure malaria. This study aims to determine antimalarial activity and survival time of A. paniculata fraction from 70% ethanolic extract (namely AS202-01) on Plasmodium berghei infected mice. Antimalarial in vivo study was conducted based on Peter's 4-days suppressive test. Thirty healthy Balb/c male mice, divided into 6 groups (n = 5), were infected intravenously with 1x10 6 parasitized erythrocytes of P. berghei. Infected mice were treated at a dose of 6.25, 12.5, 25 and 50 mg/kg BW, twice a day for four days, the untreated group of mice received CMC-Na 0.5% and the control group treated with chloroquine (10 mg/kg BW). Thin blood smears giemsa staining were made every day for seven days and observed under microscope to count parasitemia and calculate inhibition of parasite's growth. Probit analysis was conducted to determine effective dose (ED50) value. Observation of antimalarial effect of AS202-01 was continued until 14 days to evaluate survival time of infected mice. The results showed that AS202-01 was inhibited P. berghei growth with ED50 value of 6.75 mg/kg BW. It was classified as a highly active antimalarial substance. The AS202-01 was also significantly able to increase survival time of infected mice compared to untreated group.
Journal of Pharmacy & Pharmacognosy Research, 2023
Context: Andrographis paniculata has been used as a traditional medicine to treat malaria. The ethyl acetate fraction of A. paniculata containing diterpene lactone compounds was developed into a tablet dosage form, AS201-01. Aims: To determine the antimalarial activity and toxicity of AS201-01 to guarantee its efficacy and safety. Methods: Antimalarial assay in male Balb/c mice based on Peter’s four-day suppressive test at a dose of 6.25, 12.5, 25, and 50 mg/kg BW and 10 mg/kg BW of chloroquine as a positive control. In acute toxicity, AS201-01 was administered orally at a dose of 5, 50, 200, and 2,000 mg/kg BW in male rats (Wistar rats) and observed for 14 days to identify signs of toxicity and mortality. Meanwhile, AS201-01 was administered at 50, 327, and 1,000 mg/kg BW per day for 28 days in male and female rats to assess subchronic toxicity. Results: AS201-01 has antimalarial activity and exhibited the highest suppressive effect at 50 mg/kg BW dose with inhibition of 73.48%. Meanwhile, chloroquine at 10 mg/kg BW has an inhibition of 97.94%. AS201-01 was highly active as an antimalarial with an ED50 value of 5.95 mg/kg BW and increased survival time. Administration of AS201-01 is relatively safe in acute and subchronic toxicity studies. No clinical signs and mortality were observed in either study. The 50% lethal dose (LD50) was above 2,000 mg/kg BW. Conclusions: AS201-01 is effective as an antimalarial and non-toxic when administered orally at an equivalent therapeutic dose in an animal model.
Asian Pacific Journal of Health Sciences
Antimalarial effect of some medicinal plants found in Uttarakhand (India) is least explored by the scientific community locally. Advent of resistance to various antimalarial drugs by plasmodium made malaria more fatal and life-threatening disease. Therefore, present need is to invest more effort and interest in research for antimalarials from medicinal plants. Plasmodium yoelii nigeriensis (PYn) is multi drug resistance malaria parasite known for resistance to chloroquine (CQ), quinine, quinidine, amodiaquine, halofantrine, mepacrine, and mefloquine. The P. yoelii produces 100% infections in animals. Researchers in this study tried to understand the behavior of CQ -resistant plasmodium PYn with CQ, whole plant extracts of Andrographis paniculata (AP) with possibility of their resistance reversal. Wherever, 3–4 times CQ doses are not able to produce sufficient antimalarial effect in resistant PYn. Most of the pure plant extracts are also not able to produce minimal therapeutic respon...
Diterpenoids as potential anti-malarial compounds from Andrographis paniculata
Beni-Suef University Journal of Basic and Applied Sciences
Background The objectives of the current study are to evaluate the traditionally used medicinal plants Andrographis paniculata for in vitro anti-malarial activity against human malarial parasite Plasmodium falciparum and to further characterize the anti-malarial active extract of A. paniculata using spectroscopic and chromatographic methods. Results The chloroform extract of A. paniculata displayed anti-malarial activity with IC50 values 6.36 μg/ml against 3D7 strain and 5.24 μg/ml against K1 strains respectively with no evidence of significant cytotoxicity against mammalian cell line (CC50 > 100 μg/ml). LC-MS analysis of the extract led to the identification of 59 compounds based on their chromatographic and mass spectrometric features (a total of 35 compounds are present in positive ion and 24 compounds in negative ion mode). We have identified 5 flavonoids and 30 compounds as diterpenoids in positive ion mode, while in the negative mode all identified compounds were diterpenoi...
Journal of Tropical Medicine, 2011
Andrographolide (AND), the diterpene lactone compound, was purified by HPLC from the methanolic fraction of the plant Andrographis paniculata. The compound was found to have potent antiplasmodial activity when tested in isolation and in combination with curcumin and artesunate against the erythrocytic stages of Plasmodium falciparum in vitro and Plasmodium berghei ANKA in vivo. IC 50 s for artesunate (AS), andrographolide (AND), and curcumin (CUR) were found to be 0.05, 9.1 and 17.4 μM, respectively. The compound (AND) was found synergistic with curcumin (CUR) and addictively interactive with artesunate (AS). In vivo, andrographolide-curcumin exhibited better antimalarial activity, not only by reducing parasitemia (29%), compared to the control (81%), but also by extending the life span by 2-3 folds. Being nontoxic to the in vivo system this agent can be used as template molecule for designing new derivatives with improved antimalarial properties.
2021
© 2021 Funmilayo I.D. Afolayan and Oluwasekemi D. Ijidakinro. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. Abstract Resistance to parasitic medicines is a recurring problem, hence the need to discover and develop new effective drugs. Phytochemicals derived from plants play an essential role in drug discovery. Andrographis paniculata is used widely as a medicinal herb for the treatment of various ailments. In this study, Gas Chromatography-Mass Spectrophotometry (GCMS) analysis was carried out on A. paniculata. The compounds obtained from the GCMS analysis were docked against validated drug targets from Schistosoma mansoni (Dihydrofolate reductase and cathepsin B1), Leishmania major (N-myris...