scholarly journals In VitroandIn VivoAntimalarial Activity ofFicus thonningiiBlume (Moraceae) andLophira alataBanks (Ochnaceae), Identified from the Ethnomedicine of the Nigerian Middle Belt

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
M. O. Falade ◽  
D. O. Akinboye ◽  
G. O. Gbotosho ◽  
E. O. Ajaiyeoba ◽  
T. C. Happi ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Human Cell Line ◽  
New Drugs ◽  
Leaf Extracts ◽  
Potential Source ◽  
Hexane Extracts ◽  
Ficus Thonningii ◽  
Multiresistant Strains

Drug resistance inPlasmodium falciparumrequires that new drugs must be developed. Plants are a potential source for drug discovery and development. Two plants that used to treat febrile illnesses in Nigeria were tested forin vitroandin vivoantimalarial activity and cytotoxicity in cancer cell lines. Methanol, hexane, and ethyl acetate leaf extracts ofFicus thonningiiandLophira alatawere active inin vitroassays againstP. falciparumNF54 (sensitive) and K1 (multiresistant) strains. Hexane extracts ofF. thonningiiandL. alatawere the most effective extracts inin vitroassays with IC50of2.7±1.6 μg/mL and2.5±0.3 μg/mL for NF54 and10.4±1.6 μg/mL and2.5±2.1 μg/mL for K1 strain. All extracts were nontoxic in cytotoxicity assays against KB human cell line with IC50of over 20 μg/mL, demonstrating selectivity againstP. falciparum.In vivoanalysis shows that hexane extracts of both plants reduced parasitaemia. At the maximum dose tested,L. alatahad a 74.4% reduction of parasitaemia whileF. thonningiihad a reduction of 84.5%, both extracts prolonged animal survival in mice infected withP. bergheiNK65 when compared with vehicle treated controls. The antiplasmodial activity observed justifies the use of both plants in treating febrile conditions.

scholarly journals In VivoAntimalarial Activity of the 80%Methanolic Root Bark Extract and Solvent Fractions ofGardenia ternifoliaSchumach. & Thonn. (Rubiaceae) againstPlasmodium berghei

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Dejen Nureye ◽  
Solomon Assefa ◽  
Teshome Nedi ◽  
Ephrem Engidawork
Keyword(s):  
Crude Extract ◽  
Antimalarial Activity ◽  
Standard Procedure ◽  
New Drugs ◽  
Bark Extract ◽  
Root Bark ◽  
Antimalarial Agents ◽  
Loss Of Weight

Background. Evolution of antimalarial drug resistance makes the development of new drugs a necessity. Important source in search of such drugs is medicinal plants.Gardenia ternifoliaplant is used in Ethiopian traditional medicine for the treatment of malaria and is endowed within vitroantimalarial activity. Herein, thein vivoantimalarial activity of the plant was investigated.Methods. Acute toxicity was carried out using a standard procedure. A 4-day suppressive test was employed to evaluate the antimalarial effect of methanolic crude extract and solvent fractions of the plant. The curative and prophylactic effect of crude extract was further tested by Ranes’s test and residual infection procedure, respectively, usingPlasmodium berghei(ANKA strain) in Swiss albino mice.Results. The chemosuppressive effect exerted by the crude extract and fractions ranged between 30-59% and 14-51%, respectively. Curative and prophylactic effects of the crude extract were in the range of 36-63% and 24-37%, respectively. All dose levels of the crude extract prevented loss of weight, reduction in temperature, and anemia on early and established infection. Butanol and chloroform fractions also did reverse reduction in temperature, body weight, and packed cell volume.Conclusions. The results indicated that the plant has a promising antiplasmodial activity and it could be considered as a potential source to develop new antimalarial agents.

scholarly journals Antimalarial activity of traditional Kampo medicine Coptis Rhizome extract and its major active compounds

2020 ◽  
Author(s):  
Awet Alem Teklemichael ◽  
Shusaku Mizukami ◽  
Kazufumi Toume ◽  
Farhana Mosaddeque ◽  
Mohamed Gomaa Kamel ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Active Compound ◽  
Antimalarial Activity ◽  
New Drugs ◽  
Herbal Extract ◽  
Herbal Extracts ◽  
Vitro Assay ◽  
Malaria Model

Abstract Background: The herbal medicine has been a rich source of new drugs exemplified by quinine and artemisinin. In this study, examined a variety of Japanese traditional herbal medicine (Kampo) for their potential antimalarial activities. Methods: We designed a comprehensive screening to identify novel antimalarial drugs from a library of Kampo herbal extracts (n = 120) and related compounds (n=96). The antimalarial activity was initially evaluated in vitro against chloroquine/mefloquine-sensitive (3D7) and -resistant (Dd2) strains of Plasmodium falciparum . The cytotoxicity was also evaluated using primary Adult Mouse Brain cells. After being selected through the first in vitro assay, positive extracts and compounds were examined for possible in vivo antimalarial activity. Results: Out of 120 herbal extracts, Coptis Rhizome showed the highest antimalarial activity (IC 50 1.9 µg/mL of 3D7 and 4.85 µg/mL of Dd2) with a high selectivity index (SI) > 263 (3D7) and > 103 (Dd2). Three major chlorinated compounds (coptisine, berberine, and palmatine) related to Coptis Rhizome also showed antimalarial activities with IC 50 1.1, 2.6, and 6.0 µM (against 3D7) and 3.1, 6.3, and 11.8 µM (against Dd2), respectively. Among them, coptisine chloride exhibited the highest antimalarial activity (IC 50 1.1 µM against 3D7 and 3.1 µM against Dd2) with SI of 37.8 and 13.2, respectively. . Finally, the herbal extract of Coptis Rhizome and its major active compound coptisine chloride exhibited significant antimalarial activity in mice infected with P. yoelii 17X strain with respect to its activity on parasite suppression consistently from day 3 to day 7 post-challenge. The effect ranged from 50.38 to 72.13% (P <.05) for Coptis Rhizome and from 81 to 89% (P <.01) for coptisine chloride. Conclusion: Coptis Rhizome and its major active compound coptisine chloride showed promising antimalarial activity against chloroquine-sensitive (3D7) and -resistant (Dd2) strains in vitro as well as in vivo mouse malaria model. Thus Kampo herbal medicine is a potential natural resource for novel antipathogenic agents.

Activity of benzothiazoles and chemical derivatives onPlasmodium falciparum

Parasitology ◽  
2004 ◽  
Vol 129 (5) ◽  
pp. 525-542 ◽  
Author(s):  
S. HOUT ◽  
N. AZAS ◽  
A. DARQUE ◽  
M. ROBIN ◽  
C. DI GIORGIO ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
New Drugs ◽  
Health Concern ◽  
Biological Research ◽  
Monocytic Cells ◽  
Drug Candidates ◽  
Chemical Derivatives ◽  
Anthranilic Acids

Malaria is a major health concern particularly in Africa which has about 90% of the worldwide annual clinical cases. The increasing number of drug-resistantPlasmodium falciparumjustifies the search for new drugs in this field. Antimalarial activity of 2-substituted 6-nitro- and 6-amino-benzothiazoles and their anthranilic acids has been tested. Anin vitrostudy has been performed on W2 and 3D7 strains ofP. falciparumand on clinical isolates from malaria-infected patients. Toxicity has been assessed on THP1 human monocytic cells. For the most active drug candidates, thein vitrostudy was followed byin vivoassaysonP. berghei-infected mice and byin vitroassays in order to determine the stage-dependency and the mechanism of action. Of 39 derivatives testedin vitro, 2 had specific antimalarial properties. Each compound was active on all stages of the parasite, but one was markedly active on mature schizonts, while the other was more active on young schizont forms. Both drugs were also active on mitochondrial membrane potential.In vivodata confirmed efficiency with a sustained decrease of parasitaemia. Products A12 and C7 may be considered as potential antimalarial worthy of further chemical and biological research.

scholarly journals Antimalarial Activity of Stem Bark of Periploca linearifolia during Early and Established Plasmodium Infection in Mice

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Wubetu Yihunie Belay ◽  
Abyot Endale Gurmu ◽  
Zewdu Birhanu Wubneh
Keyword(s):  
Local Community ◽  
Antimalarial Activity ◽  
Stem Bark ◽  
Negative Control ◽  
Bark Extract ◽  
Control Groups ◽  
Potential Source ◽  
Stem Bark Extract

Background. In Ethiopia, stem bark of Periploca linearifolia is used for the treatment of malaria by the local community and demonstrated antimalarial activity in vitro. Despite its in vitro antimalarial activity, no scientific study has been carried out to verify its activity in vivo. Therefore, the aim of the study was to evaluate the antimalarial activity of Periploca linearifolia stem bark extract in mice. Methods. The dried stem bark of Periploca linearifolia was extracted with 80% methanol and evaluated for its antimalarial activity on both early and established Plasmodium berghei infected mice. The extract was prepared at graded doses of 200, 400, and 600 mg/kg. Chloroquine and distilled water were administered to the positive and negative control groups, respectively. Results. The crude extract, at all tested doses, suppressed parasitemia significantly (p<0.05) for 200 and 400 mg/kg and (p<0.001) for 600 mg/kg. The suppression values at these doses were 56.98, 43.33, and 38.17 percent, respectively. Periploca linearifolia extract also demonstrated schizonticidal activity in the established malaria infection. Conclusion. The plant Periploca linearifolia has a promising antimalarial activity in mice, supporting its in vitro finding. Thus, it could be considered as a potential source to develop new antimalarial agent.

scholarly journals In Vivo Antimalarial Activity of Leaf Extracts and a Major Compound Isolated from Ranunculus multifidus Forsk

Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6179
Author(s):  
Betelhem Sirak ◽  
Lea Mann ◽  
Adrian Richter ◽  
Kaleab Asres ◽  
Peter Imming
Keyword(s):  
Antimalarial Activity ◽  
Hydrolysis Product ◽  
Preparative Thin Layer Chromatography ◽  
Antimycobacterial Activity ◽  
Major Constituent ◽  
African Countries ◽  
Leaf Extracts ◽  
Chemical Structures

The leaves of Ranunculus multifidus Forsk. are traditionally used for the treatment of malaria in several African countries. In the present study, 80% methanol (RM-M) and hydrodistilled (RM-H) extracts of fresh leaves from R. multifidus and its major constituent anemonin were tested for their in vivo antimalarial activity against Plasmodium berghei in mice. Anemonin was also tested for its in vitro antimycobacterial activity against Mycobacterium smegmatis and M. abscessus in a microbroth dilution assay, and bacterial growth was analyzed by OD measurement. The isolation of anemonin from RM-H was carried out using preparative thin layer chromatography (PTLC). The chemical structures of anemonin and its hydrolysis product were elucidated using spectroscopic methods (HR–MS; 1D and 2D-NMR). Results of the study revealed that both RM-M and RM-H were active against P. berghei in mice, although the latter demonstrated superior activity (p < 0.001), as compared to the former. At a dose of 35.00 mg/kg/day, RM-H demonstrated a chemosuppression value of 70% in a 4-day suppressive test. In a 4-day suppressive, Rane’s and prophylactic antimalarial tests, anemonin showed median effective doses (ED50s) of 2.17, 2.78 and 2.70 μM, respectively. However, anemonin did not inhibit the growth of M. smegmatis and M. abscessus.

scholarly journals Plant-derived antimalarial agents: new leads and efficient phythomedicines. Part I. Alkaloids

2009 ◽  
Vol 81 (4) ◽  
pp. 715-740 ◽  
Author(s):  
Alaíde B. Oliveira ◽  
Maria Fâni Dolabela ◽  
Fernão C. Braga ◽  
Rose L.R.P. Jácome ◽  
Fernando P. Varotti ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
New Drugs ◽  
World Health ◽  
Mortality And Morbidity ◽  
Traditional Medicines ◽  
Antimalarial Agents ◽  
Amazonian Region ◽  
Structural Classes

Malaria remains one of the most serious world health problem and the major cause of mortality and morbidity in the endemic regions. Brazil is among the 30 high-burden countries and most of the cases occur in the Legal Amazonian Region. New chemotherapeutical agents are needed for the treatment of malaria. Many plant species are used in traditional medicines of malarious countries and a relatively few number of these have been investigated for evaluation of their antimalarial effect. Still lower is the number of those that have had the active natural compounds isolated and the toxicity determined. This area is, then, of great research interest. discovery project of antimalarial natural products from plants traditionally used to treat malaria must include in vitro and in vivo assays as well as bioguided isolation of active compounds. The final products would be antimalarial chemical entities, potential new drugs or templates for new drugs development, and/or standardized antimalarial extracts which are required for pre-clinical and clinical studies when the aim is the development of effective and safe phythomedicines. This review discusses these two approaches, presents briefly the screening methodologies for evaluation of antimalarial activity and focuses the activity of alkaloids belonging to different structural classes as well as its importance as new antimalarial drugs or leads and chemical markers for phytomedicines.

scholarly journals Antimalarial activity of traditional Kampo medicine Coptis Rhizome extract and its major active compounds

2020 ◽  
Author(s):  
Awet Alem Teklemichael ◽  
Shusaku Mizukami ◽  
Kazufumi Toume ◽  
Farhana Mosaddeque ◽  
Mohamed Gomaa Kamel ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Active Compound ◽  
Antimalarial Activity ◽  
New Drugs ◽  
Herbal Extract ◽  
Herbal Extracts ◽  
Related Compounds ◽  
Malaria Model

Abstract Background: The herbal medicine has been a rich source of new drugs exemplified by quinine and artemisinin. In this study, examined a variety of Japanese traditional herbal medicine (Kampo) for their potential antimalarial activities.Methods: We designed a comprehensive screening to identify novel antimalarial drugs from a library of Kampo herbal extracts (n = 120) and related compounds (n=96). The antimalarial activity was initially evaluated in vitro against chloroquine/mefloquine-sensitive (3D7) and -resistant (Dd2) strains of Plasmodium falciparum. The cytotoxicity was also evaluated using primary Adult Mouse Brain cells. After being selected through the first in vitro assay, positive extracts and compounds were examined for possible in vivo antimalarial activity.Results: Out of 120 herbal extracts, Coptis Rhizome showed the highest antimalarial activity (IC50 1.9 µg/mL of 3D7 and 4.85 µg/mL of Dd2) with a high selectivity index (SI) > 263 (3D7) and > 103 (Dd2). Three major chlorinated compounds (coptisine, berberine, and palmatine) related to Coptis Rhizome also showed antimalarial activities with IC50 1.1, 2.6, and 6.0 µM (against 3D7) and 3.1, 6.3, and 11.8 µM (against Dd2), respectively. Among them, coptisine chloride exhibited the highest antimalarial activity (IC50 1.1 µM against 3D7 and 3.1 µM against Dd2) with SI of 37.8 and 13.2, respectively. . Finally, the herbal extract of Coptis Rhizome and its major active compound coptisine chloride exhibited significant antimalarial activity in mice infected with P. yoelii 17X strain with respect to its activity on parasite suppression consistently from day 3 to day 7 post-challenge. The effect ranged from 50.38 to 72.13% (P <.05) for Coptis Rhizome and from 81 to 89% (P <.01) for coptisine chloride.Conclusion: Coptis Rhizome and its major active compound coptisine chloride showed promising antimalarial activity against chloroquine-sensitive (3D7) and -resistant (Dd2) strains in vitro as well as in vivo mouse malaria model. Thus Kampo herbal medicine is a potential natural resource for novel antipathogenic agents.

Effect of Solanun nudum Extracts on the Liver of Mice Infected with Plasmodium berghei

2001 ◽  
Vol 29 (03n04) ◽  
pp. 477-484 ◽  
Author(s):  
Echeverri Marcela ◽  
Blair Silvia ◽  
Carmona Jaime ◽  
Pérez Pilar
Keyword(s):  
Plasmodium Falciparum ◽  
Therapeutic Effect ◽  
Aqueous Extract ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
In Vivo Studies ◽  
Hexane Extracts ◽  
Liver Changes

The plant Solanum nudum has been used by the community of Tumaco (Nariño, Colombia) as a cure for malaria. Our group has confirmed the in vitro antimalarial activity against the strain of Plasmodium falciparum FCB-2. During our in vivo studies on the therapeutic effect of Solanum nudum extracts on mice infected with Plasmodium berghei, we observed yellowish tint in the palms of mice treated with the aqueous extract via ip at a concentration of 2.4% w/vol. This findings suggested the need to carry out a histology study of the liver. Plasmodium berghei infection produces liver changes such as the deposit of pigment inn sinusoids, leucocytes infiltration, esteatosis and necrosis of hepatocytes. These changes were also observed when the mice were treated with methane and hexane extracts from Solanum nudum; however necrosis of hepatocytes in mice infected with malaria decreased 47–65% when they were administered wither with queous extract, or tumacoside A and degraded diosgenone, compounds from methane and hexane extracts of Solanum nudum respectively.

Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

2020 ◽  
Vol 27 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Abdul Jalil Shah ◽  
Roohi Mohi-ud-din ◽  
Faheem Hyder Potoo ◽  
Mohd. Akbar Dar ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Natural Products ◽  
Protective Action ◽  
New Drugs ◽  
Huperzine A ◽  
Brain Disorder ◽  
Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

Antimicrobial peptides for the treatment of pulmonary tuberculosis, allies or foes?

2018 ◽  
Vol 24 (10) ◽  
pp. 1138-1147
Author(s):  
Bruno Rivas-Santiago ◽  
Flor Torres-Juarez
Keyword(s):  
Pulmonary Tuberculosis ◽  
Antimicrobial Peptides ◽  
Experimental Models ◽  
New Drugs ◽  
World Health ◽  
Public Health Issue ◽  
Health Organization ◽  
Drug Resistant Strains

Tuberculosis is an ancient disease that has become a serious public health issue in recent years, although increasing incidence has been controlled, deaths caused by Mycobacterium tuberculosis have been accentuated due to the emerging of multi-drug resistant strains and the comorbidity with diabetes mellitus and HIV. This situation is threatening the goals of World Health Organization (WHO) to eradicate tuberculosis in 2035. WHO has called for the creation of new drugs as an alternative for the treatment of pulmonary tuberculosis, among the plausible molecules that can be used are the Antimicrobial Peptides (AMPs). These peptides have demonstrated remarkable efficacy to kill mycobacteria in vitro and in vivo in experimental models, nevertheless, these peptides not only have antimicrobial activity but also have a wide variety of functions such as angiogenesis, wound healing, immunomodulation and other well-described roles into the human physiology. Therapeutic strategies for tuberculosis using AMPs must be well thought prior to their clinical use; evaluating comorbidities, family history and risk factors to other diseases, since the wide function of AMPs, they could lead to collateral undesirable effects.

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