GC-MS Characterization of Phyto-Components in the Ethanolic and Hydroalcoholic Extracts of Cocos nucifera Endocarp and Evaluation of their Antimalarial Potential

2019 ◽  
Vol 9 (4) ◽  
pp. 289-294
Author(s):  
Babita Aggarwal ◽  
Pankaj Sharma ◽  
Hardarshan Singh Lamba
Keyword(s):  
Antimalarial Activity ◽  
Cocos Nucifera ◽  
Antiplasmodial Activity ◽  
Bioactive Components ◽  
Traditional Use ◽  
Standard Drug ◽  
Ic50 Values

Background: Plants are rich and cheap source of active phytoconstituents. Present study was performed in order to authenticate the traditional use of Cocos nucifera in malaria treatment as well as to search an alternative for drug resistant parasites. Objective: In the present investigation, ethanolic (ACN) and hydroalcoholic (HACN) extracts of Cocos nucifera endocarp were evaluated for antimalarial potential as well as subjected to GC-MS analysis to characterize the bioactive components. Methods: In vitro antiplasmodial activity of ACN and HACN was assessed against P. falciparum strains MRC-02 (CQ sensitive) and RKL-09 (CQ resistant) and percentage schizont maturation inhibition was determined. To confirm the antimalarial potential, in vivo Peter’s 4-Day suppressive test using P. berghei strain was performed at a dose of 25 and 50 mg/kg/day for 4 consecutive days. Bioactive components were characterized by the application of Gas chromatography and Mass spectrometric technique to the extracts. Results: Promising in vitro antiplasmodial activity was exhibited by both alcoholic (ACN) and hydroalcoholic (HACN) extracts against P. falciparum strains MRC-02 (CQ sensitive) with IC50 values < 5 µg/mL. HACN (% Suppression = 75.43 ± 0.18; MST=19.21 days) and ACN (% Suppression = 34.65 ± 0.11; MST=10.11 days) showed moderate in vivo antimalarial activity (p < 0.05) at dose 50 mg/Kg while standard drug chloroquine (8mg/kg) suppressed 100% parasitaemia. Twenty compounds have been identified and characterized by GC-MS studies.

Discovery of 3-Cinnamamido-N-Substituted Benzamides as Potential Antimalarial Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Haicheng Liu ◽  
Yushi Futamura ◽  
Honghai Wu ◽  
Aki Ishiyama ◽  
Taotao Zhang ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antimalarial Activity ◽  
In Vitro Assays ◽  
Compound Library ◽  
Antimalarial Agents ◽  
Phenotypic Screen ◽  
Ic50 Values ◽  
Substituted Benzamides

Background: Malaria is one of the most devastating parasitic diseases, yet the discovery of antimalarial agents remains profoundly challenging. Very few new antimalarials have been developed in the past 50 years, while the emergence of drug-resistance continues to appear. Objective: This study focuses on the discovery, design, synthesis, and antimalarial evaluation of 3-cinnamamido-N-substituted benzamides. Method: In this study, a screening of our compound library was carried out against the multidrug-sensitive Plasmodium falciparum 3D7 strain. Derivatives of the hit were designed, synthesized and tested against P. falciparum 3D7 and the in vivo antimalarial activity of the most active compounds was evaluated using the method of Peters’ 4-day suppressive test. Results: The retrieved hit compound 1 containing a 3-cinnamamido-N-substituted benzamide skeleton showed moderate antimalarial activity (IC50 = 1.20 µM) for the first time. A series of derivatives were then synthesized through a simple four-step workflow, and half of them exhibited slightly better antimalarial effect than the precursor 1 during the subsequent in vitro assays. Additionally, compounds 11, 23, 30 and 31 displayed potent activity with IC50 values of approximately 0.1 µM, and weak cytotoxicity against mammalian cells. However, in vivo antimalarial activity is not effective which might be ascribed to the poor solubility of these compounds. Conclusion: In this study, phenotypic screen of our compound library resulted in the first report of 3-cinnamamide framework with antimalarial activity and 40 derivatives were then designed and synthesized. Subsequent structure-activity studies showed that compounds 11, 23, 30 and 31 exhibited the most potent and selective activity against P. falciparum 3D7 strain with IC50 values around 0.1 µM. Our work herein sets another example of phenotypic screen-based drug discovery, leading to potentially promising candidates of novel antimalarial agents once given further optimization.

scholarly journals Antimalarial Effect of the Total Glycosides of the Medicinal Plant, Ranunculus japonicus

Pathogens ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 532
Author(s):  
Hae-Soo Yun ◽  
Sylvatrie-Danne Dinzouna-Boutamba ◽  
Sanghyun Lee ◽  
Zin Moon ◽  
Dongmi Kwak ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Hematological Parameters ◽  
Significant Inhibition ◽  
Ic50 Values ◽  
The Republic

In traditional Chinese medicine, Ranunculus japonicus has been used to treat various diseases, including malaria, and the young stem of R. japonicus is consumed as a food in the Republic of Korea. However, experimental evidence of the antimalarial effect of R. japonicus has not been evaluated. Therefore, the antimalarial activity of the extract of the young stem of R. japonicus was evaluated in vitro using both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains; in vivo activity was evaluated in Plasmodium berghei-infected mice via oral administration followed by a four-day suppressive test focused on biochemical and hematological parameters. Exposure to extracts of R. japonicus resulted in significant inhibition of both chloroquine-sensitive (3D7) and resistant (Dd2) strains of P. falciparum, with IC50 values of 6.29 ± 2.78 and 5.36 ± 4.93 μg/mL, respectively. Administration of R. japonicus also resulted in potent antimalarial activity against P. berghei in infected mice with no associated toxicity; treatment also resulted in improved hepatic, renal, and hematologic parameters. These results demonstrate the antimalarial effects of R. japonicus both in vitro and in vivo with no apparent toxicity.

scholarly journals In Vitro Antimalarial Activity of Extracts of Some Indigenous Plant Species in Kebbi State

2020 ◽  
pp. 1-10
Author(s):  
Aisha Abdulrazak ◽  
Keyword(s):  
Medicinal Plants ◽  
Aqueous Extract ◽  
Antimalarial Activity ◽  
Antimicrobial Activities ◽  
Antiplasmodial Activity ◽  
Phytochemical Screening ◽  
Indigenous Plants ◽  
Traditional Use ◽  
Water As Solvent

The search for antimalarial compounds has been necessitated by the resistance of Plasmodium falciparum to almost all antimalarial drugs. The aim of this research was to determine in-vitro antimalarial activity of extracts of some indigenous plants species in Kebbi State. Plant extraction was carried-out by maceration using ethanol and water as solvent. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates of P. falciparum using WHO method of in-vitro micro test. Phytochemical screening was also carried out on the extract to deduce the active chemicals present in the plant extract. All plant extracts demonstrate dose dependent antimicrobial activities with IC50 Less than 50%. However highest growth inhibition of the P. falciparum was demonstrated by aqueous and ethanol extract of A. indica with IC50 7.4µg/ml and 8.6µg/ml respectively followed by ethanol and aqueous extract of C. occidentalis with IC50 15.3µg/ml and 18.0µg/ml respectively. Least antimalarial activity was demonstrated by aqueous extract of M. oleifera with IC50 33.5µg/ml while ethanolic extract of M. oleifera demonstrated IC50 of 20.50µg/ml. M. indica ethanolic and aqueous extract also demonstrated moderate antimalarial activity with IC50 18.8µg/ml and 24.5µg/ml. The phytochemical screening of medicinal plants showed the presence of tannins, saponins, alkaloids, flavonoid, phenol and cardiac glycosides in the extracts, which may be responsible for the antiplasmodial activity. This result justifies the traditional use of the plant in malaria treatment and further research is suggested to identify and characterize the active principles from the plants. Keywords: Antimalaria, Invitro, Medicinal Plants, Malaria, Kebbi

scholarly journals IN-VITRO HYPOGLYCEMIC EVALUATION OF FRACTIONS OF HYDRO-ACOHOLIC EXTRACT OF HEARTWOOD OF TECOMELLA UNDULATA LINN.

2017 ◽  
Vol 10 (2) ◽  
pp. 266
Author(s):  
Munish Garg ◽  
Ruby Rohilla ◽  
Chanchal Garg
Keyword(s):  
Postprandial Hyperglycemia ◽  
Alcoholic Extract ◽  
Phytochemical Screening ◽  
Bioactive Components ◽  
Standard Drug ◽  
Minimal Inhibitory Concentrations ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Tecomella Undulata

Objective: To screen α-amylase and α-glucosidase inhibitors from the different fractions of crude hydro-alcoholic extract of heartwood of Tecomella undulata Linn.Methods: Four fractions of crude hydro-alcoholic extract of heartwood of plant were used for in-vitro inhibitory assays against digestive enzymes: α-amylase and α-glucosidase. For assay, different concentrations (20, 40, 60, 80, 100 µg/ml) were used for all fractions. Standard protocol was used for preliminary phytochemical screening of different bioactive components present in all fractions.Results: The fractions have shown moderate to highest inhibitory activity against both enzymes. But, the strong inhibition was revealed by acetone fraction against α-amylase with very minimal inhibitory concentrations at IC50 values when compared with a standard drug acarbose. Several medicinally active phytocomponents such as flavanoids, saponin, anthraquinones, tannins, triterpenoids and phenols were observed in all studied fractions.Conclusion: The different fractions prepared from crude hydro-alcoholic extract of heartwood of plant are capable of inhibiting α-amylase and α-glucosidase and it can be concluded that heartwood of Tecomella undulata Linn. is partially active against postprandial hyperglycemia, thus diabetes mellitus.Keywords: Tecomella undulata Linn., Diabetes mellitus, α-Amylase, α-Glucosidase. 

scholarly journals In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues

2020 ◽  
Author(s):  
Fidelia Ijeoma Uche ◽  
Xiaozhen Guo ◽  
Jude Okokon ◽  
Imran Ullah ◽  
Paul Horrocks ◽  
...  
Keyword(s):  
Metabolic Pathways ◽  
High Performance ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Antiplasmodial Activity ◽  
Survival Times ◽  
Antiproliferative Effects ◽  
Future Evaluation

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2′-norcocsuline (3)) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semi-synthetic analogues (4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR Green 1 fluorescence assay. The in vivo antimalarial activity of cycleanine (1) is then investigated in suppressive, prophylactic and curative murine malaria models after infection with a chloroquine-sensitive Plasmodium berghei strain. BBIQ alkaloids (1–5) exerted in vitro antiplasmodial activities with IC50 at low micromolar concentrations with the two semi-synthetic cycleanine analogues showing an improved potency and selectivity than cycleanine. At oral doses of 25 and 50mg/kg body weight of infected mice, cycleanine suppressed the levels of parasitaemia, and increased mean survival times significantly compared to the control groups. The metabolites and metabolic pathways of cycleanine (1) were also studied using high performance liquid chromatography electrospray ionization tandem mass spectrometry. Twelve novel metabolites were detected in rats after intragastic administration of cycleanine. The metabolic pathways of cycleanine were demonstrated to involve hydroxylation, dehydrogenation, and demethylation. Overall, these in vitro and in vivo results provide a basis for the future evaluation of cycleanine and its analogues as leads for further development.

scholarly journals Antiplasmodial and Cytotoxic Cytochalasins from an Endophytic Fungus, Nemania sp. UM10M, Isolated from a Diseased Torreya taxifolia Leaf

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 777 ◽  
Author(s):  
Mallika Kumarihamy ◽  
Daneel Ferreira ◽  
Edward Croom ◽  
Rajnish Sahu ◽  
Babu Tekwani ◽  
...  
Keyword(s):  
Mouse Model ◽  
Solid Tumor ◽  
Endophytic Fungus ◽  
Antimalarial Activity ◽  
Vero Cells ◽  
Antiplasmodial Activity ◽  
Etoac Extract ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of an EtOAc extract of the broth of the endophytic fungus Nemania sp. UM10M (Xylariaceae) isolated from a diseased Torreya taxifolia leaf afforded three known cytochalasins, 19,20-epoxycytochalasins C (1) and D (2), and 18-deoxy-19,20-epoxy-cytochalasin C (3). All three compounds showed potent in vitro antiplasmodial activity and phytotoxicity with no cytotoxicity to Vero cells. These compounds exhibited moderate to weak cytotoxicity to some of the cell lines of a panel of solid tumor (SK-MEL, KB, BT-549, and SK-OV-3) and kidney epithelial cells (LLC-PK11). Evaluation of in vivo antimalarial activity of 19,20-epoxycytochalasin C (1) in a mouse model at 100 mg/kg dose showed that this compound had weak suppressive antiplasmodial activity and was toxic to animals.

scholarly journals In Vitro and In Vivo Effectiveness of Carvacrol, Thymol and Linalool against Leishmania infantum

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2072 ◽  
Author(s):  
Mohammad Reza Youssefi ◽  
Elham Moghaddas ◽  
Mohaddeseh Abouhosseini Tabari ◽  
Ali Akbar Moghadamnia ◽  
Seyed Mohammad Hosseini ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Leishmania Infantum ◽  
Standard Drug ◽  
In Vivo Test ◽  
Causative Agents ◽  
Ic50 Values ◽  
Vector Borne ◽  
Effective Drugs

Background: One of the most important causative agents of visceral leishmaniasis (VL) is Leishmania infantum, which is mainly spread by Phlebotomus and Lutzomyia sandflies in the Old and New World, respectively. Novel and effective drugs to manage this neglected vector-borne disease are urgently required. In this study, we evaluated the toxicity of carvacrol, thymol and linalool, three common essential oil constituents, on amastigotes and promastigotes of L. infantum. Methods: in vitro experiments were performed by 24 h MTT assay. Carvacrol, thymol and linalool at concentrations ranging from 1.3 to 10 μg/mL were tested on promastigotes of L. infantum. For in vivo test, two groups of hamsters (Mesocricetus auratus) received 100 mg/kg of body weight/day of carvacrol and thymol as intraperitoneal injection on day 7 post-infection, followed by a 48 h later injection. The third group was treated with the glucantime as standard drug (500 mg/kg) and the last group (control) just received normal saline. On the 16th day, the number of parasites and histopathological changes in liver and spleen were investigated. Results: 24 h MTT assay showed promising antileishmanial activity of thymol and carvacrol, with IC50 values of 7.2 (48 μM) and 9.8 μg/mL (65 μM), respectively. Linalool at all concentrations did not affect L. infantum promastigote viability. In vivo toxicity data of carvacrol and thymol showed that the former at 100 mg/kg was the safest and most effective treatment with little side effects on the liver. Conclusions: Overall, thymol and carvacrol are highly promising candidates for the development of effective and safe drugs in the fight against VL.

scholarly journals Andrographolide: A Novel Antimalarial Diterpene Lactone Compound fromAndrographis paniculataand Its Interaction with Curcumin and Artesunate

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Kirti Mishra ◽  
Aditya P. Dash ◽  
Nrisingha Dey
Keyword(s):  
Plasmodium Falciparum ◽  
Life Span ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Andrographis Paniculata ◽  
Antiplasmodial Activity ◽  
Template Molecule

Andrographolide (AND), the diterpene lactone compound, was purified by HPLC from the methanolic fraction of the plantAndrographis 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 ofPlasmodium falciparum in vitroandPlasmodium bergheiANKAin vivo. IC50s 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 thein vivosystem this agent can be used as template molecule for designing new derivatives with improved antimalarial properties.

scholarly journals Novel Antiplasmodial Agents from Christia vespertilionis

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Harish C. Upadhyay ◽  
Brijesh S. Sisodia ◽  
Harveer S. Cheema ◽  
Jyoti Agrawal ◽  
Anirban Pal ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Complete Suppression ◽  
The Novel ◽  
Aqueous Methanol ◽  
Isolation And Characterization ◽  
First Time ◽  
Detailed Chemical

The roots, leaves and stems of Christia vespertilionis were separately and successively extracted with methanol and aqueous-methanol (1:4, v/v) and were evaluated in vitro for their antiplasmodial potential against Plasmodium falciparum NF-54. The aqueous-methanolic stem (AS) extract was the most active (IC50 7.5 μg/mL) followed by the methanolic leaf (ML) extract (IC50 32.0 μg/mL). The in vivo antimalarial activity of the combined plant extract of C. vespertilionis was also assessed in P. berghei infected mice, which showed 87.8% suppression of parasitaemia as compared with complete suppression by chloroquine on day 8. Finally, detailed chemical investigation of C. vespertilionis resulted in the isolation and characterization of fifteen compounds (1–15), of which two (1 and 4) are being reported for the first time from nature. The novel compound 1 possesses potent antiplasmodial activity (IC50 = 9.0 μg/mL).

scholarly journals In Vivo Antiplasmodial Activity of Terminalia mantaly Stem Bark Aqueous Extract in Mice Infected by Plasmodium berghei

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Mariscal Brice Tchatat Tali ◽  
Cedric Derick Jiatsa Mbouna ◽  
Lauve Rachel Yamthe Tchokouaha ◽  
Patrick Valere Tsouh Fokou ◽  
Jaures Marius Tsakem Nangap ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Aqueous Extract ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Lethal Dose ◽  
Stem Bark ◽  
Antiplasmodial Activity ◽  
Bark Extract

Background. Terminalia mantaly is used in Cameroon traditional medicine to treat malaria and related symptoms. However, its antiplasmodial efficacy is still to be established. Objectives. The present study is aimed at evaluating the in vitro and in vivo antiplasmodial activity and the oral acute toxicity of the Terminalia mantaly extracts. Materials and Methods. Extracts were prepared from leaves and stem bark of T. mantaly, by maceration in distilled water, methanol, ethanol, dichloromethane (DCM), and hexane. All extracts were initially screened in vitro against the chloroquine-resistant strain W2 of P. falciparum to confirm its in vitro activity, and the most potent one was assessed in malaria mouse model at three concentrations (100, 200, and 400 mg/kg/bw). Biochemical, hematological, and histological parameters were also determined. Results. Overall, 7 extracts showed in vitro antiplasmodial activity with IC50 ranging from 0.809 μg/mL to 5.886 μg/mL. The aqueous extract from the stem bark of T. mantaly (Tmsbw) was the most potent (IC50=0.809 μg/mL) and was further assessed for acute toxicity and efficacy in Plasmodium berghei-infected mice. Tmsbw was safe in mice with a median lethal dose (LD50) higher than 2000 mg/kg of body weight. It also exerted a good antimalarial efficacy in vivo with ED50 of 69.50 mg/kg and had no significant effect on biochemical, hematological, and histological parameters. Conclusion. The results suggest that the stem bark extract of T. mantaly possesses antimalarial activity.

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