scholarly journals Phytochemical Investigation and In vitro Antimalarial Activity of Acalypha indica (L.) and Cocculus hirsutus (L.) From Prakasam District, Andhra Pradesh, India

2018 ◽  
Vol 11 (4) ◽  
pp. 2123-2134
Author(s):  
Pasumarthi Brahmam ◽  
Kanikaram Sunita
Keyword(s):  
Ethyl Acetate ◽  
Andhra Pradesh ◽  
Antimalarial Activity ◽  
Standard Laboratory ◽  
Phytochemical Screening ◽  
Ic50 Values ◽  
Cocculus Hirsutus ◽  
Acalypha Indica ◽  
Ethyl Acetate Extracts

The present study, report the phytochemical analysis and in vitro antimalarial activity of plants Acalypha indica (L.) and Cocculus hirsutus (L.). The A. indica and C. hirsutus plant was collected from Kadaparajupalle at Dornala mandal, Prakasam district, Andhra Pradesh, India. Leaf, stem bark and root crude extracts prepared in Soxhlet apparatus with chloroform, ethyl acetate and methanol solvents. The preliminary phytochemical screening of these extracts was conducted by following the standard methods. These extracts were tested for in vitro antimalarial activity against 3D7 and K1 strains of Plasmodium falciparum by standard laboratory protocol. In vitro cytotoxicity of the extracts was also tested by following standard laboratory method. The phytochemical screening has revealed the presence of alkaloids, saponins, terpenoids & steroids, tannins, anthocyanidins, phenolic compounds, coumarins, quinones, resins and glycosides. Amongst all the extracts screened for antimalarial activity, the leaf chloroform and ethyl acetate extracts of A. indica shown IC50 values of 3.34 µg/mL and 3.71 µg/mL respectively against 3D7 strain; the leaf chloroform and ethyl acetate extracts of A. indica shown IC50 values of 1.47 µg/mL and 2.32 µg/mL respectively against K1 strain; the root chloroform and methanol extracts of C. hirsutus shown IC50 values of <0.78 µg/mL and 3.714 µg/mL respectively against 3D7 strain; the root chloroform and methanol extracts of C. hirsutus shown IC50 values of <0.78 µg/mL and 2.10 µg/mL respectively against K1 strain. Thus, the above extracts have shown very active antimalarial activity against 3D7 and K1 strains. And all the extracts were non-toxic showing CC50 values of >20 µg/mL against Vero cell line. The presence of high alkaloids, flavonoids and terpenoids of the plant extracts suggest their antioxidant potential and justifies their therapeutic action which could be used for the drug formulation. The chloroform root extract of C. hirsutus has shown excellent antimalarial activity which can be used for the development of new antimalarial drug policies.

scholarly journals Inhibition of Heme Polymerization Invitro Assay Of Extract of Sirih Leaf (Piper betle Linn.) and Sun Flower Leaves (Helianthus annuus L.)

2020 ◽  
Vol 7 (1) ◽  
pp. 22 ◽  
Author(s):  
Ami Tjitraresmi ◽  
Moelyono Moektiwardoyo ◽  
Yasmiwar Susilawati
Keyword(s):  
Helianthus Annuus ◽  
Antimalarial Activity ◽  
Antimalarial Drugs ◽  
Piper Betle ◽  
Phytochemical Screening ◽  
Helianthus Annuus L ◽  
Betel Leaf ◽  
The People ◽  
Ic50 Values

Malaria is a disease that occurs in tropical countries like Indonesia. The incidence of malaria in the world is still quite high and the occurrence of cases of Plasmodium resistance to antimalarial drugs and the widespread of resistance have prompted researchers to look for new antimalarial drugs, especially from natural materials. Betel leaf (Piper betle Linn.) And sunflower leaf (Helianthus annuus L.) have long been used by the people of Indonesia as an antimalarial drug. The purpose of this study was to determine antimalarial activity through inhibition of heme polymerization and determine secondary metabolite compounds by phytochemical screening from betel leaves and sunflower leaves. The heme polymerization inhibition activity assay was carried out by the in-vitro method using a microplate reader at 415 nm and 630 nm wavelengths. IC50 values of betel leaf extract and sunflower leaf were 178.67 μg/ml and 160.10 μg/ml, respectively. Phytochemical screening results from betel leaf showed the presence of flavonoids, polyphenols, tannins, quinones, saponins, and monoterpenoids-sesquiterpenoids, while sunflower leaves contain alkaloids, polyphenols, flavonoids, steroids and monoterpenoids-sesquiterpenoids.Keywords: Piper betle Linn., Helianthus annuus L., Malaria, Heme Polymerization

scholarly journals COMPARISON OF INHIBITORY ACTIVITY AGAINST THE α-GLUCOSIDASE ENZYMES IN THE EXTRACTS AND FRACTIONS FROM LEAVES OF THE GARCINIA KYDIA ROXBURGH

2017 ◽  
Vol 10 (7) ◽  
pp. 401
Author(s):  
Septiani Martha ◽  
Berna Elya ◽  
Muhammad Hanafi
Keyword(s):  
Ethyl Acetate ◽  
Inhibitory Activity ◽  
Enzymatic Reaction ◽  
Active Fraction ◽  
Pharmacological Activities ◽  
Percent Inhibition ◽  
Ic50 Values ◽  
Microplate Reader ◽  
Ethyl Acetate Extracts

Objective : Garcinia kydia Roxb. is aspecies of the genus Garcinia, is based chemotaxonomic has various bioactive compounds that have been isolated by a variety of pharmacological activities, one of the activities that are being developed that inhibition of         α-glucosidase. However, α-glucosidase inhibitory activity in the extracts and fraction from leaves of the Garcinia kydia Roxb. has not been reported. In this study, seeks to evaluated of α-glucosidase inhibitory activity against extracts and fractions of potentially.Methods : The α-glucosidase inhibitory activity test, conducted by in-vitro using the enzymatic reaction is measured of quantity with a microplate reader and identify the compound from the active fraction with normal-phase thin layer chromatography.Results : The ethyl acetate and methanol extract have the potential to inhibit the α-glucosidase with the percent inhibition at a concentration of 500μg/mL of 83 and 59%, respectively. The active fraction of the ethyl acetate extracts (FEA8) with percent inhibition at concentrations of 100 mg/mL and IC50 values of 80% and 2,79μg/mL, respectively and active fraction of the methanol extracts (FMT3) with percent inhibition at concentrations of 100 mg/mL and IC50 values of 71% and 8,43 μg/mL, respectively.Conclusion: Garcinia kydia Roxb. evident has the potential to inhibit the α-glucosidase. Flavonoid and phenolic compounds that suspected of acts as α-glucosidase inhibitory activity. Thus, the research will continue the process of isolating the active compound so that it can be developed as natural therapeutic agents in the control of glucose.

scholarly journals Penentuan Aktivitas Antioksidan dan Antidiabetes Ekstrak Daun Matoa (Pometia pinnata J.R. Forst. & G. Forst.) secara In Vitro

2021 ◽  
Vol 11 (2) ◽  
pp. 132-141
Author(s):  
Lestyo Wulandari ◽  
Ari Satya Nugraha ◽  
Ulfa Aliyatul Himmah
Keyword(s):  
Antioxidant Activity ◽  
Ethyl Acetate ◽  
Leaf Extract ◽  
Pearson Correlation ◽  
The Body ◽  
Antidiabetic Activity ◽  
Ic50 Values ◽  
High Antioxidant Activity ◽  
Ethyl Acetate Extracts

Matoa (Pometia pinnata J.R. Forst. & G. Forst.) Matoa (Pometia pinnata J.R. Forst. & G. Forst.) is one of the plants that is used as a traditional medicine for diabetes mellitus due to an imbalance between the amount of ROS and antioxidants in the body. Therefore, it was carried out in vitro to see the antioxidant and antidiabetic activity in matoa leaf extract. The extraction of matoa leaves was carried out using the ultrasonication method for 30 minutes with methanol, ethanol, and ethyl acetate as solvents. Antioxidant activity is release through DPPH free radical inhibition, through the antidiabetic potential released by inhibiting the work of the α-amylase enzyme. Phytochemical test results showed the presence of secondary metabolites in the form of flavonoids, polyphenols, tannins, alkaloids, and terpenoids. The results of the research on methanol, ethanol, and ethyl acetate extracts of matoa leaves showed high antioxidant activity with IC50 values of 6.416 ± 0.176 ppm, 8.622 ± 0.066 ppm, and 170.637 ± 4.441 ppm, respectively, but they were less potent than vitamin C as a comparison which is 1.646 ± 0.015 ppm. Inhibition of the α-amylase enzyme showed IC50 values of 91.037 ± 0.750 ppm, 105,166 ± 2,423 ppm, and 785,436 ± 11,740 ppm in each of the methanol, ethanol, and ethyl acetate extracts while the IC50 value of acarbose as a comparison was 23,479 ± 0.347 ppm. The statistical data analysis of Pearson correlation showed that it had a positive relationship between the antioxidant and antidiabetic activity of matoa leaf extract as seen from the R-value of 0.998. The higher antioxidant activity, so the higher potential for inhibition of α-amylase enzyme.

scholarly journals Antimalarial Activity of Curcuma Caesia Against 3D7 and K1 Strains of Plasmodium Falciparum

2020 ◽  
Author(s):  
Monika Chaturvedi ◽  
Reena Rani ◽  
Dushyant Sharma ◽  
Jaya Parkash Yadav
Keyword(s):  
Plasmodium Falciparum ◽  
Ethyl Acetate ◽  
In Silico ◽  
Antimalarial Activity ◽  
Antimalarial Drugs ◽  
Mechanism Study ◽  
Effective Development ◽  
Ethyl Acetate Extracts

Abstract Background: Malaria is a severe and sometimes mortal tropical disease that spreads through parasites. The purpose of the study was to evaluate in vitro and in-silicoantiplasmodial potential of Curcuma caesia extracts against Plasmodium falciparum.Methods: Lack of a vaccine and the widespread resistance to antimalarial drugs have resulted in emphasis on novel antimalarial drugs development. Ethyl acetate and methanol extracts of Curcuma caesia were prepared and analysed for their antiplasmodial activity against Chloroquine sensitive (3D7) and resistant (K1) strains of P. falciparumusingfluorescence-based SYBR Green assay. The cytotoxicity tests were carried out using the verocell lines by MTT assay.The phosphoethanolamine methyltransferase enzyme ((PfPMT) essential for growth of Plasmodium falciparum was used as protein target for in-silicostudy.Result: Curcuma caesia ethyl acetate extracts showedpotentantiplasmodial activitywith IC50 values of 3.37 µg/ml and 1.53 µg/ml against 3D7 and K1 strain respectively.Docking results show that β-selinenol an oxygenized sesquiterpene had the free binding energy of -6.76 Kcal/mol.Conclusion: Sesquiterpene present in the Curcuma caesia extract was responsible for antimalarial potential analyzed by molecular modeling. The present findings, however preliminary in nature. Further studies are required to proven the antimalarial efficacy C. caesia by isolating the active compounds and in vivo mechanism study that may contribute to more effective development of antimalarial drugs in the future.

scholarly journals IN VITRO ANTIOXIDANT AND ANTIBACTERIAL ACTIVITIES OF FRACTIONATED EXTRACTS AND ISOLATION OF BIOACTIVE COMPONENTS FROM BREYNIA VITIS-IDAEA (BURM. F.) C. E. C. FISCHER LEAVES

2018 ◽  
Vol 54 (2C) ◽  
pp. 354
Author(s):  
Nguyễn Thị Lan Hương
Keyword(s):  
Ethyl Acetate ◽  
Radical Scavenging ◽  
Antibacterial Activities ◽  
Bioactive Components ◽  
Radical Scavenging Capacity ◽  
Scavenging Capacity ◽  
Ic50 Values ◽  
Ethanol Extracts ◽  
Ethyl Acetate Extracts

This study investigated the antioxidant and antibacterial activities of ethyl acetate, nbutanoland ethanol extracts of Breynia vitis-idaea (Burm.f.) C. E. C. Fischer leaves using invitro assays;and isolated bioactive compounds from the fractioned extract which showed the bestproperties by column chromatography. All extracts showed significant radical scavengingactivities and exhibited antibacterial activities against Enterococcus faecalis, Staphylococcusaureus and methicillin-resistant Staphylococcus aureus (MRSA). Ethyl acetate extracts showedthe highest free radical scavenging capacity with the IC50 values of 99.55 and 94.66 μg/ml (inDPPH and ABTS assays, respectively) and exhibited MIC values of 1.5, 1 and 1 mg/ml againstthe three bacteria, respectively. In addition, from ethyl acetate extracts, one pure compound hasbeen obtained and identified as 6-O-benzoylarbutin.

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.

In Vitro Antioxidant Activity Metaplexis Japonica Makino Extract and Derivatives

2014 ◽  
Vol 955-959 ◽  
pp. 387-389 ◽  
Author(s):  
Bao Qing Wang
Keyword(s):  
Antioxidant Activity ◽  
Linoleic Acid ◽  
Ethyl Acetate ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Acid Test ◽  
Acetone Extracts ◽  
Β Carotene ◽  
Ethyl Acetate Extracts

Antioxidant activities of acetone and ethyl acetate extracts from Metaplexis japonica Makino, one of famous medicine plants in the eastnorth region of China, named luomo in Chinese, were examined by a DPPH (1,1-Diphenyl-2-picrylhydrazyl) radical-scavenging assay and a β-carotene-linoleic acid test. In DPPH, the antioxidant activity of the acetone extracts, ethyl acetate extracts and derivative were IC50 were 313.21, 266.92 and 118.78μg/mL, respectively. In the β-carotene-linoleic acid test, IC50 were 285.09, 351.57 and 123.89μg/mL. It was concluded that Metaplexis japonica Makino and its derivatives might be a potential natural source of antioxidants .

scholarly journals Assessment of Antimalarial Activity againstPlasmodium falciparumand Phytochemical Screening of Some Yemeni Medicinal Plants

2009 ◽  
Vol 6 (4) ◽  
pp. 453-456 ◽  
Author(s):  
Mohammed A. Alshawsh ◽  
Ramzi A. Mothana ◽  
Hassan A. Al-shamahy ◽  
Salah F. Alsllami ◽  
Ulrike Lindequist
Keyword(s):  
Medicinal Plants ◽  
Antimalarial Activity ◽  
Traditional Healers ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Moderate Activity ◽  
Phytochemical Screening ◽  
Cissus Rotundifolia ◽  
Health Organization

Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. In the present study, six selected plants (Acalypha fruticosa,Azadirachta indica,Cissus rotundifolia,Echium rauwalfii,Dendrosicyos socotranaandBoswellia elongata) commonly used in Yemen by traditional healers for the treatment of malaria as well as other diseases, were collected from different localities of Yemen, dried and extracted with methanol and water successfully. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates ofPlasmodium falciparum. The selectivity parameters to evaluate the efficacy of these medicinal plants were measured byin vitromicro test (Mark III) according to World Health Organization (WHO) 1996 & WHO 2001 protocols of antimalarial drug tests. Among the investigated 12 extracts, three were found to have significant antiplasmodial activity with IC50values less than 4 µg/ml, namely the water extracts ofA. fruticosa,A. indicaandD. socotrana. Six extracts showed moderate activity with IC50values ranging from 10 to 30 µg/ml and three appeared to be inactive with IC50values more than 30 µg/ml. In addition, preliminary phytochemical screening of the methanolic and aqueous extracts indicated the presence of saponins, tannins, flavonoids, terpenoids, polysaccharides and peptides.

scholarly journals SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME NEW 3-PHENYL-2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES

2017 ◽  
Vol 9 (3) ◽  
pp. 58
Author(s):  
Mehul Zaveri ◽  
Neha Kawathekar
Keyword(s):  
Antimalarial Activity ◽  
Research Work ◽  
Aromatic Aldehydes ◽  
Maximum Activity ◽  
Spectroscopic Techniques ◽  
Activity Data ◽  
Antimalarial Agents ◽  
Ic50 Values ◽  
Current Therapies

Objective: Current therapies to treat P. falciparum malaria are heavily reliant on artemisinin-based combinations. However, resistance to artemisinin has recently been identified, and resistance to key artemisinin partner drugs is already widespread. Therefore, there is an urgent need for new antimalarial drugs with improved attributes over older therapies. The objective of this research work is to synthesize new antimalarial agents more effective against clinically relevant malarial strains.Methods: In present work, a series of ten 3-phenyl-2-thioxothiazolidin-4-one (MF1-MF10) derivatives, were synthesized by Knoevenagel condensation of N-phenyl rhodanine (I1) with substituted aromatic or hetro aromatic aldehydes using microwave irradiation. N-phenyl rhodanine (I1) was synthesized by a conventional reaction involving methyl-2-mercaptoacetate (1) and phenyl Isothiocyanates in presence of triethylamine. All the synthesized compounds were characterized by various spectroscopic techniques and evaluated for in-vitro antimalarial activity by microdilution technique against resistance strains of Plasmodium falciparum.Results: The antimalarial activity data showed that six compounds (MF1, MF3, MF4, MF5, MF7 and MF8) exhibited IC50 values ranging from 1.0-1.30 µg/ml, three compounds (MF2, MF6 and MF10) displayed IC50 values in the range of 0.9-1.0 µg/ml. Compound MF9 showed most significant result with maximum activity (IC50 = 0.85µg/ml).Conclusion: The antimalarial activity results revealed that compound MF9 possess potent activity and could be identified as a promising lead for further investigation.

Sign in / Sign up

Export Citation Format

Share Document