In vitro antiplasmodial efficacy of mangrove plant, Ipomoea pes-caprae against Plasmodium falciparum (3D7 strain)

Pothula, Veera Venkata Satish; Sunita, K.

doi:10.1016/s2222-1808(15)60963-x

Cited by 6 publications

(9 citation statements)

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“…The mechanical permanence of the erythrocytic membrane is an excellent indicator of in vitro studies for cytotoxicity screening because of its structural dynamics favoring interactions with drugs and this signifies that, the possible use of these extracts as an antiplasmodial drug in future. The mechanism of action might be due to the inhibition of hemozoin biocrystallization by the alkaloids and inhibition of protein synthesis by triterpenoids [48]. …”

Section: Discussionmentioning

confidence: 99%

Antimalarial efficacy of Pongamia pinnata (L) Pierre against Plasmodium falciparum (3D7 strain) and Plasmodium berghei (ANKA)

Satish¹,

Sunita²

2017

BMC Complement Altern Med

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BackgroundThe objective of the current study was to assess the in vitro antiplasmodial activities of leaf, bark, flower, and the root of Pongamia pinnata against chloroquine-sensitive Plasmodium falciparum (3D7 strain), cytotoxicity against Brine shrimp larvae and THP-1 cell line. For in vivo study, the plant extract which has shown potent in vitro antimalarial activity was tested against Plasmodium berghei (ANKA strain).MethodsThe plant Pongamia pinnata was collected from the herbal garden of Acharya Nagarjuna University of Guntur district, Andhra Pradesh, India. Sequentially crude extracts of methanol (polar), chloroform (non-polar), hexane (non-polar), ethyl acetate (non-polar) and aqueous (polar) of dried leaves, bark, flowers and roots of Pongamia pinnata were prepared using Soxhlet apparatus. The extracts were screened for in vitro antimalarial activity against P. falciparum 3D7 strain. The cytotoxicity studies of crude extracts were conducted against Brine shrimp larvae and THP-1 cell line. Phytochemical analysis of the plant extracts was carried out by following the standard methods. The chemical injury to erythrocytes due to the plant extracts was checked. The in vivo study was conducted on P. berghei (ANKA) infected BALB/c albino mice by following 4-Day Suppressive, Repository, and Curative tests.ResultsOut of all the tested extracts, the methanol extract of the bark of Pongamia pinnata had shown an IC50 value of 11.67 μg/mL with potent in vitro antimalarial activity and cytotoxicity evaluation revealed that this extract was not toxic against Brine shrimp and THP-1 cells. The injury to erythrocytes analysis had not shown any morphological alterations and damage to the erythrocytes after 48 h of incubation. Because methanolic bark extract of Pongamia pinnata has shown good antimalarial activity in vitro, it was also tested in vivo. So the extract had exhibited an excellent activity against P. berghei malaria parasite while decrement of parasite counts was moderately low and dose-dependent (P < 0.05) when compared to the control groups, which shown a daily increase of parasitemia, unlike the CQ-treated groups. The highest concentration of the extract (1000 mg/kg b.wt./day) had shown 83.90, 87.47 and 94.67% of chemo-suppression during Suppressive, Repository, and Curative tests respectively which is almost nearer to the standard drug Chloroquine (5 mg/kg b.wt./day). Thus, the study has revealed that the methanolic bark extract had shown promisingly high ((P < 0.05) and dose-dependent chemo-suppression. The phytochemical screening of the crude extracts had shown the presence of alkaloids, flavonoids, triterpenes, tannins, carbohydrates, phenols, coumarins, saponins, phlobatannins and steroids.ConclusionsThe present study is useful to develop new antimalarial drugs in the scenario of the growing resistance to the existing antimalarials. Thus, additional research is needed to characterize the bioactive molecules of the extracts of Pongamia pinnata that are responsible for inhibition of malaria parasite.

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Section: Discussionmentioning

confidence: 99%

Antimalarial efficacy of Pongamia pinnata (L) Pierre against Plasmodium falciparum (3D7 strain) and Plasmodium berghei (ANKA)

Satish¹,

Sunita²

2017

BMC Complement Altern Med

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“…Antimalarial assay was conducted in 96 well microtitre plates against P. falciparum 3D7 strain which sensitive to chloroquine according to the microassay by Rieckmann et al with slight modifications [22,23]. For this assay, the chalcone compounds were dissolved in dimethylsulfoxide and being prepared in a series of concentration, i.e.…”

Section: In Vitro Antimalarial Activity Assaymentioning

confidence: 99%

Synthesis, biological evaluation, QSAR analysis, and molecular docking of chalcone derivatives for antimalarial activity

Syahri

Rullah

Armunanto

et al. 2016

Asian Pac J Trop Dis

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The journal implements double-blind peer review practiced by specially invited international editorial board members. Objective: To synthesize chalcone derivatives and investigate their antimalarial activity toward chloroquine-sensitive Plasmodium falciparum 3D7 (Pf3D7) strain; to develop quantitative structureactivity relationships (QSAR) model to estimate IC 50 values for biological activity of antimalarial and compared to experimental measurement; and to determine the binding interactions of the most active compounds with targeting P. falciparum dihydrofolate reductase-thymidylate synthase using molecular docking simulation. Methods: Seven chalcone derivatives have been synthesized from substituted acetophenone and substituted benzaldehyde in ethanol with the presence of bases catalysis at reflux condition. The QSAR analysis was conducted by using Gaussian 09 software to predict IC 50 value for antimalarial activity. The in vitro test was evaluated against the chloroquine-sensitive Pf3D7 strain. Finally, the docking studies were performed with the CDOCKER protocol under the receptor-ligand interaction section in Discovery Studio® 3.1 (Accelrys, Inc., San Diego, USA). Results: Among the synthesized chalcone, a prenylated chalcone 5c and an allylated chalcones 10a showed the best IC 50 values of 1.08 and 1.73 μg/mL respectively against Pf3D7 strain (1.37 and 2.33 μg/mL based on QSAR analysis). Comparison between the prediction of IC 50 value generated from the QSAR and the outcome from an in vitro assay showed a similar result as seen from the r 2 value (r 2 = 0.99). The most active compound 5c was employed in the docking simulation to determine the potential binding interactions with active sites of P. falciparum dihydrofolate reductase-thymidylate synthase (protein data bank ID: 1J3I). The docking simulation study showed 5c bind well with Ala16, Ser108, Ile164, Trp48, and Phe58 which are the crucial interactions that could possibly interrupt the sequential catalysis reactions in the thymidylate cycle and subsequently prevent deoxythymidine monophosphate production and DNA synthesis. The formed binding interaction (H-bond) toward residues of Ala16, Ser108, and Ile164 also indicate the activity of 5c against chloroquine-resistance P. falciparum strain. Conclusions: We have successfully determined the effects of some chalcone derivatives on antimalarial activity against the chloroquine-sensitive Pf3D7 strain. Compound 5c and 10a were described a good antiplasmodial compounds. Interestingly, these in vitro results relevance with IC 50 predicted QSAR studies. Moreover, molecular docking simulation provided insight into the binding modes of 5c into the anti-folate resistance from malarial P. falciparum.

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“…Many natural product chemistry studies have been conducted on various parts of I. pes-caprae , which provides a scientific basis for certain uses of the plant in folk medicine. For instance, Pothula and Kanikaram evaluated the in vitro antimalarial activity of the root extracts of I. pes-caprae , which indicated that the methanolic extract possesses an excellent antimalarial activity with an half-maximal inhibitory concentration (IC 50 ) value of 15 µg/mL against Plasmodium falciparum strain 3D7 [ 5 ]. The phytochemical screening of the extracts of I. pes-caprae also revealed the presence of secondary metabolites, such as alkaloids, triterpenes, flavonoids, tannins, coumarins, carbohydrates, phenols, saponins, phlobatannins, and steroids [ 5 ].…”

Section: Introductionmentioning

confidence: 99%

“…For instance, Pothula and Kanikaram evaluated the in vitro antimalarial activity of the root extracts of I. pes-caprae , which indicated that the methanolic extract possesses an excellent antimalarial activity with an half-maximal inhibitory concentration (IC 50 ) value of 15 µg/mL against Plasmodium falciparum strain 3D7 [ 5 ]. The phytochemical screening of the extracts of I. pes-caprae also revealed the presence of secondary metabolites, such as alkaloids, triterpenes, flavonoids, tannins, coumarins, carbohydrates, phenols, saponins, phlobatannins, and steroids [ 5 ]. The known uses of this plant in traditional medicine can be attributed to these secondary metabolites.…”

Section: Introductionmentioning

confidence: 99%

A Medicinal Halophyte Ipomoea pes-caprae (Linn.) R. Br.: A Review of Its Botany, Traditional Uses, Phytochemistry, and Bioactivity

et al. 2022

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Ipomoea pes-caprae (Linn.) R. Br. (Convolvulaceae) is a halophytic plant that favorably grows in tropical and subtropical countries in Asia, America, Africa, and Australia. Even though this plant is considered a pan-tropical plant, I. pes-caprae has been found to occur in inland habitats and coasts of wider areas, such as Spain, Anguilla, South Africa, and Marshall Island, either through a purposeful introduction, accidentally by dispersal, or by spreading due to climate change. The plant parts are used in traditional medicine for treating a wide range of diseases, such as inflammation, gastrointestinal disorders, pain, and hypertension. Previous phytochemical analyses of the plant have revealed pharmacologically active components, such as alkaloids, glycosides, steroids, terpenoids, and flavonoids. These phytoconstituents are responsible for the wide range of biological activities possessed by I. pes-caprae plant parts and extracts. This review arranges the previous reports on the botany, distribution, traditional uses, chemical constituents, and biological activities of I. pes-caprae to facilitate further studies that would lead to the discovery of novel bioactive natural products from this halophyte.

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In vitro antiplasmodial efficacy of mangrove plant, Ipomoea pes-caprae against Plasmodium falciparum (3D7 strain)

Cited by 6 publications

References 39 publications

Antimalarial efficacy of Pongamia pinnata (L) Pierre against Plasmodium falciparum (3D7 strain) and Plasmodium berghei (ANKA)

Antimalarial efficacy of Pongamia pinnata (L) Pierre against Plasmodium falciparum (3D7 strain) and Plasmodium berghei (ANKA)

Synthesis, biological evaluation, QSAR analysis, and molecular docking of chalcone derivatives for antimalarial activity

A Medicinal Halophyte Ipomoea pes-caprae (Linn.) R. Br.: A Review of Its Botany, Traditional Uses, Phytochemistry, and Bioactivity

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