Bioguided isolation of antiplasmodial secondary metabolites from Persea americana Mill. (Lauraceae)

Abstract The antiplasmodium assay-guided investigation of the roots, stem bark, and leaves of Persea americana Mill. led to the isolation of a new fatty alcohol, perseatriol (1), along with six known compounds (2–7). Their structures were elucidated based on the analysis of their NMR and MS data. All crude extracts and fractions exhibited good antiplasmodial activity on Plasmoduim falciparum 3D7 with IC50 values ranging from 0.76 to 10.5 μg/mL; they also displayed cytotoxicity against HeLa cells with low selectivity indexes (SIs). A preliminary Plasmodium lactate dehydrogenase (pLDH) assay was also performed on the isolated compounds. 9,9′-Di-O-feruloyl-5,5′-dimethoxysecoisolariciresinol (4) turned out to be non-toxic and displayed the best activities on P. falciparum with an IC50 value of 0.05 μM, comparable to the reference drug chloroquine with an IC50 value of 0.03 μM. Furthermore, besides compound 4, this work reports the first isolation of lutein (2) and scopoletin (3) from P. americana. The crude extracts of roots, stem bark, and leaves of P. americana, their fractions and compounds completely suppressed the growth of P. falciparum. The observed activity supports the use of P. americana in folk medicine for the treatment of malaria.

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In vitro antiplasmodial activity and cytotoxicity of crude extracts and compounds from the stem bark of Kigelia africana (Lam.) Benth (Bignoniaceae)

Parasitology Research ◽

10.1007/s00436-011-2363-y ◽

2011 ◽

Vol 108 (6) ◽

pp. 1383-1390 ◽

Cited By ~ 23

Author(s):

Denis Zofou ◽

Archile Bernabe Ouambo Kengne ◽

Mathieu Tene ◽

Moses N. Ngemenya ◽

Pierre Tane ◽

...

Keyword(s):

Stem Bark ◽

Antiplasmodial Activity ◽

Crude Extracts

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In vivo Antiplasmodial and Toxicological Effects of Goniothalamus lanceolatus Crude Extracts

Natural Product Communications ◽

10.1177/1934578x1701200826 ◽

2017 ◽

Vol 12 (8) ◽

pp. 1934578X1701200 ◽

Cited By ~ 1

Author(s):

Rozaini Mohd Zohdi ◽

Shahida Muhamad Mukhtar ◽

Nur Vicky Bihud ◽

Nurulfazlina Edayah Rasol ◽

Fasihuddin Badruddin Ahmad ◽

...

Keyword(s):

Acute Toxicity ◽

Crude Extract ◽

Stem Bark ◽

Antiplasmodial Activity ◽

Bark Extract ◽

Phytochemical Analysis ◽

Root Extract ◽

Crude Extracts ◽

Leaves And Roots

This study is aimed at investigating the antiplasmodial activity and acute toxicity of the methanol (MeOH) extracts of the leaves and roots, and the dichloromethane (DCM) extracts of the stem bark, leaves, and roots of Goniothalamus lanceolatus. Phytochemical analysis was then carried out on the most active extract. In vivo antiplasmodial activity was assessed using the 4-day suppressive test against Plasmodium berghei ANKA (PbANKA) in mice. The plant extracts were administered intraperitoneally (i.p.) as a single dose (30 mg/kg) starting 4 h after infection. At a dose level of 30 mg/kg (i.p.), the DCM extracts of the stem bark and leaves, and the MeOH root extracts, prolonged the survival period of infected mice compared to that of the negative control. In addition, all crude extracts, except for the DCM root extract, exhibited parasitemia suppressive activity. The highest level of parasitemia suppression was recorded in mice treated with the DCM stem bark extract at 66.3%. No mortality was observed in mice treated with the DCM extracts of the stem bark and leaves, and the MeOH extract of the leaves, indicating that the LD50 is greater than 300 mg/kg. On the other hand, both the MeOH and DCM extracts of the roots showed toxic effects at a dose of 300 mg/kg (i.p) with an 83.3% mortality rate. The results obtained indicate that the stem bark of G. lanceolatus (DCM crude extract) possesses good antiplasmodial activity against PbANKA infected mice without causing acute toxicity. Five known styrylpyrone derivatives namely goniodiol 1, 8-epi-9-deoxygoniopypyrone 2, 9-deoxygoniopypyrone 3, digoniodiol 4 and goniothalamin 5 have been isolated from the bark of Goniothalamus lanceolatus (DCM crude extract). The structures and stereochemistry of all compounds were elucidated by interpretation of spectroscopic data. This study provides a scientific basis to support the traditional use of the plant as a remedy for malaria.

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In Vitro Antiplasmodial Activity and Cytotoxicity of Extracts of Selected Medicinal Plants Used by Traditional Healers of Western Cameroon

Malaria Research and Treatment ◽

10.4061/2011/561342 ◽

2011 ◽

Vol 2011 ◽

pp. 1-6 ◽

Cited By ~ 16

Author(s):

Denis Zofou ◽

Mathieu Tene ◽

Moses N. Ngemenya ◽

Pierre Tane ◽

Vincent P. K. Titanji

Keyword(s):

Lactate Dehydrogenase ◽

Medicinal Plants ◽

Eucalyptus Globulus ◽

Stem Bark ◽

Traditional Healers ◽

Antiplasmodial Activity ◽

Vernonia Amygdalina ◽

Remote Areas ◽

Dacryodes Edulis

Medicinal plants play a key role in malaria control in Africa, especially in remote areas where health facilities are limited. In order to assess their acclaimed potentials, eleven extracts were prepared from seven selected plants commonly used in Western Cameroon, and tested both for their antiplasmodial activity and cytotoxicity. The antiplasmodial activity was assessed using Lactate Dehydrogenase Assay (pLDH) and the cytotoxicity estimated on LLC-MK2 monkey kidney epithelial cells. Seven extracts from five different plants were significantly active, with very weak or no cytotoxicity. The Dacryodes edulis leaves showed the highest activity (IC50 of 6.45 μg/mL on 3D7 and 8.2 μg/mL on DD2) followed by the leaves of Vernonia amygdalina (IC50 of 8.72 and 11.27 μg/mL on 3D7 and DD2 resp.) and roots of V. amygdalina (IC50 of 8.72 μg/mL on 3D7), Coula edulis leaves (IC50 of 13.80 μg/mL and 5.79 μg/mL on 3D7 and DD2 resp.), Eucalyptus globulus leaves (IC50 of 16.80 μg/mL and 26.45 μg/mL on 3D7 and DD2) and Cuviera longiflora stem bark (IC50 of 20.24 μg/mL and 13.91 μg/mL on 3D7 and DD2). These findings justify the use of five of the seven plants in malaria treatment by traditional healers of Western Cameroon.

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Bisindolomonoterpenic alkaloids from the stem bark of Strychnos Nux-Vomica exibiting antiplasmodial activity

Planta Medica ◽

10.1055/s-0032-1320247 ◽

2012 ◽

Vol 78 (11) ◽

Author(s):

MC Jonville ◽

L Angenot ◽

M Tits ◽

M Frédérich

Keyword(s):

Stem Bark ◽

Antiplasmodial Activity

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Crude Extracts of Leaf and Stem Bark of CASSIA SIAMEA have IN VITRO Antimicrobial Activity

Open Journal of Biochemistry ◽

10.15764/bioc.2014.01005 ◽

2014 ◽

Vol 1 (1) ◽

pp. 43-48

Author(s):

Mahmoud Jada ◽

◽

Wurochekke Usman ◽

Muhammad Abdulazeez

Keyword(s):

Antimicrobial Activity ◽

Stem Bark ◽

Cassia Siamea ◽

In Vitro Antimicrobial Activity ◽

Crude Extracts

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New Hybrid Scaffolds Based on Carbazole-Chalcones as Potent Anticancer Agents

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520620666200721110732 ◽

2020 ◽

Vol 20 ◽

Author(s):

Faisal Rashid ◽

Sumera Zaib ◽

Aliya Ibrar ◽

Syeda Abida Ejaz ◽

Aamer Saeed ◽

...

Keyword(s):

Lactate Dehydrogenase ◽

Hela Cells ◽

Cervical Adenocarcinoma ◽

G1 Arrest ◽

Human Breast ◽

Caspase 9 ◽

Flow Cytometric ◽

Pharmacodynamic Profile ◽

Microscopic Studies ◽

Mcf 7

Background and Objectives: Despite various technological advances for the treatment of cancer, the identification of new chemical entities with potent anticancer effects remain an indispensable requirement of the time due to multi-drug resistance exhibited by previously developed anticancer drugs. Particularly, the hybrid drugs incorporating two individual bioactive pharmacophores present medicinally important structural leads, thus improving the pharmacodynamic profile of the drug molecules. The antiproliferative and pro-apoptotic activity of the carbazole-chalcone hybrids on human breast and cervical cancer cells will be examined. Materials and Methods: To overcome such complications, in the current study, we evaluated the cytotoxic effects of carbazole-chalcone hybrids on human breast adenocarcinoma (MCF-7), cervical adenocarcinoma (HeLa) cells and normal cells i.e., baby hamster kidney cells (BHK-21) using MTT (dimethyl-2-thiazolyl-2,5-diphenyl-2H-tetrazolium bromide) assay. The mechanistic studies were performed on potent compound 4g by fluorescent microscopic studies, release of lactate dehydrogenase (LDH) and mitochondrial membrane potential, activation of caspase-9 and -3 and flow cytometric analysis. Results: As revealed by MTT assay, compound 4g was identified as the most potent derivative among the tested series with IC50 values of 5.64 and 29.15 μM against HeLa and MCF-7 cells, respectively. The results were compared with cisplatin. Fluorescent microscopic studies using 4′,6-diamidino-2-phenylindole (DAPI) and propidium iodide (PI) staining confirmed the occurrence of apoptosis in HeLa cells treated with the most active compound 4g. Moreover, compound 4g also triggered the release of lactate dehydrogenase (LDH) in treated HeLa and MCF-7 cells while a luminescence assay displayed a remarkable increase in the activity of caspase-9 and -3. Moreover, flow cytometric results revealed that compound 4g caused G0/G1 arrest in the treated HeLa cells. Conclusion: Our results demonstrated that the compound 4g possesses chemotherapeutic properties against breast cancer and cervical adenocarcinoma cells, thus warranting further research to test the anticancer efficacy of this compound at clinical level.

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Evaluation of Cytotoxic Effects of Dichloromethane Extract of Guduchi (Tinospora cordifolia Miers ex Hook F & THOMS) on Cultured HeLa Cells

Evidence-based Complementary and Alternative Medicine ◽

10.1093/ecam/nel011 ◽

2006 ◽

Vol 3 (2) ◽

pp. 267-272 ◽

Cited By ~ 18

Author(s):

Ganesh Chandra Jagetia ◽

Shaival Kamalaksha Rao

Keyword(s):

Lipid Peroxidation ◽

Lactate Dehydrogenase ◽

Hela Cells ◽

Cytotoxic Effect ◽

Tinospora Cordifolia ◽

Cytotoxic Effects ◽

Optimal Duration ◽

Ldh Release ◽

Gst Activity

Extracts ofTinospora cordifolia(TCE) have been shown to possess anti-tumor properties, but the mechanism of the anti-tumor function of TCE is poorly understood. This investigation elucidates the possible mechanism underlying the cytotoxic effects of dichlormethane extracts of TCE, after selecting optimal duration and concentration for treatment. HeLa cells were exposed to various concentrations of TCE, which has resulted in a concentration-dependent decline in the clonogenicity, glutathione-S-transferase (GST) activity and a concentration-dependent increase in lipid peroxidation (TBARS) with a peak at 4 h and lactate dehydrogenase (LDH) release with a peak at 2 h. Our results suggest that the cytotoxic effect of TCE may be due to lipid peroxidation and release of LDH and decline in GST.

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Scabiosa Genus: A Rich Source of Bioactive Metabolites

Medicines ◽

10.3390/medicines5040110 ◽

2018 ◽

Vol 5 (4) ◽

pp. 110 ◽

Cited By ~ 4

Author(s):

Diana Pinto ◽

Naima Rahmouni ◽

Noureddine Beghidja ◽

Artur Silva

Keyword(s):

Secondary Metabolites ◽

Liver Diseases ◽

Mediterranean Region ◽

Folk Medicine ◽

In Vivo Studies ◽

Bioactive Metabolites ◽

Pentacyclic Triterpenoids ◽

Medical Settings ◽

Plant Names

The genus Scabiosa (family Caprifoliaceae) is considered large (618 scientific plant names of species) although only 62 have accepted Latin binominal names. The majority of the Scabiosa species are widely distributed in the Mediterranean region and some Scabiosa species are used in traditional medicine systems. For instance, Scabiosa columbaria L. is used traditionally against diphtheria while S. comosa Fisch. Ex Roem. and Schult. is used in Mongolian and Tibetan traditional medical settings to treat liver diseases. The richness of Scabiosa species in secondary metabolites such as iridoids, flavonoids and pentacyclic triterpenoids may contribute to its use in folk medicine. Details on the most recent and relevant pharmacological in vivo studies on the bioactive secondary metabolites isolated from Scabiosa species will be summarized and thoroughly discussed.

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ETHNOBOTANICAL, PHYTOCHEMICAL, AND PHARMACOLOGICAL PROPERTIES OF NEPENTHES SPECIES: A REVIEW

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i11.20050 ◽

2017 ◽

Vol 10 (11) ◽

pp. 16 ◽

Cited By ~ 3

Author(s):

Shuaibu Babaji Sanusi ◽

Mohd Fadzelly Abu Bakar ◽

Maryati Mohamed ◽

Siti Fatimah Sabran ◽

Muhammad Murtala Mainasara

Keyword(s):

Folk Medicine ◽

Therapeutic Agents ◽

Bioactive Components ◽

Pharmacological Activities ◽

Crude Extracts ◽

Gastrointestinal Discomfort ◽

Wide Range ◽

Long Time ◽

Phytochemical Compounds ◽

Ethnobotanical Uses

The genus Nepenthes (Nepenthaceae) has been utilized in folk medicine for a long time in India and Southeast Asia countries. They are used in the treatment of leprosy, cholera, night blindness, gastrointestinal discomfort, dysentery, stomachache, and bed-wetting among others. This review highlights the ethnobotanical uses, phytochemicals, and pharmacological activities of both crude extracts and pure bioactive compounds of Nepenthes spp. The phytochemical compounds isolated from Nepenthes species include flavonoids, terpenoids, tannins, alkaloids, and steroids among other phytochemicals. A wide range of pharmacological activities was exhibited by the crude extracts and pure bioactive components such as antibacterial, antifungal, antimalarial antioxidant, antidiabetic, antiosteoporotic, anti-inflammatory, cytotoxicity, and hypolipidemic activities. This review revealed that many active compounds are present in Nepenthes spp. However, many pharmacological screenings such as anticancer, antiviral, wound healing, antihelminthic, antidiarrheal properties, among others have not been carried out yet. Therefore, more biological investigations and phytochemical screenings are required to fully explore the genus Nepenthes which may lead to development of new therapeutic agents.

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