Crude Ethanolic Stem Bark Extract of Zanthoxylum zanthoxyloides and Its Fractions: In-Vitro and In-Vivo Antiplasmodial Activity

Malaria is a global problem, as treatment failure has hampered the efficacy of most anti-malarial medications. The goal of this study was to see if stem bark extract from Zanthoxylum zanthoxyloides had antiplasmodial properties that could be used to treat both susceptible and resistant parasites. The stem bark of Z. zanthoxyloides (500g) was crushed and extracted with ethanol. The extract was tested for antiplasmodial activity in vitro against the chloroquine-sensitive (CQS) strain NF54 and chloroquine-resistant strains (CQR) K1 of P. falciparum, as well as in vivo against the CQS(NK65) strain of P. berghei at 100, 200, and 400 mg/kg bw. Bioassay-guided fractionation of the extract was performed. The crude extract had an in vitro activity of 1076.4 56.4 and 1315.1 121.6 ng/ml against chloroquine sensitive and resistant parasites, respectively while standard drugs (chloroquine and artesunate) were 10.94 nM (3478.92 ng/ml) and 9.24 nM (3215.52ng/ml) for CQS and 310.68 nM (98796 ng/ml) and 10.94 nM (3650.52 ng/ml) for CQR respectively. At Day 7, mice treated with 100, 200, and 400 mg/kg bw crude extract had parasite densities of 1159, 928, and 869 parasites/ µl, respectively (compared to positive control that had 123 parasites /µl). In vitro antiplasmodial activity was best in the K2, K4, and K6 fractions (IC50 were 6670, 6890, and 6480 ng/ml), but in vivo antiplasmodial activity was best in the K4 fraction (1183 parasites/ µl).The stem bark extract of Z. zanthoxyloides have remarkable antiplasmodial activity against both chloroquine sensitive and drug resistant P. falciparum supporting it ethnomedicinal use in malaria treatment.The extract of Z. zanthoxyloides has promising antiplasmodial activity and could be used to generate therapeutic leads against the multidrug-resistant K1 strain of P. falciparum, in addition to providing an alternative allopathic antiplasmodial medication.

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ANTI-INFLAMMATORY ACTIVITY OF KNEMA ATTENUATA (HOOK. F. AND THOMSON) WARB ETHANOLIC STEM BARK EXTRACT IN ALBINO WISTAR RATS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i4.30500 ◽

2019 ◽

pp. 330-334

Author(s):

SUPRIYA RAJA H

Keyword(s):

Stem Bark ◽

Inflammatory Activity ◽

Assay Method ◽

Bark Extract ◽

Raw 264.7 ◽

Myeloperoxidase Activity ◽

Stem Bark Extract ◽

Anti Inflammatory

Objective: Knema attenuata (Myristicaceae), popularly known as “wild nutmeg,” is an endemic tree species from Western Ghats, which has been used in folk medicine. Conventionally, the stem bark of K. attenuata is used for treating inflammatory conditions without any scientific information available for the same. The present study was undertaken to evaluate the anti-inflammatory activity of the ethanolic stem bark extract (ESBE) of K. attenuata using in vivo and in vitro screening models. Methods: The ethanolic extract of stem bark was prepared by soxhlation, and its cytotoxicity in RAW 264.7 cell line was assessed using MTT assay method. In vivo anti-inflammatory effect of extract was estimated in rats using carrageenan-induced paw edema model and cotton pellet-induced granuloma model. The in vitro anti-inflammatory activity of the extract was evaluated by cyclooxygenase and lipoxygenase inhibition assay, estimation of myeloperoxidase activity, and determination of cellular nitrite levels in lipopolysaccharide-stimulated RAW 264.7 macrophage cells. Results: Toxic symptoms were not observed for the ESBE. The extract demonstrated significant anti-inflammatory activity in both in vivo and in vitro models. The anti-inflammatory action exhibited by the extract was a result of the inhibition of leukocyte migration and nitric oxide pathway and partially by inhibition of mediators such as prostaglandins and leukotrienes. Conclusion: Findings from the study provide the evidence for the popular use of stem bark extract of K. attenuata as a potential anti-inflammatory agent.

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

Journal of Parasitology Research ◽

10.1155/2020/4580526 ◽

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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In vitro antiplasmodial activity, cytotoxicity, antioxidant action and GC-FID analysis of Allanblackia floribunda Oliv

SN Applied Sciences ◽

10.1007/s42452-021-04812-0 ◽

2021 ◽

Vol 3 (10) ◽

Author(s):

Francis Irabor ◽

Osamudiamen Ebohon ◽

Nekpen Erhunse ◽

Osariemen T. Okugbo ◽

Ehimwenma S. Omoregie

Keyword(s):

Cell Line ◽

Normal Cell ◽

Leaf Extract ◽

Stem Bark ◽

Antiplasmodial Activity ◽

Bark Extract ◽

Active Fraction ◽

Vero Cell Line ◽

Stem Bark Extract

Abstract This study evaluated the in vitro antiplasmodial efficacy and cytotoxicity of Allanbackia floribunda stem bark extract, leaf extract and oil. It also assessed the phytochemical compositions and antioxidant action of the stem bark fractions as well as the phytochemical fingerprint of the most active fraction (dichloromethane). Trager and Jensen method was used to culture Plasmodium falciparum, Mark III test developed by WHO was used to assess the antiplasmodial activity of the plant’s crude extract and fractions against the ring stage of P. falciparum strain, Pf3D7. Cytotoxicity was determined against Vero cell line using microculture tetrazolium (MTT) test. Gas chromatography with flame ionization detection (GC-FID) was employed to identify phytochemical fingerprint of the most active fraction. The stem bark extract had better antiplasmodial activity (IC50Pf3D7 of 4.3 ± 0.17 μg/mL) compared with the leaf extract (IC50Pf3D7, 8.0 ± 0.28 μg/mL) and oil (IC50Pf3D7 > 100 μg/mL). Both the leaf and stem bark extracts were found to be non-cytotoxic compared with the standard cytotoxic drug, doxorubicin. The selectivity indices (S.I.) of the extracts against the parasite were 20.06 and 8.85 for the stem bark and leaf respectively. Dichloromethane fraction had the highest inhibition against the P. falciparum parasite with IC50Pf3D7 of 1.51 μg/ mL. GC-FID analysis showed high presence antiplasmodial flavonoids and terpenes. This investigation confirmed that A. floribunda stem bark has potent activity against P. falciparum, and it is relatively safe to normal cell. Article Highlights Allanblackia floribunda methanol stem bark and leaf extracts could inhibit the growth of chloroquine sensitive Plasmodium falciparum (Pf3D7) in vitro. The stem bark infusion of Allanblackia floribunda was found to be nontoxic and safe at moderate doses to normal cell line (Vero cell line). Dichloromethane fraction of the stem bark showed excellent inhibition against chloroquine sensitive malaria parasite.

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In Vitro Antiplasmodial Activity, Cytotoxicity, Antioxidant Action and GC-FID Analysis of Allanblackia Floribunda Extracts

10.21203/rs.3.rs-32060/v1 ◽

2020 ◽

Author(s):

Francis Irabor ◽

Osamudiamen Ebohon ◽

Nekpen Erhunse ◽

Osariemen Tinu Okugbo ◽

Ehimwenma Sheena Omoregie

Keyword(s):

Plasmodium Falciparum ◽

Stem Bark ◽

Antiplasmodial Activity ◽

Bark Extract ◽

Complete Medium ◽

Active Fraction ◽

Bioactive Constituents ◽

Vero Cell Line ◽

Stem Bark Extract

Abstract Background: Malaria is a disease that is caused by Plasmodium parasite that has resulted in death of so many persons in the world especially children below 5 years. Plasmodium falciparum is one of the most widespread etiological agent for human malaria and has become increasingly resistant to standard antimalarial drugs. This study was therefore aimed at evaluating the in vitro antiplasmodial efficacy and cytotoxicity of Allanbackia floribunda stem bark, leaf and oil. Methods: Trager and Jensen method was used to culture Plasmodium falciparum and maintained in fresh O + human erythrocytes at 3% hematocrit in complete medium (Roswell Park Memorial Institute-RPMI 1640). Mark III test developed by WHO was used to assess the antiplasmodial activity of the plant’s crude extract and fractions against the ring stage of P. falciparum strains Pf3D7. Cytotoxicity was determined against Vero cell line using microculture tetrazolium (MTT). GC-FID was employed to identify bioactive constituents in the most active fraction. Results: The plant extracts showed varied degrees of inhibition of parasitaemia with IC 50Pf3D7 values ranging between 4.0 to 1000 μg/ mL. The methanol stem bark extract of A. floribunda exhibited very active antiplasmodial activity (IC 50Pf3D7 = 4.3 ± 0.17μg / mL), the leaf extract showed active antiplasmodial activity (IC 50Pf3D7 = 8.0 ± 0.28 μg / mL) while the oil extract was inactive against the parasite (IC 50 > 100 μg / mL). Both the leaf and stem bark extracts were found to be non-cytotoxic in contrast to the standard cytotoxic drug, doxorubicin. The selectivity indices (S.I.) of the extracts against the parasites were 13.32 and 8.18 for the stem bark and leaf, respectively. Among the stem bark fractions, dichloromethane (DCM) had the best inhibition against the P. falciparum parasite (DCM IC 50Pf3D7 of 1.51 μg/ mL) and was closely followed by the hydromethanol (HMet) fraction (HMet IC 50Pf3D7 of 5.0 μg/ mL) while that of ethylacetate (EAct) and hexane (Hxn) fractions were almost similar (IC 50 Pf3D7 of 6 and 6.25 μg/ mL, respectively).GC-FID analysis of the most active fraction, DCM, showed high presence antiplasmodial flavonoids (naringenin, luteolin, kaemferor and myricetin) and terpenes (α-pinene and β-caryophyllene) which may have been responsible for the excellent antiplasmodial action of the most active fraction. Conclusion: This investigation confirmed that A. floribunda stem bark has potent activity against P. falciparum and it is relatively safe to normal cell. The antiplasmodial action is credited to the presence of bioactive flavonoids and terpenes that may have acted singly or synergistically.

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AKTIVITAS INHIBISI ENZIM ALFA-GLUKOSIDASE DARI EKSTRAK KULIT BATANG BUNGA KUPU-KUPU (Bauhinia semibifida Roxb) SECARA IN VITRO

Jurnal Ilmiah Ibnu Sina (JIIS): Ilmu Farmasi dan Kesehatan ◽

10.36387/jiis.v6i2.701 ◽

2021 ◽

Vol 6 (2) ◽

pp. 223-231

Author(s):

Haiyul Fadhli ◽

◽

Nofri Hendri Sandi ◽

Ainun Nurain Nurdin

Keyword(s):

Ethyl Acetate ◽

Inhibitory Activity ◽

Stem Bark ◽

Positive Control ◽

Bark Extract ◽

In Vitro Testing ◽

Ic50 Value ◽

Microplate Reader ◽

Stem Bark Extract

Research on the activity of ?-glucosidase inhibition of Bunga Kupu-Kupu stem bark extract (Bauhinia semibifida Roxb) has been carried out in vitro. This study aims to determine the inhibitory activity of the extracts of B. semibifida Roxb. stem bark against the ?-glucosidase enzyme in vitro. Testing the inhibitory activity of the ?-glucosidase enzyme using extracts of n-hexane, ethyl acetate, and methanol from the stem bark of the Bunga Kupu-Kupu and the Akarbose as a positive control. In vitro testing was carried out using a microplate reader instrument with a wavelength of 410 nm. The results showed that the extract of n-hexane extract of the B. semibifida stem bark had an IC50 value 15,625 µg/mL, ethyl acetate extract had an IC50 value 35,495 µg/mL, and the methanol extract had an IC50 value 34,279 µg/mL. By category, the three B. semibifida stem bark extracts have the active ability to inhibit the ?-glucosidase enzyme, while the Akarbose had an IC50 value 0,384 µg/mL as a positive control has a very active ability as an antidiabetic through the inhibition of the ?-glucosidase enzyme. The results showed that extraction of ?-glucosidase inhibitor compound with n-hexane yielded extract with highest inhibitor activity.

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Evaluation of toxicity of Calophyllum brasiliense stem bark extract by in vivo and in vitro assays

Journal of Ethnopharmacology ◽

10.1016/j.jep.2014.06.019 ◽

2014 ◽

Vol 155 (1) ◽

pp. 30-38 ◽

Cited By ~ 10

Author(s):

Mariana Canevari Oliveira ◽

Larissa Maria Scalon Lemos ◽

Ruberlei Godinho de Oliveira ◽

Evandro Luiz Dall׳Oglio ◽

Paulo Teixeira de Sousa Júnior ◽

...

Keyword(s):

Stem Bark ◽

In Vitro Assays ◽

Bark Extract ◽

Calophyllum Brasiliense ◽

Stem Bark Extract

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

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/4169397 ◽

2018 ◽

Vol 2018 ◽

pp. 1-7 ◽

Cited By ~ 6

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.

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