In vitro and ex vivo activity of an Azadirachta indica A.Juss. seed kernel extract on early sporogonic development of Plasmodium in comparison with azadirachtin A, its most abundant constituent

Dahiya, Nisha; Chianese, Giuseppina; Abay, Solomón Mequanente; Taglialatela‐Scafati, Orazio; Esposito, Fulvio; Lupidi, Giulio; Bramucci, Massimo; Quassinti, Luana; Christophides, George K.; Habluetzel, Annette; Lucantoni, Leonardo

doi:10.1016/j.phymed.2016.10.019

Cited by 19 publications

(15 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This plant is indigenous to South Asia and abundant in the tropical belt [6]. The plant has been reported to have anti-hyperglycaemic, antibacterial [7], antifungal, anthelmintic [8], antioxidant, anti-inflammatory and antimalarial [9] activities. The plant has been reported to contain diterpenoids, triterpenoids, alkaloids, flavonoids and phenolic compounds [10].…”

Section: Introductionmentioning

confidence: 99%

In vivo Antimalarial Activities of Five Ugandan Medicinal Plants on Plasmodium berghei in Mice

Ajayi

Elujoba

Okella

et al. 2020

EJMP

View full text Add to dashboard Cite

Aim: Medicinal plants have played an important role in the treatment of different ailments including malaria in developing countries particularly in Africa. This study has evaluated the antimalarial activities of Azadirachta indica A. Juss (Meliaceae), Cymbopogon citratus Stapf. (Poaceae), Moringa oleifera Lam. (Moringaceae), Tithonia diversifolia (Hemsl) A. Grey (Asteraceae) and Vernonia amygdalina Del. (Asteraceae) which are commonly-used for malaria treatment in Uganda. Study Design: This is an experimental laboratory report on antimalarial activities of some Ugandan medicinal plants for subsequent profiling in an herbal pharmacopoeia and eventual drug development. Place and Duration of Study: The Animal Research Facility and the Clinical and Research Laboratory, Faculty of Medicine, Mbarara University of Science and Technology, Uganda, between July 2019 and March 2020. Methodology: The antimalarial activity of the hot infusion of each leaf was evaluated on chloroquine-sensitive Plasmodium berghei ANKA-infected mice using 4-day test at 100 – 400 mg/kg with chloroquine (10 mg/kg) and artemether-lumefantrine (4 mg/kg) as positive controls; and distilled water as negative control. The observed haematological responses of the animals were determined with an automated haematometer. Results: The results showed dose-dependent activities in the animals treated with the extract of each plant leaf in varying degrees. Thus, V. amygdalina and T. diversifolia showed the highest antimalarial activities with the chemosuppression values of 75% and 66% at 400 mg/kg, respectively. The results of V. amygdalina, T. diversifolia and M. oleifera, extracts gave the lowest ED50 of 141, 195 and 231 mg/kg, respectively being significantly different from A. indica (ED50 319 mg/kg) and C. citratus (ED50 346 mg/kg) with V. amygdalina as the most potent extract among the five plant leaves. Conclusion: The observed activities of the five plants have therefore supported their folkloric uses as antimalarial remedies by the Ugandan traditional medicine practitioners with obvious potentials for drug development.

show abstract

Section: Introductionmentioning

confidence: 99%

In vivo Antimalarial Activities of Five Ugandan Medicinal Plants on Plasmodium berghei in Mice

Ajayi

Elujoba

Okella

et al. 2020

EJMP

View full text Add to dashboard Cite

show abstract

“…The latter two, isolated from Azadirachta indica fruits, inhibit Plasmodium falciparum (W2 chloroquine-resistant strain) schizogonic replication by 50% at a concentration lower than 2 μM [11]. Azadirachtin—not active against blood stages—was found to interfere with early sporogonic development in the mosquito vector [12, 13], inhibiting 50% of ookinete formation in vitro at about 17 µM [14].…”

Section: Introductionmentioning

confidence: 99%

Effects of Azadirachta indica seed kernel extracts on early erythrocytic schizogony of Plasmodium berghei and pro-inflammatory response in inbred mice

Habluetzel

Pinto

Tapanelli

et al. 2019

Malar J

Self Cite

View full text Add to dashboard Cite

BackgroundMedicinal plant research may contribute to develop new pharmacological control tools for vector borne diseases, such as malaria.MethodsThe effects of methanol extracts (ME) obtained from seed kernel of ripe and unripe Azadirachta indica fruits were studied on erythrocytic proliferation of the rodent malaria parasite Plasmodium berghei strain ANKA and on mice pro-inflammatory response, as evaluated by measuring the matrix-metalloproteinase-9 (MMP-9) and tumour necrosis factor (TNF) plasma levels, in two mouse strains (C57BL/6 and BALB/c) which are considered as prototypical of Th1 and Th2 immune response, respectively.ResultsME obtained from seed kernel of unripe Azadirachta indica fruits decreased by about 30% the proportion of erythrocytes infected with the malaria parasite in C57BL/6 mice in the 4 days suppressive test. In this treatment group, MMP-9 and TNF levels were notably higher than those measured in the same mouse strain treated with the anti-malarial drug artesunate, Azadirachta indica kernel extracts from ripe fruits or solvent. In BALB/c mice, treatment with kernel extracts did not influence parasitaemia. MMP-9 and TNF levels measured in this mouse strain were notably lower than those recorded in C57BL/6 mice and did not vary among treatment groups.ConclusionsThe effects of the ME on the parasite-host interactions appeared to be mouse strain-dependent, but also related to the ripening stage of the neem fruits, as only the unripe fruit seed kernel extracts displayed appreciable bioactivity.Electronic supplementary materialThe online version of this article (10.1186/s12936-019-2671-8) contains supplementary material, which is available to authorized users.

show abstract

“…Structure-activity relationship analysis showed that the hemi-acetal moiety on carbon-11 to be critical for the observed pharmacological effect of these compounds. Azadirachtin A additionally inhibits exflagellation of gametes ex vivo and blocks development of ESS [88]. The MoA of azadirachtin A has been elucidated to be an impairment of microtubules formation during exflagellation [90].…”

Section: Mycotoxinsmentioning

confidence: 99%

“…Azadirachta indica (Meliaceae), the neem tree native to India where it has been used for >3500 years for malaria treatment, has been comprehensively studied for its transmission-blocking activity [ 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 ]. A. indica fractions are active in vitro against both early- and late-stage P. falciparum gametocytes (IC 50 = 0.001 µg/mL) [ 85 , 87 ].…”

Section: Effectiveness Of Natural Products Against Transmission-blmentioning

confidence: 99%

Natural Products: A Potential Source of Malaria Transmission Blocking Drugs?

et al. 2020

View full text Add to dashboard Cite

The ability to block human-to-mosquito and mosquito-to-human transmission of Plasmodium parasites is fundamental to accomplish the ambitious goal of malaria elimination. The WHO currently recommends only primaquine as a transmission-blocking drug but its use is severely restricted by toxicity in some populations. New, safe and clinically effective transmission-blocking drugs therefore need to be discovered. While natural products have been extensively investigated for the development of chemotherapeutic antimalarial agents, their potential use as transmission-blocking drugs is comparatively poorly explored. Here, we provide a comprehensive summary of the activities of natural products (and their derivatives) of plant and microbial origins against sexual stages of Plasmodium parasites and the Anopheles mosquito vector. We identify the prevailing challenges and opportunities and suggest how these can be mitigated and/or exploited in an endeavor to expedite transmission-blocking drug discovery efforts from natural products.

show abstract

In vitro and ex vivo activity of an Azadirachta indica A.Juss. seed kernel extract on early sporogonic development of Plasmodium in comparison with azadirachtin A, its most abundant constituent

Cited by 19 publications

References 28 publications

In vivo Antimalarial Activities of Five Ugandan Medicinal Plants on Plasmodium berghei in Mice

In vivo Antimalarial Activities of Five Ugandan Medicinal Plants on Plasmodium berghei in Mice

Effects of Azadirachta indica seed kernel extracts on early erythrocytic schizogony of Plasmodium berghei and pro-inflammatory response in inbred mice

Natural Products: A Potential Source of Malaria Transmission Blocking Drugs?

Contact Info

Product

Resources

About