artemisinin

Dried Leaf Artemisia Annua Improves Bioavailability of Artemisinin via Cytochrome P450 Inhibition and Enhances Artemisinin Efficacy Downstream

Tags:

artemisia annua, artemisinin, artemisinin efficacy

Author(s):

Desrosiers MR, Mittelman A, Weathers PJ

Reference:

Biomolecules. 2020 Feb 7;10(2). pii: E254

Artemisia annua L. and artemisinin, have been used for millennia to treat malaria. We used human liver microsomes (HLM) and rats to compare hepatic metabolism, tissue distribution, and inflammation attenuation by dried leaves of A. annua (DLA) and pure artemisinin. For HLM assays, extracts, teas, and phytochemicals from DLA were tested and IC50 values for CYP2B6 and CYP3A4 were measured.

Synthesis of [3,3-2H2]-Dihydroartemisinic Acid to Measure the Rate of Nonenzymatic Conversion of Dihydroartemisinic Acid to Artemisinin

Tags:

Dihydroartemisinic Acid, Nonenzymatic Conversion, artemisinin

Author(s):

Varela K, Arman HD, Yoshimoto FK

Reference:

J. Nat. Prod. 2019, Dec 20.

Dihydroartemisinic acid is the biosynthetic precursor to artemisinin, the endoperoxide-containing natural product used to treat malaria. The conversion of dihydroartemisinic acid to artemisinin is a cascade reaction that involves C–C bond cleavage, hydroperoxide incorporation, and polycyclization to form the endoperoxide. Whether or not this reaction is enzymatically controlled has been controversial.

NOT Open Access | Oligomers of carrageenan regulate functional activities and artemisinin production in Artemisia annua L. exposed to arsenic stress

Tags:

Oligomers, carrageenan, artemisinin, artemisia annua L, arsenic stress

Author(s):

Naeem M, Nabi A, Aftab T, Khan MMA

Reference:

Protoplasma, 2019 Dec 24

Recently, a promising technique has come forward in field of radiation-agriculture in which the natural polysaccharides are modified into useful oligomers after depolymerization. Ionizing radiation technology is a simple, pioneering, eco-friendly, and single step degradation process which is used in exploiting the efficiency of the natural polysaccharides as plant growth promoters. Arsenic (As) is a noxious and toxic to growth and development of medicinal plants. Artemisinin is obtained from the leaves of Artemisia annua L., which is effective in the treatment of malaria.

NOT Open Access | Modification of pfap2μ and pfubp1 Markedly Reduces Ring-Stage Susceptibility of Plasmodium falciparum to Artemisinin In Vitro

Tags:

pfap2μ, pfubp1, plasmodium falciparum, artemisinin, in vitro

Author(s):

Henrici RC, van Schalkwyk DA, Sutherland CJ

Reference:

Antimicrob Agents Chemother. 2019 Dec 20;64(1). pii: e01542-19

Management of uncomplicated malaria worldwide is threatened by the emergence in Asia of Plasmodium falciparum carrying variants of the pfk13 locus and exhibiting reduced susceptibility to artemisinin. Mutations in two other genes, ubp1 and ap2μ, are associated with artemisinin resistance in rodent malaria and with clinical failure of combination therapy in African malaria patients. Transgenic P. falciparum clones, each carrying orthologues of mutations in pfap2μ and pfubp1 associated with artemisinin resistance in Plasmodium chabaudi, were derived by Cas9 gene editing.

NOT Open Access | Activation of Artemisinin and Heme Degradation in Leishmania tarentolae Promastigotes: A Possible Link

Tags:

Leishmania, artemisinin, endoperoxide, radicals, heme

Author(s):

Geroldinger G, Tonner M, Gille L, et al.

Reference:

Biochem Pharmacol. 2019 Nov 28:113737

Endoperoxides (EPs) appear to be promising drug candidates against protozoal diseases, including malaria and leishmaniasis. Previous studies have shown that these drugs need an intracellular activation to exert their pharmacological potential. The efficiency of these drugs is linked to the extensive iron demand of these intracellular protozoal parasites.

Protective mechanism of artemisinin on rat bone marrow-derived mesenchymal stem cells against apoptosis induced by hydrogen peroxide via activation of c-Raf-Erk1/2-p90rsk-CREB pathway

Tags:

malaria, artemisinin, plasmodium falciparum

Author(s):

Jiankang Fang, Xia Zhao, Shuai Li, Xingan Xing, Haitao Wang, Philip Lazarovici & Wenhua Zheng

Reference:

Stem Cell Research & Therapy volume 10, Article number: 312 (2019)

These studies demonstrate the proof of concept of artemisinin therapeutic potential to improve survival in vitro of BMSCs exposed to ROS-induced apoptosis and suggest that artemisinin-mediated protection occurs via the activation of c-Raf-Erk1/2-p90rsk-CREB signaling pathway.

Not Open Access | Unconventional secretory pathway activation restores hair cell mechanotransduction in an USH3A model

Tags:

artemisinin

Author(s):

Suhasini R. Gopal, Yvonne T. Lee, Ruben Stepanyan, Brian M. McDermott Jr., and Kumar N. Alagramam

Reference:

PNAS May 28, 2019 116 (22) 11000-11009

The pathogenic variant c.144T>G (p.N48K) in the clarin1 gene (CLRN1) results in progressive loss of vision and hearing in Usher syndrome IIIA (USH3A) patients.

NOT Open Access | Combination of artemisinin-based natural compounds from Artemisia annua L. for the treatment of malaria: Pharmacodynamic and pharmacokinetic studies

Tags:

malaria, plasmodium, artemisinin

Author(s):

Jing Li, Chao Zhang, Muxin Gong and Manyuan Wang

Reference:

Phytotherapy Research banner Volume32, Issue7 July 2018 Pages 1415-1420

Currently, the most effective antimalarial is artemisinin, which is extracted from the leaves of medicinal herb Artemisia annua L. (A. annua).

Medical Treatment:

antimalarials

An optimised age-based dosing regimen for single low-dose primaquine for blocking malaria transmission in Cambodia

Tags:

malaria, artemisinin, plasmodium, falciparum

Author(s):

Leang R, Khu N, Mukaka M, Debackere M, Tripura R, Kheang S, Chy S, Kak N, Buchy P, Tarantola A, Menard D, Roca-Felterer A, Fairhurst R, Kheng S, Muth S, Ngak S, Dondorp A, White N, Taylor W

Reference:

BMC Medicine 2016, 14 :171 (27 October 2016)

In 2012, the World Health Organization recommended the addition of single low-dose primaquine (SLDPQ, 0.25 mg base/kg body weight) to artemisinin combination therapies to block the transmission of Plasmodium falciparum without testing for glucose-6-phosphate dehydrogenase deficiency.

Clinical and molecular surveillance of artemisinin resistant falciparum malaria in Myanmar (2009–2013)

Tags:

falciparum, malaria, artemisinin

Author(s):

Myat Htut Nyunt, Myat Thu Soe, Hla Win Myint, Htet Wai Oo, Moe Moe Aye, Soe Soe Han, Ni Ni Zaw, Cho Cho, Phyo Zaw Aung, Khin Thiri Kyaw, Thin Thin Aye, Naychi Aung San, Leonard Ortega, Krongthong Thimasarn, Maria Dorina G. Bustos, Sherwin Galit…

Reference:

Malaria Journal 2017 16:333, 14 August 2017

Apart from k13, pfarps10, pffd and pfmdr2 are also useful for molecular surveillance of artemisinin resistance especially where k13 mutation has not been reported.

Medical Treatment:

artemisinin-based combination therapy (ACT)

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