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NOT Open Access | Integrating network pharmacology and experimental models to investigate the mechanisms of dihydroartemisinin in preventing NSCLC progression via mTOR/HIF-1α signaling

August 17, 2021 - 14:18 -- NOT Open Access
Li Y, Xiao X, Wang H, Zhou Q, Jin Z, Zhang Y, Wang Y, Yue F, Zhou S, Yang J
Eur J Pharmacol. 2021 Aug 11:174411

Advanced Non-small cell lung cancer (NSCLC) is the most common type of lung cancer with a poor prognosis. The anti-malaria compounds dihydroartemisinin (DHA) have shown to regulate multiple targets and signaling pathways in cancers, but a global view of its mechanism of action remains elusive. In present study, we integrated network pharmacology and in vitro and in vivo experimental models to investigate the mechanisms of DHA in preventing NSCLC proliferation.

Toward New Transmission-Blocking Combination Therapies: Pharmacokinetics of 10-Amino-Artemisinins and 11-Aza-Artemisinin and Comparison with Dihydroartemisinin and Artemether

August 4, 2021 - 16:26 -- Open Access
Daniel J Watson, Lizahn Laing, Liezl Gibhard, Ho Ning Wong, Richard K Haynes, Lubbe Wiesner
Antimicrob Agents Chemother. 2021 Jul 16;65(8):e0099021

As artemisinin combination therapies (ACTs) are compromised by resistance, we are evaluating triple combination therapies (TACTs) comprising an amino-artemisinin, a redox drug, and a third drug with a different mode of action. Thus, here we briefly review efficacy data on artemisone, artemiside, other amino-artemisinins, and 11-aza-artemisinin and conduct absorption, distribution, and metabolism and excretion (ADME) profiling in vitro and pharmacokinetic (PK) profiling in vivo via intravenous (i.v.) and oral (p.o.) administration to mice.

Not Open Access | Murine pharmacokinetics and antimalarial pharmacodynamics of dihydroartemisinin trimer self-assembled nanoparticles

July 20, 2021 - 14:30 -- NOT Open Access
Guo W, Li N, Ren G, Wang R, Chai L, Li Y, Wang X, Yang Q, Wang R, Zhang G, Yang L, Yi B, Zhang S
Parasitol Res. 2021 Jul 17

Currently, conjugation of artemisinin-derived dimers, trimers, and tetramers is a viable strategy for developing new effective antimalarial candidates. Furthermore, nanotechnology is an effective means to achieve intravenous administration of hydrophobic drugs. In this paper, an ester-linked dihydroartemisinin trimer (DHA3) was synthesized and further prepared as self-assembled nanoparticles (DHA3NPs) by a one-step nanoprecipitation method. The pharmacokinetics and antimalarial pharmacodynamics of DHA3NPs were studied in rats and mice infected with Plasmodium yoelii BY265 (PyBY265). DHA3NPs had a regular spherical shape with a uniform size distribution of 140.27 ± 3.59 nm, entrapment efficiency (EE) of 99.63 ± 0.17%, and drug loading efficiency (DL) of 79.62 ± 0.11%.

Effect of α-tocopheryloxy acetic acid, a vitamin E derivative mitocan, on the experimental infection of mice with Plasmodium yoelii

June 30, 2021 - 12:17 -- Open Access
Kasumi Kawamura, Aiko Kume, Rika Umemiya-Shirafuji, Shunji Kasai and Hiroshi Suzuki
Malaria Journal 2021 20:280, 24 June 2021

Malaria parasites are known to be vulnerable to oxidative stress. In this study, the effects of the administration of α-tocopheryloxy acetic acid (α-TEA), which is a vitamin E analogue mitocan, on Plasmodium yoelii infection in mice were examined.

Restructured Mitochondrial-Nuclear Interaction in Plasmodium falciparum Dormancy and Persister Survival after Artemisinin Exposure

June 1, 2021 - 15:38 -- Open Access
Connelly SV, Manzella-Lapeira J, Levine ZC, Brzostowski J, Krymskaya L, Rahman RS, Ellis AC, Amin SN, Sá JM, Wellems TE
mBio. 2021 May 28:e0075321

Artemisinin and its semisynthetic derivatives (ART) are fast acting, potent antimalarials; however, their use in malaria treatment is frequently confounded by recrudescences from bloodstream Plasmodium parasites that enter into and later reactivate from a dormant persister state. Here, we provide evidence that the mitochondria of dihydroartemisinin (DHA)-exposed persisters are dramatically altered and enlarged relative to the mitochondria of young, actively replicating ring forms. Restructured mitochondrial-nuclear associations and an altered metabolic state are consistent with stress from reactive oxygen species.

Not Open Access | Dihydroartemisinin alleviates skin fibrosis and endothelial dysfunction in bleomycin-induced skin fibrosis models

May 25, 2021 - 14:59 -- NOT Open Access
Li R, Yin H, Wang J, He D, Yan Q, Lu L
Clin Rheumatol. 2021 May 19

The present study was to investigate whether dihydroartemisinin (DHA), which is a highly effective and safe drug in the treatment of malaria, could be repurposed for the treatment of skin fibrosis and vascular dysfunction in systemic sclerosis (SSc).

NOT Open Access | In Vitro Susceptibility of Plasmodium falciparum Isolates from the China-Myanmar Border Area to Piperaquine and Association with Candidate Markers

March 13, 2021 - 16:31 -- NOT Open Access
Si Y, Zeng W, Cui L, et al.
Antimicrob Agents Chemother. 2021 Mar 8:AAC.02305-20

Plasmodium falciparum from the Greater Mekong subregion has evolved resistance to the artemisinin-based combination therapy dihydroartemisinin and the partner drug piperaquine. To monitor the potential westward spread or independent evolution of piperaquine resistance, we evaluated the in vitro susceptibility of 120 P. falciparum isolates collected at the China-Myanmar border during 2007-2016.

Artesunate and Dihydroartemisinin Inhibit Rabies Virus Replication

March 10, 2021 - 13:29 -- Open Access
Luo J, Zhang Y, Wang Y, Liu Q, Li J, He H, Luo Y, Huang S, Guo X
Virol Sin. 2021 Mar 4:1-9

Rabies is caused by infection of rabies virus (RABV) and remains a serious threat to the global public health. Except for the requirement for cold chain and high cost of human rabies immune globulin, no small molecule drugs are currently available for clinical treatment of rabies. So, it is of great importance to identify novel compounds that can effectively inhibit RABV infection. Artesunate (ART) and dihydroartemisinin (DHA), two derivatives of artemisinin, are widely used for treatment of malaria in adults and children, showing high safety. In this study, we found that both ART and DHA were able to inhibit RABV replication in host cells at a low concentration (0.1 μmol/L).

Effect of Body Weight and Age on the Pharmacokinetics of Dihydroartemisinin: FDA Basis for Dose Determination of Artesunate for Injection in Pediatric Patients with Severe Malaria

February 23, 2021 - 12:48 -- Open Access
Kitabi E, Bensman TJ, Earp JC, Chilukuri DM, Smith H, Ball L, O'Shaughnessy E, Yasinskaya Y, Colangelo PM, Reynolds KS
Clin Infect Dis. 2021 Feb 19:ciab149

For treatment of severe malaria, the WHO recommends 3 mg/kg intravenous artesunate in pediatric patients weighing less than 20 kg.

NOT Open Access | Dihydroartemisinin, an active metabolite of artemisinin, interferes with Leishmania braziliensis mitochondrial bioenergetics and survival

January 12, 2021 - 14:55 -- NOT Open Access
Grazzia N, Boaventura S Jr, Garcia VL, Gadelha FR, Miguel DC
Parasitol Res. 2021 Jan 8

Leishmaniasis is one of the most neglected parasitic infections of the world and current therapeutic options show several limitations. In the search for more effective drugs, plant compounds represent a powerful natural source. Artemisinin is a sesquiterpene lactone extracted from Artemisia annua L. leaves, from which dihydroartemisinin (DQHS) and artesunic acid (AA)/artesunate are examples of active derivatives.


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