Synthesis and Characterization of Dimeric Artesunate Glycerol Monocaprylate Conjugate and Formulation of Nanoemulsion Preconcentrate DOI Creative Commons
Rana Hore, Nazmul Hasan,

Karsten Mäder

et al.

Molecules, Journal Year: 2023, Volume and Issue: 28(13), P. 5208 - 5208

Published: July 4, 2023

Malaria is one of the major life-threatening health problems worldwide. Artesunate most potent antimalarial drug to combat severe malaria. However, development resistance, short plasma half-life, and poor bioavailability limit efficacy this drug. Here, we applied dimerization concept synthesize dimeric artesunate glycerol monocaprylate conjugate (D-AS-GC) by conjugating (AS) with (GC) via esterification reaction. D-AS-GC conjugate, AS, GC were well characterized 1H NMR, attached proton test (APT) 13C NMR 2D spectroscopy. was further analyzed ESI-TOF MS. Finally, a series nanoemulsion preconcentrate (F1–F6) prepared mixing different ratios oil surfactant/cosurfactant evaluated after dilution an aqueous phase. The optimized formulation (F6) exhibits clear hydrodynamic diameter dispersed phase determined DLS DOSY morphology droplets F6 investigated AFM, which revealed formation tiny on hydrophilic mica substrate. Moreover, using less polar silicon wafer led larger spherical core shell-like structure. Overall, rational design artesunate-based could potentially be used in more efficient delivery systems.

Language: Английский

Visible‐Light‐Induced Photoreduction of Carborane Phosphonium Salts: Efficient Synthesis of Carborane‐Oxindole‐Pharmaceutical Hybrids DOI Open Access
Qiang Liu,

Bei‐Bei Zhang,

Sheng He

et al.

Angewandte Chemie International Edition, Journal Year: 2023, Volume and Issue: 62(31)

Published: April 29, 2023

Visible-light-induced photoreaction of carboranes is an effective approach to prepare carborane-containing compounds. While several methods involving boron-centered carboranyl radicals have been established, those for carbon-centered are underdeveloped, except the UV-light-promoted photohomolysis. Herein, we describe a simple but access by photoreduction carborane phosphonium salts under blue light irradiation without using transition metals and photocatalysts. The utility method was demonstrated successfully preparing range carborane-oxindole-pharmaceutical hybrids radical cascade reactions. Computational experimental studies suggest that generated single-electron transfer photoactive charge-transfer complexes between additive potassium acetate.

Language: Английский

Citations

13
Therapeutic applications of artemisinin in ophthalmic diseases DOI Creative Commons

Hao Sun,

Zhao Ping,

Lianghui Zhao

et al.

Heliyon, Journal Year: 2025, Volume and Issue: 11(2), P. e42066 - e42066

Published: Jan. 1, 2025

Artemisinin is a sesquiterpene lactone extracted from the chrysanthemum plant, Artemisia annua. It known for its curative effects in treatment of pulmonary hypertension, leukemia, diabetes, malaria, and other diseases, owing to abundant biological activity. In recent years, with development plant secondary metabolite research, potential pharmacological artemisinin-based drugs have received increasing attention; particular, reports their application ophthalmology-related diseases gradually increased. Recently, studies confirmed that artemisinin plays therapeutic roles eye through regulation signaling pathways, such asNrf2/HO-1/Keap1, TLR/MyD88/NF-κb, PI3K/AKT/mTOR, FASN/Kmal-mTOR/SREBP1, factors, as protein kinase B, AMP-activated kinase, tumor necrosis factor alpha, nod-like receptor 3, vascular endothelial growth factor, malonyl-coenzyme A cytochrome C. However, since ocular are often caused by various how can play good disease prevention role modulating these factors needs be further verified, most current focus on vitro animal experiments, lacking sufficient information clinical trial studies. To better explore perfect mechanism action ophthalmic promote artemisinin, this study reviews latest progress uveitis, uveal melanoma, age-related macular degeneration, diabetic retinopathy, neovascularization, dry eye, it will provide theoretical support large-scale future.

Language: Английский

Citations

0
Exploring the mechanism of artemisinin in alleviating lung injury caused by cardiac arrest and cardiopulmonary resuscitation based on network pharmacology and molecular docking technology DOI Creative Commons

Encong Hu,

Jianjiang Fang,

Shaoyan Lu

et al.

Research Square (Research Square), Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 29, 2025

Abstract Objective:To elucidate the mechanisms through which artemisinin mitigates lung injury post-cardiac arrest and cardiopulmonary resuscitation (CA-CPR), this study applies network pharmacology molecular docking techniques. Methods:Target proteins for were pinpointed using TCM System Pharmacology Database Analysis Platform, Herb Database, GeneCards. Predictive analyses injury-related targets post-CA-CPR conducted GeneCards, with intersections analyzed to identify shared targets. The STRING was utilized create a protein-protein interaction (PPI) network, core determined Cytoscape 3.7.2 software. Gene ontology (GO) Kyoto Encyclopedia of Genes Genomes (KEGG) performed via Weisenxin online mapping website, while executed Autodock Vina 1.1.2, visualization achieved PyMOL 2.1 Results:A total 202 targets, 7348 disease 195 intersecting 21 identified. GO analysis revealed 78 cell components, 2873 biological processes, 186 functions. KEGG highlighted involvement in pathways such as PI3K-Akt, AGE-RAGE, apoptosis, TNF. Molecular results indicated strong binding activity Conclusion:Artemisinin may mitigate following cardiac various suggesting new avenues further basic clinical research.

Language: Английский

Citations

0
Integrated transcriptomic and proteomic profiling reveals the anti-inflammatory mechanism of dihydroartemisinin in the treatment of acute liver injury by targeting CYBA and CYBB DOI

Honglian Li,

Jiayun Chen, Huiyi Guo

et al.

Biochemical and Biophysical Research Communications, Journal Year: 2025, Volume and Issue: 764, P. 151821 - 151821

Published: April 15, 2025

Language: Английский

Citations

0
Targeting self-enhanced ROS-responsive artesunatum prodrug nanoassembly potentiates gemcitabine activity by down-regulating CDA expression in cervical cancer DOI
Shengtao Wang, Kunyi Yu, Zhiyu Yu

et al.

Chinese Chemical Letters, Journal Year: 2023, Volume and Issue: 34(7), P. 108184 - 108184

Published: Feb. 7, 2023

Language: Английский

Citations

10
Autofluorescent antimalarials by hybridization of artemisinin and coumarin: in vitro/in vivo studies and live-cell imaging DOI Creative Commons

Lars Herrmann,

Maria Leidenberger,

A. Morais

et al.

Chemical Science, Journal Year: 2023, Volume and Issue: 14(45), P. 12941 - 12952

Published: Jan. 1, 2023

First antimalarial autofluorescent artemisinin–coumarin hybrids are highly in vitro / vivo active, able to overcome drug resistances and suitable for investigating their mode of action living P. falciparum parasites by fluorescence microscopy.

Language: Английский

Citations

10
Therapeutical Utilization and Repurposing of Artemisinin and Its Derivatives: A Narrative Review DOI
Lin Guan,

Huiyong Wang,

Xiaolong Xu

et al.

Advanced Biology, Journal Year: 2023, Volume and Issue: 7(8)

Published: May 13, 2023

Abstract Artemisinin (ART) and its derivatives have great therapeutical utility as antimalarials can be repurposed for other indications, such viral infections, autoimmune diseases, cancer. This review presents a comprehensive overview of the therapeutic effects ART‐based drugs, beyond their antimalarial effects. also summarizes information on repurposing in pathologies, with hope that it will guide future optimization use drugs treatment strategies listed diseases. By reviewing related literature, ART extraction structure well synthesis are presented. Subsequently, traditional roles against malaria reviewed, including mechanism occurrence resistance. Finally, potential to diseases summarized. The may useful control emerging corresponding research should directed toward more effective or better combinations.

Language: Английский

Citations

9
Tumor Microenvironment-Responsive Biodegradable Nanomedicine for Self-Enhanced Synergistic Chemo-, Photothermal, and Chemodynamic Therapy DOI
Hanxiao Tang,

Zhi-Hang He,

Chenguang Liu

et al.

ACS Applied Materials & Interfaces, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 20, 2024

The nanoscale multidrug codelivery system for synergistic therapy is an effective strategy tumor treatment. However, the low drug delivery efficiency and poor therapeutic effects limit its application. Here, based on coordination effect of Artemisinin (Art), quercetin (Qc), Fe

Language: Английский

Citations

3
Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus DOI
Lakshmi Goswami, Lovely Gupta, Sayantan Paul

et al.

RSC Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 13(8), P. 955 - 962

Published: Jan. 1, 2022

Design and synthesis of eugenol isoeugenol based glycoconjugates other analogous have been achieved using click chemistry. Two out all the synthesized compounds exhibited significant antifungal activities against A. fumigatus .

Language: Английский

Citations

15
The current scenario on anticancer activity of artemisinin metal complexes, hybrids, and dimers DOI
Shu Zhang, Chuan Yi, Weiwei Li

et al.

Archiv der Pharmazie, Journal Year: 2022, Volume and Issue: 355(8)

Published: April 28, 2022

Abstract Cancer, the most significant cause of morbidity and mortality, has already posed a heavy burden on health care systems globally. In recent years, cancer treatment made breakthrough, but cells inevitably acquire resistance, efficacy is greatly reduced as tumor progresses. To overcome above issues, novel chemotherapeutics are needed urgently. Artemisinin its derivatives—sesquiterpene lactone compounds possessing unique peroxy bridge moiety—exhibit excellent safety tolerability profiles. Mechanistically, artemisinin derivatives can promote cell apoptosis, induce cycle arrest autophagy, inhibit invasion migration. Accordingly, demonstrate promising anticancer both in vitro vivo, even clinical Phase I/II trials. The purpose present review article to provide an emphasis current scenario (January 2017–January 2022) with potential activity, inclusive metal complexes, hybrids, dimers. structure–activity relationships mechanisms action also discussed facilitate further rational design more effective candidates.

Language: Английский

Citations

14