A concise review on Artemisia annua L.: A major source of diverse medicinal compounds

Industrial Crops and Products, Journal Year: 2022, Volume and Issue: 184, P. 115072 - 115072

Published: May 18, 2022

Language: Английский

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Artemisinin and Its Derivatives as Potential Anticancer Agents

Molecules, Journal Year: 2024, Volume and Issue: 29(16), P. 3886 - 3886

Published: Aug. 16, 2024

Artemisinin is a natural sesquiterpene lactone obtained from the traditional Chinese medicinal herb Artemisia annua L. (qinghao). and its derivatives share an unusual endoperoxide bridge are extensively used for malaria treatment worldwide. In addition to antimalarial activities, artemisinin have been reported exhibit promising anticancer effects in recent decades. this review, we focused on research progress of with potential activities. The pharmacological effects, mechanisms, clinical trials cancer therapy were discussed. This review may facilitate future exploration as effective agents.

Language: Английский

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New Imidazo[4,5‐c]pyridine‐piperidine Hybrids as Potential Anti‐cancer Agents and In‐Silico Studies

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(2)

Published: Jan. 10, 2024

Abstract Design and synthesis of a series novel hybrid molecules that combine Imidazo[4,5‐c] pyridines with piperdines are presented in this paper. Total 17 derivatives were meticulously synthesized characterized using 1 H NMR, 13 C MS elemental analysis techniques. The vitroanticancer activities estimated by verifying their effectiveness against the MCF‐7 human breast adenocarcinoma A549 lung cancer cell line, cisplatin doxorubicin serving as reference drugs. Several these compounds demonstrated significant potential, displaying IC 50 values within range 12.26–84.5 μM for A549, 13.37–69.82 MCF‐7. Notably, compound 11 b is found to be more potent than standard drug an 12.26±0.8 cells, while d exhibited highest inhibition 13.37±0.4 cells. Although its was moderately lower when compared doxorubicin, it still retained substantial anticancer activity. Molecular docking studies performed decouple binding affinity ligand interactions estrogen receptor alpha (ERα) (PDB ID: 3ERT). pharmacokinetic evaluation revealed favourable drug‐likeness properties all molecules, suggesting potential therapeutic agents.

Language: Английский

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Multiple stimuli-responsive nanosystem for potent, ROS-amplifying, chemo-sonodynamic antitumor therapy

Bioactive Materials, Journal Year: 2021, Volume and Issue: 15, P. 355 - 371

Published: Dec. 20, 2021

Although sonodynamic therapy (SDT) is a promising non-invasive tumor treatment strategy due to its safety, tissue penetration depth and low cost, the hypoxic microenvironment limits therapeutic effects. Herein, we have designed developed an oxygen-independent, ROS-amplifying chemo-sonodynamic antitumor based on novel pH/GSH/ROS triple-responsive PEG-PPMDT nanoparticles. The formulated artemether (ART)/Fe3O4-loaded NPs can rapidly release drug under synergistic effect of acidic endoplasmic pH high intracellular GSH/ROS levels inhibit cancer cell growth. Besides, ROS level in NPs-treated cells magnified by ART via interactions with both Fe2+ ions formed situ at external ultrasound irradiation, which not affected hypoxia microenvironment. Consequently, enriched cause direct necrosis ROS-stressed further accelerate from ROS-responsive NPs, achieving incredible potency. Specifically, upon ART/Fe3O4-loaded all xenotransplants human hepatocellular carcinoma (HepG2) nude mice shrank significantly, 40% tumors were completely eliminated. Importantly, Fe3O4 encapsulated efficient MRI contrast agent be used guide procedures. Further, biosafety analyses show that possess minimal toxicity main organs. Thus, our combined method for potent controlled facile exogenous generation abundant target sites.

Language: Английский

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Synthesis and Anticancer Evaluation of Novel Indole Based Arylsulfonylhydrazides against Human Breast Cancer Cells

ACS Omega, Journal Year: 2022, Volume and Issue: 7(46), P. 42036 - 42043

Published: Nov. 10, 2022

A series of novel indole based sulfonohydrazide derivatives (5a-k) containing morpholine heterocyclic ring were synthesized through multistep chemical reactions. The target compounds prepared by the reaction substituted phenyl sulfonylhydrazides (2a-k) with derivative 3-carboxaldehyde. All screened for their anticancer activity in vitro against estrogen receptor-positive breast cancer line MCF-7 and triple-negative cell line, MDA-MB-468. It was found that among all evaluated compounds, chemotype 4-chloro-N'-((1-(2-morpholinoethyl)-1H-indol-3-yl)methylene)benzenesulfonohydrazide (5f) showed promising inhibition both MDA-MB-468 cells respective IC50 values 13.2 μM 8.2 μM. Compound 5f to be nontoxic HEK 293 noncancerous studied concentration range, therefore indicating such chemotypes inhibit proliferation cancerous selectively significantly.

Language: Английский

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Inverse α-Effect as the Ariadne’s Thread on the Way to Tricyclic Aminoperoxides: Avoiding Thermodynamic Traps in the Labyrinth of Possibilities

Journal of the American Chemical Society, Journal Year: 2022, Volume and Issue: 144(16), P. 7264 - 7282

Published: April 14, 2022

Stable tricyclic aminoperoxides can be selectively assembled via a catalyst-free three-component condensation of β,δ'-triketones, H2O2, and an NH-group source such as aqueous ammonia or ammonium salts. This procedure is scalable produce gram quantities heterocycles, containing peroxide, nitrogen, oxygen cycles in one molecule. Amazingly, complex molecules are formed despite the multitude alternative reaction routes, equilibration hemiaminal, monoperoxyacetal, peroxyhemiaminal functionalities! The initiated by "stereoelectronic frustration" H2O2 combines elements thermodynamic kinetic control with variety mono-, bi-, structures evolving under conditions until they reach wall created inverse α-effect, that is, stereoelectronic penalty for formation peroxycarbenium ions related transition states. Under these conditions, stops before reaching most thermodynamically stable products at stage where three different heterocycles fused acyclic precursor frame.

Language: Английский

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An updated review on distribution, biosynthesis and pharmacological effects of artemisinin: A wonder drug

Phytochemistry, Journal Year: 2023, Volume and Issue: 214, P. 113798 - 113798

Published: July 28, 2023

Language: Английский

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Tween 80 Micelles Loaded with Fe3O4 Nanoparticles and Artemisinin for Combined Oxygen-Independent Ferroptosis Therapy of Cancer

Pharmaceutics, Journal Year: 2024, Volume and Issue: 16(5), P. 639 - 639

Published: May 9, 2024

Artemisinin has an endoperoxide bridge structure, which can be cleaved by ferrous ions to generate various carbonyl radicals in oxygen-independent manner, highlighting its potential for treating hypoxic tumors. In our study, we fabricated Tween 80 micelles loaded with Fe3O4 nanoparticles and artemisinin cancer therapy. The synthesized drug-loaded have particle sizes of about 5 nm nm, respectively, both exhibiting excellent dispersibility stability. After uptake MCF-7 cells, release Fe2+ ART into the cytoplasm, effectively inducing generation reactive oxygen species (ROS) conditions, thereby enhancing toxicity against cells. vitro vivo studies demonstrated that are encapsulated form micelles, prevent premature during circulation body. Although free inhibit tumor growth, TW80-Fe3O4-ART demonstrate a more pronounced inhibitory effect, suppression rate up 85%. A novel strategy based on ferroptosis is thus offered, holding favorable prospect

Language: Английский

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Exploration of artemisinin derivatives and synthetic peroxides in antimalarial drug discovery research

European Journal of Medicinal Chemistry, Journal Year: 2021, Volume and Issue: 213, P. 113193 - 113193

Published: Jan. 18, 2021

Language: Английский

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Artemisinin‐derived dimers from a chemical perspective

Medicinal Research Reviews, Journal Year: 2021, Volume and Issue: 41(6), P. 2927 - 2970

Published: June 11, 2021

Abstract Considerable progress has been made with the rather recently developed dimer approach, which already found applications in development of new effective artemisinin‐derived antimalarial, anticancer, and antiviral agents. One observation common to these potential is significant (i.e., much more than double) improvement activity artemisinin based dimers, are not toxic normal cells have fewer or less harmful side effects, respect monomers against parasites, cancer viruses. Due high dimerization concept, many compounds their biological activities reported. In this review an overview synthesis drug candidates on clinically used its semisynthetic derivatives given. Besides highlighting selected main focus set different synthetic approaches toward dimers containing a broad variety symmetric nonsymmetric linking moieties.

Language: Английский

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