Preparation and anti-tumor activity of PEG-PCL polymersomes loaded with curcumol derivative in HepG2 cell line

Wang, Dazhuang; Luo, Fuyao; He, Fang; Lu, Fu-Hsing; Song, Ke; Zhao, Jinghua; Chen, Lijiang

doi:10.1016/j.jddst.2021.102782

Cited by 3 publications

(3 citation statements)

References 26 publications

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“…They are among the most important chemical structures widely distributed in biologically active compounds that have been discovered due to their conjugated double bond and Michael acceptor activity. [11][12][13] Curcumol, one of the major active components from zedoary turmeric essential oil, [14][15][16] has a variety of biological activities, such as anti-tumor activity, [17,18] anti-proliferative activity, [19,20] anti-inflammation, [21] antifungal activity, [22,23] anti-virus, [24] and so on. Until now, studies on curcumol and its derivatives have mainly focused on the antitumor activity, with fewer reports about the anti-phytopathogenic fungal activity.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antifungal Activity of Curcumol Derivatives

Gao

Jin

Jian

et al. 2023

Chemistry & Biodiversity

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To discover novel and effective antifungal candidates, a series of new curcumol derivatives were designed, synthesized, and evaluated their antifungal activity against five phytopathogenic fungi by the mycelium growth rate method. Derivatives c4, c22 and c23 exhibited excellent antifungal activity against Phomopsis sp. with EC50 values of 3.06, 3.07, and 3.16 μM, respectively. Specifically, compound c4 exhibited the strongest antifungal activity against Phomopsis sp., which was 44 times that of pyrimethanil (EC50=134.37 μM). The results of scanning electron microscopy (SEM) and transmission electron microscopy (TEM) indicated that compound c4 could cause cell senescence and death of Phomopsis sp. by changing the normal hyphal morphology and disrupting the normal metabolism of hyphal cells. Moreover, compound c4 showed excellent curative effect against Phomopsis sp. on kiwifruit. These findings confirmed that compound c4 has great potential as a potent antifungal agent.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Antifungal Activity of Curcumol Derivatives

Gao

Jin

Jian

et al. 2023

Chemistry & Biodiversity

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“…For this reason hydrophilic poly(ethylene glycol) (PEG) was incorporated into or blended with Poly(ε-caprolactone) to increase the hydrophilicity and the biodegradation rate. [3] Doxorubicin hydrochloride (DOX⋅HCl) is an anthracycline drug. Doxorubicin hydrochloride (DOX⋅HCl), have been re-ported with a common uses in ovarium, breast and lung cancer as well as malignant lymphoma at the same time, the cardiotoxicity related side-effect restricts its long term use for such clinic aims.…”

Section: Introductionmentioning

confidence: 99%

“…This characteristic limits PCL use as a carrier in the controlled drug delivery system. For this reason hydrophilic poly(ethylene glycol) (PEG) was incorporated into or blended with Poly(ϵ‐caprolactone) to increase the hydrophilicity and the biodegradation rate [3] …”

Section: Introductionmentioning

confidence: 99%

Design and Fabrication of Anticancer Drug‐Loaded Poly(ϵ‐caprolactone)‐Poly(ethylene glycol)‐Poly(ϵ‐caprolactone) Micelles as Controlled Release System

Kocabay¹,

İsmail

2023

ChemistrySelect

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In this study, doxorubicin (DOX) loaded polymeric micelles (PMs) were synthesized based on biodegradable poly(εcaprolactone)-poly(ethylene glycol)-poly(ε-caprolactone) (PCEC) triblock copolymers. So four parameters (shaking speed (rpm) X 1 , time of contact (hour) X 2 , amount of triethylamine (TEA) (μL) X 3 , DOX% X 4 ) were optimized. Then by adding valspodar (PSC 833) or D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS 1000) to the formulations DOX/PSC 833-PMs or DOX/ TPGS 1000-PMs were prepared by a nanoprecipitation method. The synthesized micelles exhibited high drug-loading encapsu-lation efficiency (> 78.98 %), high stability, and pH-dependent drug release. The results showed that the encapsulation efficiencies were not compromised by co-encapsulation of two agents. Finally, it was observed that the association of both DOX and PSC 833 or both DOX and TPGS 1000 within a single micelle formulation elicited the most soluble DOX as compared to DOX loaded formulations (DOX-PMs) while using a lower amount of polymer compared to separated micelle formulations.

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