Mapping the interactions and bioactivity of quercetin⿿(2-hydroxypropyl)-β-cyclodextrin complex

Kellici, Tahsin F.; Chatziathanasiadou, Μaria V.; Diamantis, Dimitris; Chatzikonstantinou, Alexandra V.; Andreadelis, Ioannis; Christodoulou, Eirini; Valsami, Georgia; Mavromoustakos, Thomas; Tzakos, Andreas G.

doi:10.1016/j.ijpharm.2016.07.008

Cited by 52 publications

(33 citation statements)

References 41 publications

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“…To conquer this, various approaches are being exploited at the moment. These include, but are not limited to: a) utilization of drug delivery vehicles and formulates like nanoparticles [ 24 ] and calixarenes or cyclodextrins [ 25 – 26 ], where the cytotoxic drug is loaded and can be released at the malignant tumor site; b) installation of labile chemical groups to the tumor microenvironment (i.e., low pH) able to mask the cytotoxic drug and form a prodrug with enhanced plasma stability and/or cell permeability [ 27 ] and in the same time diminished toxicity for normal cells; c) covalent attachment of a drug on a tumor-targeting element (small molecule, peptide or antibody) able to selectively target and permeate cancer cells. The conjugation is being conducted via a rationally designed linker able to release the drug inside the cancer microenvironment [ 19 ].…”

Section: Reviewmentioning

confidence: 99%

On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

Vrettos

Mező

Tzakos

2018

Beilstein J. Org. Chem.

120

124

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Cancer is the second leading cause of death affecting nearly one in two people, and the appearance of new cases is projected to rise by >70% by 2030. To effectively combat the menace of cancer, a variety of strategies have been exploited. Among them, the development of peptide–drug conjugates (PDCs) is considered as an inextricable part of this armamentarium and is continuously explored as a viable approach to target malignant tumors. The general architecture of PDCs consists of three building blocks: the tumor-homing peptide, the cytotoxic agent and the biodegradable connecting linker. The aim of the current review is to provide a spherical perspective on the basic principles governing PDCs, as also the methodology to construct them. We aim to offer basic and integral knowledge on the rational design towards the construction of PDCs through analyzing each building block, as also to highlight the overall progress of this rapidly growing field. Therefore, we focus on several intriguing examples from the recent literature, including important PDCs that have progressed to phase III clinical trials. Last, we address possible difficulties that may emerge during the synthesis of PDCs, as also report ways to overcome them.

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Section: Reviewmentioning

confidence: 99%

On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

Vrettos

Mező

Tzakos

2018

Beilstein J. Org. Chem.

120

124

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“…HP-Cyd dibuat dengan memodifikasi struktur β-siklodekstrin, yang mana struktur molekul β-siklodekstrin diperoleh dari ccdc.cam.ac.uk dengan kode BUVSEQ02 [28]. Model β-siklodekstrin dengan kode ini telah digunakan pada beberapa penelitian sebelumnya [29][30][31][32][33][34] Sama seperti pada penelitian sebelumnya [20], Skema proses pelarutan kompleks inklusi HP-Cyd dan Hklrkn diperlihatkan oleh Gambar 2. E1, E2, E3, secara berturut-turut adalah energi Hklrkn, HP-Cyd, kompleks inklusi HP-Cyd dan Hklrkn pada kondisi vakum atau fasa gas.…”

Section: Prosedurunclassified

Kajian Teoretis Interaksi Antarmolekul pada Kompleks Inklusi Hidroksipropil-β-Siklodekstrin dan Hidroksiklorokuin

Ivansyah

2020

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Di penghujung tahun 2019, terjadi wabah dengan gejala yang mirip dengan SARS di Republik Rakyat China yang disebabkan oleh virus SARS-CoV-2. Penyebaran virus yang masif, termasuk di Indonesia, menyebabkan WHO mengeluarkan status pandemi. Salah satu alternatif untuk mengurangi pasien COVID-19 adalah dengan menggunakan obat-obatan yang ada, hingga vaksin ditemukan dan siap digunakan. Saat ini, hidroksiklorokuin telah banyak diteliti sebagai kandidat obat anti COVID-19, yang kini telah memasuki tahap uji klinis. Namun kelarutan hidroksiklorokuin dalam air sangat kecil sehingga berdampak pada rendahnya ketersediaan hayati dalam tubuh manusia. Salah satu cara untuk meningkatkan kelarutan hidroksiklorokuin dalam air adalah melalui pembentukan kompleks inklusi yang stabil dengan hidroksipropil-β-siklodekstrin. Pada penelitian ini telah dilakukan studi komputasi dengan metode penambatan molekul dan metode kuantum semiempiris untuk mengetahui interaksi antara hidroksipropil-β-siklodekstrin dan hidroksiklorokuin. Hasil studi komputasi ini menunjukkan bahwa hidroksipropil-β-siklodekstrin dan hidroksiklorokuin membentuk kompleks inklusi yang stabil. Selain itu, kelarutan hidroksiklorokuin dalam larutan air dapat ditingkatkan dengan membentuk kompleks inklusi dengan hidroksipropil-β-siklodekstrin.Kata Kunci: Hidroksipropil-β-Siklodekstrin; Hidroksiklorokuin; SARS-CoV-2; COVID-19; Kompleks Inklusi.

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“…Quercetin (QUE), a flavonoid aglycone, has illustrated a broad spectrum of bioactivities, especially due to its potential to kill cancer cells, while sparing normal cells . Recently, a QUE‐(2‐hydroxypropyl)‐β‐cyclodextrin (HP‐β‐CD) complex was reported by us with amplified aqueous solubility and significant bioactivity in T24 human bladder cancer . After using a multidisciplinary approach employing biochemical and physicochemical assays we revealed that QUE binds directly to the BH3 domain of Bcl‐xL and Bcl‐2 proteins, thus promoting cancer cell apoptosis .…”

Section: Figurementioning

confidence: 99%

Three Regioselectively Acylated Flavonoid Aglycone Derivatives in Equimolar Yield at One Blow

et al. 2018

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Mapping the interactions and bioactivity of quercetin⿿(2-hydroxypropyl)-β-cyclodextrin complex

Cited by 52 publications

References 41 publications

On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

Kajian Teoretis Interaksi Antarmolekul pada Kompleks Inklusi Hidroksipropil-β-Siklodekstrin dan Hidroksiklorokuin

Three Regioselectively Acylated Flavonoid Aglycone Derivatives in Equimolar Yield at One Blow

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