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1.
Chem Pharm Bull (Tokyo) ; 70(6): 420-426, 2022 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-35342147

RESUMO

Cationic liposomal formulations of the telomeric G-quadruplex stabilizing ligand, 13-(2-naphthylmethoxy)berberine bromide (1), have been developed with the purpose of delivering 1 into the nucleus of cancer cells for potential telomere targeting. Berberine derivative 1 was encapsulated in various cationic lipids 2-4 by the thin film evaporation method; these lipids are cationic after amine protonation. The most appropriate liposomal berberine formulation was that of 1 and the cholesterol derived cationic lipid 4 in a weight ratio of 1 : 20 with 76.5% encapsulation efficiency of 1. Cellular uptake studies in the HeLa and HT-29 cancer cells lines showed that the liposomal berberine derivative uptake in the cells was higher and more stable than for berberine derivative 1 alone while free 1 was completely decomposed in the cells within 60 min exposure to the cells. Anticancer activity of the liposomal berberine derivative 1 based on 4 was greater than that for the free berberine derivative 1 in the MCF-7, HeLa and HT-29 cell line by 2.3-, 4.9- and 5.3-fold, respectively, and also, interestingly, superior to the anticancer drug doxorubicin against the HT29 cancer cell line.


Assuntos
Berberina , Lipossomos , Berberina/farmacologia , Cátions , Doxorrubicina , Humanos , Lipídeos
2.
Nat Prod Res ; 35(1): 80-87, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31135214

RESUMO

Phytochemical investigation of the roots of Cissampelos pareira Linn. led to the isolation of one new pyrrole alkaloid, cissampeline (1), together with ten known alkaloids, (-)-curine (2), (-)-cyclanoline (3), (+)-tetrandrine (4), (+)-obaberine (5), (+)-obamegine (6), (-)-oblongine (7), (+)-homoaromoline (8), (-)-nor-N׳-chondrocurine (9), trans-N-feruloyltyramine (10) and (+)-coclaurine (11). Their structures were elucidated by extensive NMR and MS spectroscopic analyses. Interestingly, compound 1 represents the first example of pyrrole alkaloid found in the genus Cissampelos. Moreover, compounds 5-11 were isolated for the first time from this genus. Among them, compound 6 showed the highest anti-acetylcholinesterase activity with an IC50 value of 3.26 µM, whereas compound 8 displayed the most potent cytotoxicity against human colon cancer (HT29) cells with an IC50 value of 7.89 µM.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Inibidores da Colinesterase/farmacologia , Cissampelos/química , Alcaloides/isolamento & purificação , Inibidores da Colinesterase/química , Avaliação Pré-Clínica de Medicamentos , Células HT29 , Células HeLa , Humanos , Isoquinolinas/isolamento & purificação , Isoquinolinas/farmacologia , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Raízes de Plantas/química , Pirróis/química
3.
Nat Prod Res ; 34(21): 3019-3026, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32962428

RESUMO

A new ent-abietane lactone, 3-oxojolkinolide A (1), together with 16 known compounds, helioscopinolide E (2), helioscopinolide A (3), 3-methyl-9H-carbazole (4), carbalexin (5), carbalexin B (6), glycaborinine (7), arborinine (8), 1H-indole-3-carbaldehyde (9), glycoamide A (10), glycoamide B (11), 2-(N-methyl-2-phenylacetamido)benzoic acid (12), 2-(methylamine)-methylbenzoate (13), fraxidin (14), scopoletin (15), (-)-syringaresinol (16) and ferulic acid (17) were isolated from Glycosmis pentaphylla. The structures of these compounds were elucidated using spectroscopic techniques such as NMR and MS. Among them, compounds 1-3, 9 and 12-17 were isolated from the genus Glycosmis for the first time.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Lactonas/química , Rutaceae/química , Abietanos/química , Abietanos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Ácidos Cumáricos/química , Ácidos Cumáricos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Células HT29 , Células HeLa , Humanos , Indóis/química , Indóis/isolamento & purificação , Lactonas/isolamento & purificação , Células MCF-7 , Espectroscopia de Ressonância Magnética , Estrutura Molecular
4.
RSC Adv ; 8(33): 18204-18215, 2018 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-35541146

RESUMO

Six new 14-membered ring cyclopeptide alkaloids, cambodines A-F (1-6), and two known compounds, frangufoline (7) and lotusanine B (8), were isolated from the root bark extract of Ziziphus cambodiana Pierre. Their structures and configurations were established based on 1D and 2D NMR, HRMS, ECD, and X-ray crystallographic data. Compounds 1 and 3 are rare 5(14)-type cyclopeptide alkaloids that possess an imidazolidin-4-one ring in the terminal unit. The cyclopeptides were tested for their in vitro antiplasmodial, antitubercular, and cytotoxic effects against three cancer cell lines. Compound 3 showed significant antiplasmodial activity against the malarial parasite Plasmodium falciparum, with an IC50 value of 6.09 µM.

5.
Biol Pharm Bull ; 37(9): 1534-42, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25177036

RESUMO

Lipid-mediated delivery of DNA into cells holds great promise both for gene therapy and basic research applications. The primary approach to improving transfection efficiency is the design and synthesis of novel cationic lipids. Alternatively, using the synergistic effect of different cationic mixtures can provide another approach to increasing transfection efficiency. This paper describes the synergistic effect of lipids with different polarheads, central core structures and hydrophobic tails. The enhancement of cellular transfection into HEK293 cells was observed by combining two lipids having aminoglycerol and di(hydroxylethyl)amino core structures at a 1 : 1 weight ratio. Additionally, the liposome formation of these lipids with the helper lipid, 1,2-dioleoyl-propyl-3-phosphatidylethanolamine (DOPE), at the weight ratio of 1 : 1 can provide higher transfection efficiency into HEK293, MCF-7 and HeLa cells than Lipofectamine™ 2000. Our finding indicated that cationic liposomes comprised of a mixture of lipids with different polarheads, central core structures and hydrophobic tails should be very promising in liposome-mediated gene delivery in vitro and in vivo.


Assuntos
DNA/administração & dosagem , Lipídeos/química , Transfecção/métodos , Sobrevivência Celular , DNA/química , Células HEK293 , Células HeLa , Humanos , Interações Hidrofóbicas e Hidrofílicas , Lipossomos , Células MCF-7
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