共查询到20条相似文献,搜索用时 31 毫秒
1.
N. Apiratikul T. Penglong K. Suksen S. Svasti A. Chairoungdua B. Yingyongnarongkul 《Russian Journal of Bioorganic Chemistry》2013,39(4):444-450
A new cholesterol-based cationic lipid was synthesized; liposomes prepared on its basis were evaluated as drug delivery vehicles for curcumin. Free and liposome-encapsulated curcumin cytotoxicity against HeLa, A549, HepG2, K562 and 1301 cell lines was assessed. Liposomal curcumin with ED50 values ranging from 2.5–10 μM exhibited 2–8 times higher cytotoxicity than free curcumin. The synthetic cholesterol-based cationic lipid also enhanced cellular uptake of curcumin into tested cells. Cationic liposome alone showed low cytotoxicity at high doses with ED50 values of 90–210 μM. 相似文献
2.
Vivek Kumar Mukesh M. Mudgal Nidhi Rani Amrita Jha Manu Jaggi Anu T. Singh 《Journal of enzyme inhibition and medicinal chemistry》2013,28(3):763-770
A new series of functionalized amino acid derivatives N-substituted 1-N-(tert-butoxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidine carboxamide (1-17) and 1-N-substituted-3-amino-2-hydroxy-3-phenylpropane-1-carboxamide (18-34) were synthesized and evaluated for their in vitro cytotoxicity against human cancer cell lines. Compound 6 has shown interesting cytotoxicity (IC50 = 5.67 μm) in ovarian cancer, while compound 10 exhibited promising cytotoxicity in ovarian (IC50 = 6.1 μm) and oral (IC50 = 4.17 μm) cancers. These compounds could be of use in designing new anti-cancer agents. 相似文献
3.
Guo‐Zhen Liu Yan Liu Yan‐Ping Sun Xiao‐Mao Li Zhen‐Peng Xu Peng Jiang Xiao‐Hui Rong Bing‐You Yang Hai‐Xue Kuang 《化学与生物多样性》2020,17(4)
Fifteen constituents, including one new lignan (schisandroside E) and one new terpenoid (schisandenoid A) as well as nine known lignans and four known terpenoids, were isolated from Schisandra chinensis leaves. The structures of schisandroside E and schisandenoid A were established by entirely meticulous spectroscopic analysis (NMR, MS, CD, IR and UV). All compounds were tested for cytotoxicity against MGC‐803, Caco‐2 and Ishikawa cell lines. Some compounds showed strong cytotoxicity against these three cancer cell lines with IC50<1 μm . 相似文献
4.
Novel semisynthetic derivatives of betulin and betulinic acid with cytotoxic activity 总被引:1,自引:0,他引:1
Rita C. Santos Jorge A.R. Salvador Silvia Marín Marta Cascante 《Bioorganic & medicinal chemistry》2009,17(17):6241-6250
A series of new imidazole carboxylic esters (carbamates) and N-acylimidazole derivatives of betulin and betulinic acid (14–29) have been synthesized. The new compounds were screened for in vitro cytotoxicity activity against human cancer cell lines HepG2, Jurkat and HeLa. A number of compounds have shown IC50 values lower than 2 μM against the cancer cell lines tested and the vast majority has shown a better cytotoxicity profile than betulinic acid, including the betulin derivatives. N-Acylimidazole derivatives 26 and 27 (IC50 0.8 and 1.7 μM in HepG2 cells) and the C-3 carbamate derivative 16 (IC50 2.0 μM in HepG2 cells) were the most promising compounds. Based on the observed cytotoxicity, structure–activity relationships have been established. 相似文献
5.
Dae‐Won Ki Takeshi Kodama Ahmed H. El‐Desoky Chin Piow Wong Hien Minh Nguyen Kiep Minh Do Quang Minh Thai Lien Huong Ton Nu Hiroyuki Morita 《化学与生物多样性》2020,17(9)
A new decenoic acid derivative, gelliodesinic acid, and a naturally new alkaloid, together with three known furanoterpenoids and two known indole alkaloids, were isolated from the MeOH extract of the marine sponge Gelliodes sp. collected in Vietnam. The chemical structures of the isolated compounds were determined by analyses of 1D‐ and 2D‐NMR and MS data and by comparisons of the data with those reported in the literature. The cytotoxicity assay against HeLa, MCF‐7, and A549 cancer cell lines revealed that the three known furanoterpenes exhibited cytotoxic activities with IC50 values ranging from 23.6 to 75.5 μM against the three cell lines, and that 1H‐indole‐3‐carboxylic acid showed cytotoxicity with an IC50 value of 89.2 μM against A549 cancer cell lines. 相似文献
6.
Polypyridyl coordinating ligands are common in metal complexes used in medicinal inorganic chemistry. These ligands possess intrinsic cytotoxicity, but detailed data on this phenomenon are sparse, and cytotoxicity values vary widely and are often irreproducible. To provide new insights into the biological effects of bipyridyl-type ligands and structurally related metal-binding systems, reports of free ligand cytotoxicity were reviewed. The cytotoxicity of 25 derivatives of 2,2′-bipyridine and 1,10-phenanthroline demonstrates that there is no correlation between IC50 values and ligand properties such as pKa, log D, polarizability volume, and electron density, as indicated by NMR shifts. As a result of these observations, as well as the various reported mechanisms of action of polypyridyl ligands, we offer the hypothesis that biological effects are governed by the availability of and affinity for specific metal ions within the experimental model. 相似文献
7.
Nada M. Abdel-Wahab Harwoko Harwoko Werner E.G. Müller Alexandra Hamacher Matthias U. Kassack Mostafa A. Fouad Mohamed S. Kamel Wenhan Lin Weaam Ebrahim Zhen Liu Peter Proksch 《Bioorganic & medicinal chemistry》2019,27(17):3954-3959
Three new cyclic heptapeptides (1–3) together with three known compounds (4–6) were isolated from a solid rice culture of the soil-derived fungus Clonostachys rosea. Fermentation of the fungus on white beans instead of rice afforded a new γ-lactam (7) and a known γ-lactone (8) that were not detected in the former extracts. The structures of the new compounds were elucidated on the basis of 1D and 2D NMR spectra as well as by HRESIMS data. Compounds 1 and 4 exhibited significant cytotoxicity against the L5178Y mouse lymphoma cell line with IC50 values of 4.1 and 0.1 µM, respectively. Compound 4 also displayed cytotoxicity against the A2780 human ovarian cancer cell line with an IC50 value of 3.5 µM. The preliminary structure-activity relationships are discussed. 相似文献
8.
《Phytochemistry》1987,26(6):1623-1625
A new naturally occurring phenanthrene-1,4-quinone, annoquinone-A, along with parietin (physcion) and β-sitostenone were isolated from the stem bark of Annona montana. The structure of annoquinone-A was elucidated by spectral methods and synthesis. Annoquinone-A demonstrated potent antimicrobial activity against Bacillus subtilis and Micrococcus luteus as well as cytotoxicity in the KB (ED50 = 0.16 μg/ml) tissue culture assay. β-Sitostenone also showed significant cytotoxicity. 相似文献
9.
Claudio Luis Donnici Maria Helena Araújo Henrique S. Oliveira Diogo Rodrigo Magalhães Moreira Valéria R. Alves Pereira Marina de Assis Souza Maria Carolina Accioly Brelaz de Castro Ana Cristina Lima Leite 《Bioorganic & medicinal chemistry》2009,17(14):5038-5043
Although effective against epimastigotes (proliferative form) and of low cytotoxicity in mammals, the aryl-4-oxothiazolylhydrazones (ATZ) display only limited activity against trypomastigotes (bloodstream form) of Trypanosoma cruzi. Considering the metal complexation approach with bioactive ligands as one possible strategy for improving the biological efficacy of ATZ, a set of eight new ruthenium–ATZ complexes (RuCl2ATZCOD, COD is 1,5-cyclooctadiene) were prepared, chemically and biologically characterized, including in vitro assays against epimastigotes and trypomastigote forms of the parasite and also assessment of cytotoxicity in mammals. Two of these complexes presented antitrypanosomal activity at non-cytotoxic concentrations on mammalian cells and of higher potency than its metal–free ligands, while the metallic precursor [RuCl2COD(MeCN)2] showed only moderate antitrypanosomal activity. Comparative analysis between the ruthenium complexes and metal–free ligands demonstrated the usefulness of this approach, with the establishment of new SAR data. Additional pharmacological tests, including a DNA bond assay, gave rise to the proposal of a single preliminary explanation for the molecular origin of the bioactivity. 相似文献
10.
11.
《Free radical research》2013,47(6):407-418
The effect of a range of iron chelates on the cytotoxicity of H2O2 was studied on a mammalian epithelial cell line. Iron complexes which were internalised enhanced the cytotoxicity of H2O2 measured by delayed thymidine incorporation. Iron complexed to 8-hydroxyquinoline (Fe/8-HQ) potentiated the cytotoxicity of 50 µM by 38% and Fe/dextran by 23%. Pre-exposure of cells to Fe/dextran at 4°C did not result in any potentiation of H2O2-induced cytotoxicity which we ascribe to failure of the Fe/dextran to be endocytosed at low temperature. Iron complexes which are slowly taken up or remain extracellular protected the cells from H2O2-induced cytotoxicity. Thus, Fe/EDTA inhibited the cytotoxicity of 50 µM H2O2 by 33%; Fe/ADP by 80% and Fe/ATP by 88%, suggesting mutual extracellular detoxification. 相似文献
12.
Synthesis and antitumor activity of biotinylated camptothecin derivatives as potent cytotoxic agents
Cheng-Ting Zi Liu Yang Feng-Qing Xu Fa-Wu Dong Rui-Jing Ma Yan Li Jun Zhou Zhong-Tao Ding Zi-Hua Jiang Jiang-Miao Hu 《Bioorganic & medicinal chemistry letters》2019,29(2):234-237
A series of biotinylated camptothecin derivatives were designed and synthesized. The key to the synthesis was achieved by employing an esterification reaction and click chemistry. All of the new derivatives were tested for cytotoxicity against five human tumor cell lines, including HL-60, SMMC-7721, A-549, MCF-7, and SW480 with IC50 values ranging from 0.13 to 21.53?μM. Most of the derivatives exhibited potent cytotoxicity, especially compound 17 (IC50?=?0.13–3.31?μM) and compound 18 (IC50?=?0.23–1.48?μM), which exhibited the highest potencies. The structure-activity relationships (SARs) of the biotinylated camptothecin derivatives were discussed for exploring novel anticancer agents. 相似文献
13.
Three new (psganpenes A-C), one known eremophilane sesquiterpene and one newrelated derivative (psganpene D) were isolated from the culture of endophytic fungus Nemania sp. HDF-Br-5, which derived from Pseudotsuga gaussenii Flous, anendangered conifer endemic to China. Their structures were deduced by extensive spectroscopic methods. All isolates were screened for cytotoxicity and antibacterial activity. Psganpene D showed promising cytotoxicity against KB, HCT116 and Hela cell strains, with IC50 values in the range of 15.1–32.3 μM. 相似文献
14.
The nephrotoxic fungal toxins ochratoxin A (OA), ochratoxin B (OB) and citrinin (CIT) are natural contaminants of foods and feeds. While cytotoxicity assays have proven useful for establishing relative toxicity and structure–function relationships within groups of fungal toxins, a drawback of in vitro bioassays is their susceptibility to variation depending on endpoint, target cell, and dosing strategy. These variables were explored for OA, OB, CIT using two continuous kidney cell lines (LLC-PK1 and OK) and four cytotoxicity assay endpoints. The nephrotoxic antibiotic gentamicin was used as a positive control for cytotoxicity throughout. In general, fungal toxin-induced cytotoxicity was more pronounced in LLC-PK1 cultures using mitochondrial dehydrogenase inhibition (MTT assay) as the endpoint. Altered dosing strategy, but not seeding density, consistently influenced cytotoxicity: CIT was more toxic to cells when added at the time of seeding, whereas OA was more toxic when added 24 h after cultures were seeded. Toxicity rankings for the fungal toxins were consistent with in vivo studies and were, in order of most to least toxic, OA>OB>CIT. The data indicate that LLC-PK1 and OK cells compare favorably to existing models in terms of sensitivity to nephrotoxic fungal toxins, but also that relatively minor changes in assay protocols can affect the cytotoxicity of individual toxins and comparative toxicity within a group of toxins. 相似文献
15.
Clyde Gorapava Puilingi Yuta Kudo Yuko Cho Keiichi Konoki 《Bioscience, biotechnology, and biochemistry》2017,81(2):222-225
A new sarasinoside congener (sarasinoside M2) and known sarasinoside B1 were obtained from a marine sponge. Sarasinoside M2 was suggested to have the same aglycon as sarasinoside M although the internal glucose in its sugar moiety is replaced by xylose. Sarasinosides B1 and M2 showed moderate cytotoxicity (approximate IC50 5–18 μM) toward Neuro-2a and HepG2 cell lines. 相似文献
16.
You‐Heng Gao Zhi‐Xiong Wei Yi Cheng Teng‐Hua Wang Lin Ni Xiao‐Hong Zhou Li‐Yuan Zhang 《化学与生物多样性》2013,10(8):1487-1493
Four new ent‐kaurane diterpenoids, rabdonervosins G–J ( 1 – 4 , resp.), were isolated from the leaves and stems of Isodon nervosus. Their structures were elucidated by extensive spectroscopic analyses, including 1D‐, 2D‐NMR and HR mass spectra. Compound 2 showed potent cytotoxicity against the HepG2 and PC‐9/ZD cell lines with IC50 values of 2.36 and 6.07 μM , respectively, and compound 3 exhibited cytotoxicity against the HepG2 and CNE2 cell lines with IC50 values of 8.64 and 9.77 μM , respectively. 相似文献
17.
Bazargan L Fouladdel S Shafiee A Amini M Ghaffari SM Azizi E 《Cell biology and toxicology》2008,24(2):165-174
Failure of current anticancer drugs mandates screening for new compounds of synthetic or biological origin to be used in cancer
therapy. Multidrug resistance (MDR) is one of the main obstacles in the chemotherapy of cancer. Efflux of cytotoxic agents
mediated by P-glycoprotein (P-gp or MDR1) is believed to be an important mechanism of multidrug resistance. Therefore, we
decided to investigate the antiproliferative effects of seven newly synthesized 1,4-dihydropyridine (DHP) derivatives in comparison
to verapamil (VP) and doxorubicin (DOX) on human breast cancer T47D cells and its MDR1 overexpressed and moderately resistant
cells (RS cells) using MTT cytotoxicity assay. We also examined the effects of these compounds on cytotoxicity of DOX in these
two cell types. The cytotoxicity assays using MTT showed that most of the tested new DHP derivatives and VP at 10 μM concentration
had varying levels of toxicity on both T47D and RS cells. The toxicity was mostly in the range of 10–25%. However, the cytotoxicity
of these DHP derivatives, similar to VP, was significantly less than DOX when comparing IC50 values. Furthermore, these compounds in general had relatively more cytotoxicity on T47D vs RS cells at 10-μM concentration.
Among new DHPs, compounds 7a (3,5-dibenzoyl-4-(2-methylthiazol-4-yl)-1,4-dihydro-2,6-dimethylpyridine) and 7d (3,5-diacetyl-4-[2-(2-chlorophenyl)thiazol-4-yl)]-1,4-dihydro-2,6-dimethylpyridine)
showed noticeable potentiation of DOX cytotoxicity (reduction of DOX IC50) compared to DOX alone in both cells, particularly in RS cells. This effect was similar to that of VP, a known prototype
of MDR1 reversal agent. In other words, compounds 7a and 7d resensitized RS cells to DOX or reversed their resistance. Results
indicate that compound 7d exerts highest effect on RS cells. Therefore, these two newly synthesized DHP derivatives, compounds
7a and 7d, are promising as potential new MDR1 reversal agents and should be further studied on other highly resistant cells
due to MDR1 overexpression and with further molecular investigation. 相似文献
18.
Four new 2-arylbenzofuran derivatives wittifurans O, N, K and L (1–4) were isolated from the stem bark of Morus wittiorum. Their structures were elucidated on the basis of spectroscopic analysis. Compounds 1–3 were evaluated for their cytotoxicity against five human cancer cell lines. Compounds 1 and 2 exhibited selective cytotoxicity against human ovarian cancer cell line A2780 with IC50 (μM) values of 1.80 and 1.32, respectively. 相似文献
19.
《Journal of enzyme inhibition and medicinal chemistry》2013,28(3):330-338
New hydrazone ligands (HL) derived from 5-substituted isatins and 1-(4-(2-methoxybenzyl)-6-arylpyridazin-3-yl)hydrazines and its complexes with Co(II) and Cu(II) were synthesized. The new hydrazones and their complexes were characterized by means of elemental, spectral analyses and magnetic studies. Primary cytotoxicity evaluation of HL 5a and the new complexes showed that these complexes could act as anticancer agents since they reduced the growth of samples of human tumour cell lines (HCT116(Colon), MCF7(Breast) and HELA(Cervix)) to ≤18.5 μg/mL for the new complexes. 相似文献
20.
Kang Ding Ya-Yao Zhang Ting Yang Wen-Wen Lian Cong-Yuan Xia Wen-Ping Wang Wei-Ku Zhang Jun He Jie-Kun Xu 《化学与生物多样性》2023,20(3):e202300013
Phytochemical investigation of the roots of Euphorbia ebracteolata Hayata resulted in the isolation of three new rosane diterpenoids, euphebracteolatins C–E ( 1 – 3 ), along with fourteen known analogs ( 4 – 17 ). Their structures were determined on the basis of extensive spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR. Euphebracteolatin C ( 1 ) contains a C-1/C-10 double bond and a keto group at C-7, and euphebracteolatins D and E ( 2 – 3 ) possess an aromatic ring-A in their skeleton. The plausible biogenetic pathways of all the isolates were also proposed. Furthermore, compounds 1 and 9 showed selective cytotoxicity against HepG2 cells with IC50 values of 14.29 and 12.33 μM, respectively, and 2 – 3 displayed moderate cytotoxicity against three human cancer lines, with IC50 values ranging from 23.69 to 39.25 μM. 相似文献