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Phthalocyanines (Pcs) which have been proposed as sensitizers to supersede haematoporphyrin derivatives, are currently undergoing clinical trials for use in the photo- dynamic therapy (PDT) of cancer . This is due to the superior molar absorptivity of these compounds ,at wavelengths permitting greater penetration of light in normal tissues , when compared with photofrin . Among the unsubstituted phthalocyanines, zinc phthalocyanine has been investigated as a possible second- generation PDT sensitizer. Zinc phthalocyanine itself, because of its water insolubility, is used in liposomal form and has shown sufficient PDT activity . Zinc phthalo- cyanine sulfonic acids have perhaps received the closest attention, and their water solubility is a distinct advantage . Methods for synthesis of sulfonated phthalocyanines, however, often yield complex mixtures composed of different levels of substitution and regioisomers . To overcome such solubility problems, we proposed and synthesized the polyfluoroalkoxyl substituted zinc phthalo- cyanines as sensitizers for PDT. First, the improved solubility of the alkyl-, alkoxyl- or fluorine-substituted phthalocyanines makes their separation and identifion more easy ; second, fluorine is similar in size to hydro- gen and can mimic hydrogen in biological environments . But these quite hydrophobic photosensitizers also need to be bound with cancer-specific antibodies or cyclodextrin dimers for an increase of bioactivity and a decrease of unwanted side reactions . The literature reported preparation procedures are quite intricate. On the other hand, the improved solubility in most organic solvents renders the designated drugs more amenable for formulation in various vehicles, including water–oil emul- sions and nanoparticles and leads to enhanced interaction with membrane . In this report we synthesized tetra(tri- fluoroethoxyl) zinc phthalocyanine , which was used with perfluorocarbon emulsifying agent F68 for photodynamic actions. These studies were performed on myeloma cells and Chinese hamster ovary cells in vitro. |

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酞菁(PCS)已被提議作為敏來取代血卟啉衍生物,目前正在進(jìn)行臨床試驗(yàn)中使用的照片動(dòng)力療法(PDT)的癌癥。這是由于優(yōu)越的摩爾吸光系數(shù)為這些化合物中,在波長允許更大的滲透在正常組織中的光相比,當(dāng)與photofrin的。其中的未取代的酞菁,鋅酞菁已被研究作為一個(gè)可能的第二代PDT增敏劑。鋅酞菁本身因?yàn)樗乃蝗苄裕灾|(zhì)體的形式使用并表現(xiàn)出足夠的PDT活動(dòng)。鋅酞菁磺酸也許已經(jīng)收到最接近 注意,和水溶性是一個(gè)明顯的優(yōu)勢;腔嫉暮铣煞椒,然而,往往產(chǎn)生復(fù)雜的混合物組成的的取代和區(qū)域異構(gòu)體的不同的水平。為了克服這樣的溶解度問題,我們提出并合成polyfluoroalkoxyl的取代鋅酞為PDT敏菁。首先,改進(jìn)的烷基,烷氧基或氟取代的溶解度酞菁使得他們的分離和identifion的更多容易;第二,氟大小相似,水電在生物環(huán)境中的根可以模仿氫。但這些完全疏水性光敏劑也需要綁定與癌特異性抗體或環(huán)糊精二聚體的生物活性增加和減少不需要的副反應(yīng)。文獻(xiàn)報(bào)告的編寫程序是相當(dāng)復(fù)雜的。在另一方面,改進(jìn)的溶解度大多數(shù)有機(jī)溶劑呈現(xiàn)指定的藥物更適合制定各車輛,包括水油乳化sions和增強(qiáng)互動(dòng)的納米粒子,并導(dǎo)致膜。在這份報(bào)告中,我們合成的四(三fluoroethoxyl)的酞菁鋅,達(dá)用全氟化碳乳化劑F68光動(dòng)力行動(dòng)。這些究進(jìn)行 骨髓瘤細(xì)胞和中國倉鼠卵巢細(xì)胞的體外培養(yǎng)。 |
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