共查询到19条相似文献,搜索用时 62 毫秒
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用于光动力治疗的金属酞菁配合物-- 两亲性酞菁锌配合物ZnPcS2P2的制备、表征及抗癌活性 总被引:12,自引:0,他引:12
用直接取代法合成得到含磺基和邻苯二甲酰亚胺甲基的一系列双取代的酞菁锌化合物, 产物经反相高效液相色谱法分离得5种不同组分, 经膜分离法进一步纯化和浓缩后, 用元素分析、红外光谱等进行表征. 测定各组分在光照下产生单线态氧的能力,并通过离体试验比较它们杀伤癌细胞的能力. 对其中具有较高光动力抗癌活性的物种二磺基二邻苯二甲酰亚胺甲基酞菁锌(ZnPcS2P2)进一步用紫外可见光谱、核磁、热分析、质谱等方法进行结构表征. 研究了ZnPcS2P2的在体抗肿瘤活性, 结果表明, 在670 nm激光的激发下(光照剂量为72 J/cm2), ZnPcS2P2(药剂量为2 mg/kg)对小鼠的U14和S180移植瘤的抑瘤率分别达到89.8%和90.8%. 探讨了构效关系, 初步分析了ZnPcS2P2具有较高活性的结构原因. 相似文献
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通过光谱法研究了三种磺化酞菁(α位四磺化酞菁、β位四磺化酞菁和α位单取代磺化酞菁)与人血清白蛋白(HSA)的相互作用.结果 表明,HSA对α位四磺化酞菁的存在状态(单体、聚集体)影响显著,而对β位四磺化酞菁和α位单取代磺化酞菁的存在状态没有明显影响.磺化酞菁与HSA均存在明显的相互作用,且.四磺化酞菁与HSA的结合作用... 相似文献
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光动力治疗(Photodynamic therapy,PDT)作为一种有别于传统癌症治疗方式的新型疗法,近些年来受到了科学家们越来越多的关注.它凭借着自身创伤性小,毒性低微,适用性好,可协同手术治疗以及可重复治疗等独特优势,在许多肿瘤的治疗方面有着广泛的应用.本文简要概述了光动力疗法的原理以及光敏剂的发展历程,并对理想光敏剂的特点作了总结.目前,以酞菁类化合物为主的第三代光敏剂已经成为光动力疗法的研究热点,然而如何提高光敏剂分子的靶向性达到精准的光动力治疗仍然是亟待解决的问题.因此,主要综述了近年来靶向性酞菁类光敏剂的研究进展,并对未来光敏剂的重点研究方向做出了展望.从目前来看,如何克服癌症低氧微环境的限制,发展Type I型不依赖氧的体系以及光穿透力强的靶向光敏剂在光动力治疗方面存在着巨大的潜质,有望成为新一代十分优良的光动力疗法用光敏剂. 相似文献
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新型单取代两亲性酞菁锌的制备及其光动力活性研究 总被引:5,自引:2,他引:3
设计并制备了一种组成和结构单一的新型两亲性酞菁锌光敏剂. 采用固相合成法合成出2-单羧基取代酞菁锌, 并使之与五聚赖氨酸偶联成五聚赖氨酸2-羰基酞菁锌. 综合运用各种分析及光谱方法对所得化合物进行表征和确认. 研究了在光照下五聚赖氨酸2-羰基酞菁锌对3种肿瘤细胞(人源肝癌细胞Bel7402、人源胃癌细胞BGC823和人源白血病细胞K562) 与一种正常细胞(人源胚肺成纤维细胞HELF)的杀灭活性. 该光敏剂不仅克服了酞菁锌在水中溶解度低的问题, 且因所偶联的五聚赖氨酸对肿瘤细胞有靶向作用, 具有较高的杀灭肿瘤细胞活性. 相似文献
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Corrole光敏剂在光动力治疗中的重原子效应 总被引:1,自引:1,他引:0
最近, 我们合成了一系列Corrole衍生物, 经过鼻咽癌(Nasopharyngeal carcinoma,NPC) 细胞的体外PDT试验后, 筛选出了一个具有优良PDT活性的Corrole光敏剂. 本文报道该类Corrole光敏剂在PDT中的重原子效应. 相似文献
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通过成酰胺键的方式制备了一系列含羧基酞菁和白蛋白(牛血清白蛋白(BSA),人血清白蛋白(HSA))之间的共价结合物,所涉及到的酞菁分别是α-四(4-羧基苯氧基)酞菁锌(1)和α-四[4-(2-羧基乙基)苯氧基]酞菁锌(3),以及它们相应的β位四取代酞菁锌(化合物2和4).比较了游离酞菁以及它们的白蛋白结合物在磷酸盐缓冲溶液(PBS)中的光谱性质.结果表明,当酞菁被共价固定于白蛋白大分子上之后,展现出比游离酞菁更明显的单体特征吸收,而且结合物中的酞菁光谱特征不受体系pH值变化的影响.羧基在酞菁环上的取代位置,对酞菁与白蛋白结合前后的光谱转变幅度有影响,α位取代比β位取代更有利于光谱的变化.化合物1和3的白蛋白共价结合物在PBS溶液中甚至呈现出单体形式为主的光谱特征,Q带最大吸收波长分别位于697和706nm附近. 相似文献
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YU Qing HUANG Xuan ZHANG Tian WANG Weili YANG Dongliang SHAO Jinjun DONG Xiaochen 《高等学校化学研究》2021,37(4):951-959
The widespread use of high-dose antibiotics will not only lead to the rapid acquisition of antibiotic resistance and increased incidence of drug-resistant bacterial infections, but also produce toxic side effects on normal tissues. Herein, two near-infrared dyes BDP-4PTZ and BDP-4DPA were synthesized, and the electron donors of diphenylamine and phenothiazine with the only difference of sulphur(S)-lock between the two phenyl rings were introduced onto the electron acceptor aza-dipyrromethene boron difluoride(aza-BODIPY) through molecular surgery. Through co-precipitation into nanoparticles(NPs), BDP-4PTZ NPs and BDP-4DPA NPs were fabricated with good biocompatibility. Upon 660 nm photoirradiation, BDP-4PTZ NPs and BDP-4DPA NPs showed excellent photothermal conversion efficiency(43% and 50%, respectively) and reactive oxygen species(ROS) production performance(ca. 3.6 and 6 times higher than that of indocyanine green, respectively). In vitro antibacterial experiments indicated that both NPs could effectively destroy the bacteria's membrane to eradicate drug-resistant bacteria. Furthermore, the bacterial abscess was effectively eliminated after treatment with BDP-4DPA NPs under 660 nm photoirradiation without adverse effects. Thus, through molecular surgery, BDP-4DPA without the S-lock demonstrates synergistic photothermal and photodynamic antimicrobial activities, which is promising for further molecular design towards effective neo-antimicrobial phototherapy. 相似文献
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《Arabian Journal of Chemistry》2023,16(4):104583
Resistance to antimicrobial drugs is an impending healthcare problem of growing significance. In the post-antibiotic era, there is a huge push to develop new tools for effectively treating bacterial infections. Photodynamic therapy involves the use of a photosensitizer that is activated by the use of light of an appropriate wavelength in the presence of oxygen. This results in the generation of singlet oxygen molecules that can kill the target cells, including cancerous cells and microbial cells. Photodynamic therapy is shown to be effective against parasites, viruses, algae, and bacteria. To achieve high antimicrobial activity, a sufficient concentration of photosensitizer should enter the microbial cells. Generally, photosensitizers tend to aggregate in aqueous environments resulting in the weakening of photochemical activity and lowering their uptake into cells. Nanocarrier systems are shown to be efficient in targeting photosensitizers into microbial cells and improve their therapeutic efficiency by enhancing the internalization of photosensitizers into microbial cells. This review aims to highlight the basic principles of photodynamic therapy with a special emphasis on the use of nanosystems in delivering photosensitizers for improving antimicrobial photodynamic therapy. 相似文献
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Qingle Chen Yanhong Ma Jisi Zhao Mei Zhao Wenjing Li Qian Liu Li Xiong Wenjie Wu Zhangyong Hong 《中国化学快报》2018,29(7):1171-1178
A serial of peptide-conjugated zinc phthalocyanines with finely tuned structure modification were prepared and one optimized conjugate showed improved targeting towards tumors and abolished inoculated tumors with only a single PDT treatment in a subcutaneous xenograft tumor model, making this approach a promising therapeutic agent for the treatment of cancer. 相似文献
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Mengqi Yan Junlong Zhao Dan Sun Wei Sun Borui Zhang Wenting Deng Dandan Zhang Lanying Wang 《Tetrahedron》2017,73(24):3355-3362
Photodynamic therapy (PDT) represents a modern and noninvasive therapeutic approach, however, it relies on the development of photosensitizers. Here five new benzo[c,d]indole rhodamine complex merocyanines (BIRCM) D1-D5, displaying low dark toxicity and significant photo toxicity, were synthesized as PDT photosensitizers, and characterized by 1H NMR, IR, UV–Vis and HRMS. The investigation of their absorption spectra in different solvents showed that the absorption maxima and molar extinction coefficient were in the region 507–679 nm and 0.21 × 104–1.27 × 105 L · mol?1cm?1, respectively. The evaluation of PDT activity showed that only irradiation could not kill SMMC-7721 cells, and the cell survival rate and inhibition rate at the application dose and duration was 92%–87% and 78%–49%, respectively. Especially, using D2, absorbed in the red zone, as photosensitizer for PDT analyzed its effect on SMMC-7721 cells survival, it could be found that the cell survival rate was 92% without irradiating and the cell inhibited rate was 78% under irradiating at concentrations of 2.5 × 10?6 mol/L, displaying low dark toxicity and high photo toxicity, which was valuable for PDT of some microvascular diseases or other superficial diseases. 相似文献
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Hooi Ling Kee Jayeeta Bhaumik James R. Diers Pawel Mroz Michael R. Hamblin David F. Bocian Jonathan S. Lindsey Dewey Holten 《Journal of photochemistry and photobiology. A, Chemistry》2008,200(2-3):346-355
The photophysical properties of four imidazolium-substituted metalloporphyrins have been assessed to gain insights into the relative efficacy of the compounds for photodynamic therapy (PDT). A set of zinc(II), palladium(II), and chloro-indium(III) porphyrins all bear a net positive charge owing to the diethylimidazolium unit; one zinc chelate bears a negative charge owing to a bis(sulfobutyl)imidazolium unit. The photophysical properties of the cationic and anionic zinc porphyrins are very similar to one another in organic solvents, phosphate-buffered saline, and in the presence of bovine serum albumin. The properties of the zinc and palladium porphyrins bearing charged peripheral groups are generally similar to those of neutral analogs in organic solvents. The palladium porphyrin shows an essentially quantitative yield (≥0.99) of the triplet excited state compared to the zinc porphyrins (0.9), and all are quantitatively quenched (at the diffusion limit) by molecular oxygen in air-saturated fluid solution. If the rate constant and yield of quenching of the triplet excited state by energy or electron transfer to molecular oxygen is the same in the cellular environment as in solution, then these processes combined with the triplet yield contribute only a factor of 1.3 to the higher PDT activity of analogous palladium versus zinc porphyrins, which is much smaller than what is observed. Therefore, other factors such as transient reduction of the excited porphyrin or delivery to the target site must predominantly underlie the difference in PDT efficacy of these sensitizers. 相似文献