1351043-94-1Relevant articles and documents
Synthetic probes for in vitro purification and in vivo tracking of hepatocytes derived from human pluripotent stem cells
Park, Ji Young,Han, Jiyou,Jung, Hyo Sung,Lee, Gyunggyu,Kim, Hyo Jin,Cho, Gun-Sik,Park, Han-Jin,Han, Choongseong,Kim, Jong Seung,Kim, Jong-Hoon
, (2019)
Hepatocytes derived from human pluripotent stem cells (hPSCs) are promising candidates for cell therapy and drug discovery. However, it remains challenging to efficiently purify hepatocytes from undesired cell types after differentiation and to accurately monitor grafted cells after transplantation. Indocyanine Green (ICG), an FDA-approved, near-infrared (NIR) dye, has been used for various clinical purposes and is exclusively taken up by hepatocytes. However, ICG has a long emission wavelength (λem > 800 nm) that is beyond the detection range of fluorescence-activated cell sorting (FACS) systems. Moreover, it is easily eliminated from hepatocytes, hindering its application for NIR imaging. Here, we designed and synthesized two different probes based on the properties of ICG; 1) hepatocyte purifying agent (HPA, λem = 562 nm) for in vitro sorting and 2) hepatocyte imaging agent (HIA, λem = 817 nm) for efficient in vivo NIR imaging. We obtained highly enriched populations of hPSC-derived hepatocytes (hPSC-Heps) from various hPSC lines using HPA probe-based FACS purification. In addition, HIA labelling and NIR imaging allowed the direct visualization and tracking of grafted hPSC-Heps in animals with liver injuries. These results demonstrated that these two probes could be used as powerful tools with hPSC-Heps in both cell replacement therapy and drug screening.
Design, synthesis, and evaluation of monoamine oxidase A inhibitors–indocyanine dyes conjugates as targeted antitumor agents
Yang, Xiao-Guang,Mou, Yan-Hua,Wang, Yong-Jun,Wang, Jian,Li, Yan-Yu,Kong, Rui-Heng,Ding, Meng,Wang, Dun,Guo, Chun
, (2019)
Monoamine oxidase A (MAOA) is an important mitochondria-bound enzyme that catalyzes the oxidative deamination of monoamine neurotransmitters. Accumulating evidence suggests a significant association of increased MAOA expression and advanced high-grade prostate cancer (PCa) progression and metastasis. Herein, a series of novel conjugates combining the MAOA inhibitor isoniazid (INH) and tumor-targeting near-infrared (NIR) heptamethine cyanine dyes were designed and synthesized. The synthesized compounds G1–G13 were evaluated in vitro for their cytotoxicity against PC-3 cells using the MTT assay, and molecular docking studies were performed. Results showed that most tested compounds exhibited improved antitumor efficacy compared with INH. Moreover, conjugates G10 and G11 showed potent anticancer activity with IC50 values (0.85 and 0.4 μM respectively) comparable to that of doxorubicin (DOX). This may be attributable to the preferential accumulation of these conjugates in tumor cells. G10, G11, and G12 also demonstrated moderate MAOA inhibitory activities. This result and the results of molecular docking studies were consistent with their cytotoxicity activities. Taken together, these data suggest that a combination of the MAOA inhibitor INH with tumor-targeting heptamethine cyanine dyes may prove to be a highly promising tool for the treatment of advanced prostate cancer.
PROCESS FOR THE PREPARATION OF SODIUM 4-(2-((1E,3E,5E,7Z)-7-(1,1-DIMETHYL-3-(4-SULFONATOBUTYL)-1H-BENZO[e]INDOL-2(3H)-YLIDENE) HEPTA-1,3,5-TRIENYL)-1,1-DIMETHYL-1H-BENZO[e]INDOLIUM-3-YL) BUTANE-1-SULFONATE (INDOCYANINE GREEN)
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, (2019/11/19)
A process for the preparation of substantially pure Indocyanine green of formula with purity greater than 99.0% is provided. More particularly, the embodiments relate to the process for the preparation of Indocyanine green of formula and its intermediates thereof. It further provides crystalline form I of Indocyanine green of formula and process thereof.
Indocyanine green, and preparation method and application thereof
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Paragraph 0030-0032; 0035; 0036, (2017/07/01)
The invention provides indocyanine green, and a preparation method and application thereof. The indocyanine green is shown as formula 1. The method is performed according to a path recorded in the specification. According to the path, 2, 3, 3-trimethyl-4, 5-benzoindoles, 1, 4-butyl sultone and 2-glutarate diphenylamine hydrochloride, as raw materials, are compounded into the indocyanine green shown as the target compound formula 1. The method has a short compounding path, simple process and high yield, does not need heavy metal catalysis, and meets requirements of 'green chemical' development.
