- 15 the position escapes acetylprotoaescigenin 13 bit linear amino sulfonic acid substituted hypocrellin derivative and its preparation method and application
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The invention discloses a site-15 deacetylation and site-13 straight-chain sulfamic acid substituted hypocrellin derivative, a preparation method and application thereof. The structural general formula of the derivative is shown as the formula I (disclosed in the specification). The derivative is a novel hypocrellin derivative designed specially aiming at photodynamic medical treatment of micrangium diseases such as related retina macular degeneration, and the like. The maximum light absorption wavelength of the derivative is 58 nm, and the light tissue penetration depth in the wavelength range conforms to the focus depth of the micrangium diseases, meanwhile, the absorption spectrum of visual pigment is kept away as far as possible; and in addition, the derivative has optimized dual affiliation to fat and water and can be directly dissolved into normal saline to prepare intravenous injection solutions without complicated preparation technologies.
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Paragraph 0031; 0032
(2016/10/08)
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- Quantitative and site-directed chemical modification of hypocrellins toward direct drug delivery and effective photodynamic activity
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For photodynamic therapy (PDT) treatment of microvascular diseases, drugs are delivered via blood circulation and the targets are vasculature endothelial cells, for which the contradictory requirements of hydrophilicity and lipophilicity of the drugs have been achieved by liposome preparations. Herein, it is demonstrated that the drug delivery and target affinity are achieved by a single chemical compound, hypocrellin B (HB) derivative 6 selected from three novel aminoalkanesulfonic acid HB derivatives, 5-7. 6 exhibits a much higher PDT activity (IC50 = 22 nM) on human gastric carcinoma BGC823 cells than HB, while it has no cellular toxicity in the dark. On the basis of estimation of the clinically required concentration according to relative PDT activity and clinical criteria, it can be predicted that 6 is directly deliverable to and PDT effective on target cells. The enhanced red absorption and superhigh photoactivity suggest that 6 is more powerful for PDT of tumors than HB.
- Deng, Hong,Liu, Xin,Xie, Jie,Yin, Rong,Huang, Naiyan,Gu, Ying,Zhao, Jingquan
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experimental part
p. 1910 - 1919
(2012/05/20)
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- Methotrexate analogues. 32. Chain extension, α-carboxyl deletion, and γ-carboxyl replacement by sulfonate and phosphonate: Effect on enzyme binding and cell-growth inhibition
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Analogues of methotrexate (MTX) and aminopterin (AMT) with aminophosphonoalkanoic, aminoalkanesulfonic, and aminoalkanephosphonic acid side chains in place of glutamate were synthesized and tested as inhibitors of folylpolyglutamate synthetase (FPGS) from mouse liver. The aminophosphonoalkanoic acid analogues were also tested as inhibitors of dihydrofolate reductase (DHFR) from L1210 murine leukemia cells and as inhibitors of the growth of MTX-sensitive (L1210) and MTX-resistant (L1210/R81) cells in culture. The optimal number of CH2 groups in aminophosphonoalkanoic acid analogues of AMT was found to be two for both enzyme inhibition and cell growth inhibition but was especially critical for activity against FPGS. Deletion of the α-carboxyl also led to diminished anti-FPGS activity in comparison with previously studied homocysteic acid and 2-amino-4-phosphonobutyric acid analogues. In the aminoalkanesulfonic acid analogues of MTX without an α-carboxyl, anti-FPGS activity was low and showed minimal variation as the number of CH2 groups between the carboxamide and sulfonate moieties was changed from one to four. In similar aminoalkanephosphonic acid analogues of MTX, anti-FPGS activity was also low, was comparable for two and three CH2 groups between the carboxamide and phosphonate moieties, and was diminished by monoesterification of the phosphonate group. These effects demonstrate that the α-carboxyl group of folate analogues is involved in binding to the active site of FPGS, and that an α-carboxyl group should be retained as part of the structure of FPGS inhibitors.
- Rosowsky,Forsch,Moran,Kohler,Freisheim
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p. 1326 - 1331
(2007/10/02)
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- Probiotics. Antistaphylococcal and antifibrinolytic activities of omega amino and omega guanidinoalkanesulfonic acids
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A series of ;. aminoalkanesulfonic acid and ω guanidinoalkanesulfonic acids was tested for antistaphylococcal and antifibrinolytic activities. Most of the former and one of the latter class gave better protection against Staphylococcus aureus infections in mice than 4 aminobutyryl L histidine. Most of the ω aminoalkanesulfonic acids showed antifibrinolytic activity, one of them having activity equal to or greater than that of aminocaproic acid, whereas none of the ω guanidinoalkanesulfonic acids had significant antifibrinolytic activity.
- Fujii,Cook
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p. 502 - 505
(2007/10/05)
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