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<p>Modifying ICCA with Trp-Phe-Phe to Enhance in vivo Activity and Form Nano-Medicine</p>

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Figure 1 In vivo activities of Trp-Phe-Phe (WFF), n=12: (WFF to serum P-selectin of arterial thrombosis rats; (Abbreviation:A) anti-tumor activity of WFF against S180 mice; (B) anti-thrombotic activity of WFF on rat model; (C) inhibition ofD) inhibition of
Figure 2 Docking feature of ICCA and ICCA-WFF in the active site of P-selectin and GPIIb/IIIa: (A) docking feature of ICCA and ICCA-WFF in the active site of P-selectin;(B) docking feature of ICCA and ICCA-WFF in the active site of GPIIb/IIIa.Abbreviations: ICCA, 1-(4-isopropylphenyl)-β-carboline-3-carboxylic acid; ICCA-WFF, 1-(4-isopropylphenyl)-β-carboline-3-carbonyl-Trp-Phe-Phe.
Figure 3 Synthetic route of ICCA-WFF: i) TFA, CHhydrochloride in ethyl acetate (4M); vi) Pd/C and H2Cl2; ii) SeO2, 1,4-dioxane and 70 °C; iii) aqueous NaOH (2M), 1,4-dioxane and 0°C; iv) anhydrous THF, HOBt, DCC; v)2.Abbreviations: ICCA, 1-(4-isopropylphenyl)-β-carboline-3-carboxylic acid; TFA, trifluoroacetic acid;CH2Cl2, dichloromethane;SeO2, selenium dioxide; NaOH, sodiumhydroxide; THF, tetrahydrofuran; HOBt, 1-Hydroxybenzotriazole; ICCA-WFF, 1-(4-isopropylphenyl)-β-carboline-3-carbonyl-Tyr-Phe-Phe.
Figure 5 Tyndall effect of ICCA-WFFinvarious aqueous: (solution of ICCA-WFF in ultrapure water of pH 7.4 with 650 nm laser radiation.Abbreviation:pH 7.4 without radiation; (solution of ICCA-WFF in ultrapure waterof pH 6.8 without radiation; (ICCA-WFF in ultrapure waterof pH 5.8 with 650 nm laser radiation; (of ICCA-WFF in ultrapure water of pH 2.0 without radiation; (A)ultrapurewaterof pH2.0 withoutradiation; (B)ultrapurewaterof pH2.0 with 650 nm laser radiation; (C) 3.7μM solutionD) 3.7 μM solution of ICCA-WFF in ultrapure water of pH 2.0 with 650 nm laser radiation; (E) ultrapure water of pH 5.8without radiation; (F) ultrapure water of pH 5.8 with 650 nm laser radiation; (G) 3.7 μM solution of ICCA-WFF in ultrapure water of pH 5.8 without radiation; (H) 3.7 μM solution ofI) ultrapure waterof pH 6.8 withoutradiation; (J) ultrapure waterof pH6.8 with 650 nm laser radiation; (K) 3.7 μML) 3.7 μM solution of ICCA-WFF in ultrapure waterof pH 6.8 with 650 nm laser radiation; (M) ultrapure waterofN) ultrapure water of pH 7.4 with 650 nm laser radiation; (O) 3.7 μM solution of ICCA-WFF in ultrapure water of pH 7.4 without radiation; (P) 3.7 μM ICCA-WFF, 1-(4-isopropylphenyl)-β-carboline-3-carbonyl-Tyr-Phe-Phe.
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