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Drug Design, Development and Therapy Volume 10, 2016 - Issue
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Original Research

RGD(F/S/V)-Dex: towards the development of novel, effective, and safe glucocorticoids

Xueyun Jiang1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China
,
Ming Zhao1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China;2 Faculty of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, TaiwanCorrespondence[email protected] [email protected]
,
Yuji Wang1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China
,
Haimei Zhu1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China
,
Shurui Zhao1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China
,
Jianhui Wu1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of China
,
Yuanbo Song3 Guangxi Pusen Biotechnology Co. Ltd., Nanning, Guangxi, People’s Republic of China
&
Shiqi Peng1 Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, People’s Republic of ChinaCorrespondence[email protected] [email protected]
 show all
Pages 1059-1076 | Published online: 08 Mar 2016

Figures & data

Figure 1 Structure of RGDV-Dex, RGDS-Dex, and RGDF-Dex.

Abbreviations: RGDV, Arg-Gly-Asp-Val; RGDS, Arg-Gly-Asp-Ser; RGDF, Arg-Gly-Asp-Phe; Dex, dexamethasone.
Figure 1 Structure of RGDV-Dex, RGDS-Dex, and RGDF-Dex.

Figure 2 TEM images showing the effects of concentration.

Notes: (A) TEM images of 10−8, 10−10, and 10−12 M of RGDF-Dex in ultrapure water (pH 7.0); (B) TEM images of 10−8, 10−10, and 10−12 M of RGDS-Dex in ultrapure water (pH 7.0); (C) TEM images of 10−8, 10−10, and 10−12 M of RGDV-Dex in ultrapure water (pH 7.0).
Abbreviations: TEM, transmission electron microscope; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; RGDV, Arg-Gly-Asp-Val; Dex, dexamethasone.
Figure 2 TEM images showing the effects of concentration.

Figure 3 AFM images.

Notes: (A) AFM images of rat plasma alone; (B) AFM images of 10−8 M of RGDF-Dex in rat plasma; (C) AFM images of 10−8 M of RGDS-Dex in rat plasma; (D) AFM images of 10−8 M of RGDV-Dex in rat plasma; (E) AFM images of ultrapure water alone; (F) AFM images of 10−8 M of RGDF-Dex in ultrapure water; (G) AFM images of 10−8 M of RGDS-Dex in ultrapure water; (H) AFM images of 10−8 M of RGDV-Dex in ultrapure water. Inset in each figure shows magnified area identified by the red triangles.
Abbreviations: AFM, atomic force microscopy; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; RGDV, Arg-Gly-Asp-Val; Dex, dexamethasone.
Figure 3 AFM images.

Figure 4 Nanoproperties of 10−8 M solution of RGDF-Dex, RGDS-Dex, and RGDV-Dex in water.

Notes: (A) Faraday–Tyndall effect of RGDF-Dex: (i) in ultrapure water without laser beam irradiation, (ii) in pH 7.0 ultrapure water with 650 nm laser beam irradiation, (iii) in pH 2.0 ultrapure water with 650 nm laser beam irradiation; (B) Faraday–Tyndall effect of RGDS-Dex: (i) in ultrapure water without laser beam irradiation, (ii) in pH 7.0 ultrapure water with 650 nm laser beam irradiation, (iii) in pH 2.0 ultrapure water with 650 nm laser beam irradiation; (C) Faraday–Tyndall effect of RGDV-Dex: (i) in ultrapure water without laser beam irradiation, (ii) in pH 7.0 ultrapure water with 650 nm laser beam irradiation, (iii) in pH 2.0 ultrapure water with 650 nm laser beam irradiation; (D) Faraday–Tyndall effect of ultrapure water: (i) in pH 7.0 ultrapure water without laser beam irradiation, (ii) in pH 7.0 ultrapure water with 650 nm laser beam irradiation, (iii) in pH 2.0 ultrapure water with 650 nm laser beam irradiation; (E) size distribution of RGDF-Dex: (left) in pH 2.0 ultrapure water, (right) in pH 7.0 ultrapure water; (F) size distribution of RGDS-Dex: (left) in pH 2.0 ultrapure water, (right) in pH 7.0 ultrapure water; (G) size distribution of RGDV-Dex: (left) in pH 2.0 ultrapure water, (right) in pH 7.0 ultrapure water; (H) ζ-potential of RGDF-Dex in pH 7.0 ultrapure water; (I) ζ-potential of RGDS-Dex in pH 7.0 ultrapure water; (J) ζ-potential of RGDV-Dex in pH 7.0 ultrapure water.
Abbreviations: St dev, standard deviation; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; RGDV, Arg-Gly-Asp-Val; Dex, dexamethasone.
Figure 4 Nanoproperties of 10−8 M solution of RGDF-Dex, RGDS-Dex, and RGDV-Dex in water.

Figure 5 The effect of RGDV-Dex, RGDS-Dex, and RGDF-Dex on ConA-induced proliferation of the spleen lymphocytes of BALB/C mouse, n=3.

Abbreviations: Dex, dexamethasone; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; RGDV, Arg-Gly-Asp-Val; ConA, concanavalin; IC50, half maximal inhibitory concentration; SD, standard deviation.
Figure 5 The effect of RGDV-Dex, RGDS-Dex, and RGDF-Dex on ConA-induced proliferation of the spleen lymphocytes of BALB/C mouse, n=3.

Figure 6 The survival time of the implanted myocardium in the “pocket” near the distal edge of the ear of BALB/C mice, n=12.

Abbreviations: Dex, dexamethasone; CMCNa, carmellose sodium; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; CsA, cyclosporine A; SD, standard deviation.
Figure 6 The survival time of the implanted myocardium in the “pocket” near the distal edge of the ear of BALB/C mice, n=12.

Figure 7 Tail bleeding time of RGDV-Dex-, RGDS-Dex-, and RGDF-Dex-treated mice, n=12.

Abbreviations: CMCNa, carmellose sodium; Dex, dexamethasone; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; SD, standard deviation.
Figure 7 Tail bleeding time of RGDV-Dex-, RGDS-Dex-, and RGDF-Dex-treated mice, n=12.

Figure 8 Anti-thrombotic activities of Dex, RGDV-Dex, RGDS-Dex, and RGDF-Dex, n=12.

Abbreviations: CMCNa, carmellose sodium; Dex, dexamethasone; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; SD, standard deviation.
Figure 8 Anti-thrombotic activities of Dex, RGDV-Dex, RGDS-Dex, and RGDF-Dex, n=12.

Figure 9 Body weight of the treated BALB/C mice, n=12.

Abbreviations: Dex, dexamethasone; CMCNa, carmellose sodium; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; CsA, cyclosporine A; SD, standard deviation.
Figure 9 Body weight of the treated BALB/C mice, n=12.

Figure 10 Spleen index of the treated BALB/C mice, n=12.

Abbreviations: Dex, dexamethasone; CMCNa, carmellose sodium; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; CsA, cyclosporine A; SD, standard deviation.
Figure 10 Spleen index of the treated BALB/C mice, n=12.

Figure 11 Liver index of the treated BALB/C mice, n=12.

Abbreviations: Dex, dexamethasone; CMCNa, carmellose sodium; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; CsA, cyclosporine A; SD, standard deviation.
Figure 11 Liver index of the treated BALB/C mice, n=12.

Figure 12 Serum ALT levels of the mice on which acute toxicity assay was performed, n=12.

Abbreviations: ALT, alanine transaminase; CMCNa, carmellose sodium; Dex, dexamethasone; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; SD, standard deviation.
Figure 12 Serum ALT levels of the mice on which acute toxicity assay was performed, n=12.

Figure 13 AST levels of the mice on which acute toxicity assay was performed, n=12.

Abbreviations: AST, aspartate transaminase; CMCNa, carmellose sodium; Dex, dexamethasone; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; SD, standard deviation.
Figure 13 AST levels of the mice on which acute toxicity assay was performed, n=12.

Figure 14 Serum Cr levels of the mice on which acute toxicity assay was performed, n=12.

Abbreviations: Cr, creatinine; CMCNa, carmellose sodium; Dex, dexamethasone; RGDV, Arg-Gly-Asp-Val; RGDF, Arg-Gly-Asp-Phe; RGDS, Arg-Gly-Asp-Ser; SD, standard deviation.
Figure 14 Serum Cr levels of the mice on which acute toxicity assay was performed, n=12.

Figure S1 1HNMR of RGDV-Dex.

Abbreviations: 1HNMR, proton nuclear magnetic resonance; RGDV, Arg-Gly-Asp-Val; Dex, dexamethasone.
Figure S1 1HNMR of RGDV-Dex.

Figure S2 13C NMR of RGDV-Dex.

Abbreviations: 13C NMR, carbon-13 nuclear magnetic resonance; RGDV, Arg-Gly-Asp-Val; Dex, dexamethasone.
Figure S2 13C NMR of RGDV-Dex.

Figure S3 1H NMR of RGDS-Dex.

Abbreviations: 1H NMR, proton nuclear magnetic resonance; RGDS, Arg-Gly-Asp-Ser; Dex, dexamethasone.
Figure S3 1H NMR of RGDS-Dex.

Figure S4 13C NMR of RGDS-Dex.

Abbreviations: 13C NMR, carbon-13 nuclear magnetic resonance; RGDS, Arg-Gly-Asp-Ser; Dex, dexamethasone.
Figure S4 13C NMR of RGDS-Dex.

Figure S5 1H NMR of RGDF-Dex.

Abbreviations: 1H NMR, proton nuclear magnetic resonance; RGDF, Arg-Gly-Asp-Phe; Dex, dexamethasone.
Figure S5 1H NMR of RGDF-Dex.

Figure S6 13C NMR of RGDF-Dex.

Abbreviations: 13C NMR, carbon-13 nuclear magnetic resonance; RGDF, Arg-Gly-Asp-Phe; Dex, dexamethasone.
Figure S6 13C NMR of RGDF-Dex.

Figure S7 HPLC chromatogram of RGDF-Dex.

Note: Mobile phase: CH3OH: Water=15%:85%.
Abbreviations: HPLC, high performance liquid chromatography; RGDF, Arg-Gly-Asp-Phe; Dex, dexamethasone.
Figure S7 HPLC chromatogram of RGDF-Dex.

Figure S8 HPLC chromatogram of RGDV-Dex.

Note: Mobile phase: CH3OH: Water=15%:85%.
Abbreviations: HPLC, high performance liquid chromatography; RGDV, Arg-Gly-Asp-Val; Dex, dexamethasone.
Figure S8 HPLC chromatogram of RGDV-Dex.

Figure S9 HPLC chromatogram of RGDS-Dex.

Note: Mobile phase: CH3OH: Water=85%:15%
Abbreviations: HPLC, high performance liquid chromatography; RGDS, Arg-Gly-Asp-Ser; Dex, dexamethasone.
Figure S9 HPLC chromatogram of RGDS-Dex.

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