IP Library Granted Patent US 8,530,183
Granted Patent B2
US 8,530,183 · App. 13/158,011 · Granted Sep 10, 2013

Zinc sensors for cellular imaging

Inventors: Wen-Hong Li (Dallas, TX); Daliang Li (Dallas, TX)
Assignee: The Board of Regents of the University of Texas System
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Quick Facts
Patent No.
US 8,530,183
App. No.
13/158,011
Granted
Sep 10, 2013
Kind
B2
Abstract

The present invention provides compounds for use as zinc ligand sensors in cellular imaging. These compounds are sensitive imaging agents that can be used with techniques such a laser scanning microscopy in intact cells in culture or in tissue preparations.

Claims (60)

1. A method of detecting zinc ion (Zn 2+ ) release by a cell comprising:

(a) contacting a cell with a compound having the formula:

wherein

R 1 and R 4 are independently H, or —CH 2 (CH 2 ) a COOH, CH 2 (CH 2 ) b SO 3 H, wherein

a = is 0, 1 or 2 and b, 1, 2 or 3;

R 2 and R 3 are independently H, or linear or branched C 1-20 alkyl;

R 5 and R 6 are independently H, F, Cl, Br;

R7 is H, or linear or branched C 1-4 alkyl or acetate;

R8 and R9 are independently H, or linear or branched C 1-4 alkyl or acetate; and

m is 1, 2 or 3;

n is 1, 2, 3 or 4; and

o is 1,2, 3 or 4;

and pharmaceutically acceptable salts thereof, and

(b) detecting fluorescence of said compound following zinc release by said cell and binding of zinc by said compound.

2. The method of claim 1 , wherein said cell is pancreatic beta cell, a submandibular salivary gland cell, a prostate epithelial cell, a paneth cell, a mast cell, a granulocyte, a pituitary cell, a or a CNS neuron.

3. The method of claim 1 , wherein detecting comprises confocal laser scanning microscopy, two photon laser scanning microscopy, or total internal reflection fluorescence microscopy.

4. The method of claim 1 , wherein said cell is an isolated cell.

5. The method of claim 1 , wherein said cell is in an intact tissue.

6. The method of claim 5 , wherein said tissue is an isolated pancreatic islet.

7. The method of claim 1 , further comprising detecting fluorescence at multiple time points.

8. The method of claim 1 , further comprising stimulating said cell with a zinc ion release agent.

9. The method of claim. 1 , wherein the concentration of said compound is between 1 nM and 100 μM.

10. The method of claim 1 , wherein the concentration is between 5 nM and 1 μM.

11. The method of claim 1 , wherein R 5 , R 6 , R 7 , R 8 and R 9 are H, in and n are 1 and o is 2.

12. The method of claim 11 wherein R 1 and R 4 are the same.

13. The method of claim 11 , wherein R 2 and R 3 are the same.

14. The method of claim 12 , wherein R 2 and R 3 are the same.

15. The method of claim 14 , wherein R 1 and R 4 are —CH 2 COOH, and R 2 and R 3 are —CH 2 CH 3 or —(CH 2 ) 11 CH 3 .

16. A compound having the formula:

wherein

R 1 and R 4 are independently H, or —CH 2 (CH 2 ) a COOH, CH 2 (CH 2 ) b SO 3 H, wherein a is 0, 1 or 2 and b 1, 2 or 3;

R 2 and R 3 are independently H, or linear or branched C 1-20 alkyl;

R 5 and R 6 are independently H, F, Cl, Br;

R7 is H, or linear or branched C 1-4 alkyl or acetate;

R8 and R9 are independently H, or linear or branched C 1-4 alkyl or acetate; and

m is 1, 2 or 3;

n is 1, 2, 3 or 4; and

o is 1 2, 3 or 4;

and pharmaceutically acceptable salts thereof.

17. The compound of claim 16 , wherein R 5 , R 6 , R 7 , R 8 and R 9 are H, m and n are 1 and o is 2.

18. The compound of claim 17 , wherein R 1 and R 4 are the same.

19. The compound of claim 17 , wherein R 2 and R 3 are the same.

20. The compound of claim 18 , wherein R 2 and R 3 are the same

21. The compound of claim 20 , wherein R 1 and R 4 are —CH 2 COOH and R 2 and R 3 are —CH 2 CH 3 or —(CH 2 ) 11 CH 3 .

22. A ligand metal complex having the formula:

wherein

R 1 and R 4 are independently H, or —CH 2 (CH 2 ) a COOH, CH 2 (CH 2 ) b SO 3 H, wherein a is 0, 1 or 2 and b 1, 2 or 3;

R 2 and R 3 are independently H, or linear or branched C 1-20 alkyl;

R 5 and R 6 are independently H, F, Cl, Br;

R7 is H, or linear or branched C 1-4 alkyl or acetate;

R8 and R9 are independently H, or linear or branched C 1-4 alkyl or acetate; and

m is 1, 2 or 3;

n is 1, 2, 3 or 4; and

o is 1, 2, 3 or 4;

and pharmaceutically acceptable salts thereof.

23. The ligand metal complex of claim 22 , wherein R 5 , R 6 , R 7 , R 8 and R 9 are H, m and n are 1 and o is 2.

24. The ligand metal complex of claim 23 , wherein R 1 and R 4 are the same.

25. The ligand metal complex of claim 23 , wherein R 2 and R 3 are the same.

26. The ligand metal complex of claim 24 . wherein R 2 and R 3 are the same

27. The ligand metal complex of claim 26 , wherein R 1 and R 4 are —CH 2 COOH and R 2 and R 3 are —CH 2 CH 3 or —(CH 2 ) 11 CH 3 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2011
From: LI, WEN-HONG; LI, DALIANG
To: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Reel/Frame 026937/0228 →
CONFIRMATORY LICENSE Recorded Aug 3, 2011
From: THE BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 026691/0843 →
Continuity (2)
Provisional Application 61353477 · Jun 10, 2010
Related Publication 20120009617A1 · Jan 12, 2012