FEATURED STORY Peptide Has Promise for Treating Spinal Cord Injury     read at        http://www.dddmag.com/news/2014/12/peptide-has-promise-treating-spinal-cord-injury?et_cid=4300209&et_rid=523035093&type=cta

Case Western Reserve scientists have developed a new chemical compound that shows extraordinary promise in restoring function lost to spinal cord injury. The compound, which the researchers dubbed intracellular sigma peptide (ISP), allowed paralyzed muscles to activate in more than 80 percent of the animals tested. Read more... FULL STORY

Antibacterial activities and antioxidant capacity of Aloe vera

Antibacterial activities and antioxidant capacity of Aloe vera

Fatemeh Nejatzadeh-Barandozi

• Correspondence: Fatemeh Nejatzadeh-Barandozifnejatzadeh@yahoo.com

Department of Horticulture, Faculty of Agriculture, Khoy Branch, Islamic Azad University, P.O. Box 58168–44799, Khoy, Ira
http://www.orgmedchemlett.com/content/3/1/5

Organic and Medicinal Chemistry Letters 2013, 3:5  doi:10.1186/2191-2858-3-5

The electronic version of this article is the complete one and can be found online at:http://www.orgmedchemlett.com/content/3/1/5

Background

The aim of this study was to identify, quantify, and compare the phytochemical contents, antioxidant capacities, and antibacterial activities of Aloe vera lyophilized leaf gel (LGE) and 95% ethanol leaf gel extracts (ELGE) using GC-MS and spectrophotometric methods.

EU approves Lilly diabetes drug Trulicity, dulaglutide

EU approves Lilly diabetes drug Trulicity, dulaglutide

Regulators in Europe have given the green light to Eli Lilly’s Trulicity, its once-weekly glucagon-like peptide-1 receptor agonist for type 2 diabetes.

Read more at: http://www.pharmatimes.com/Article/14-11-25/EU_approves_Lilly_diabetes_drug_Trulicity.aspx

Dulaglutide is a glucagon-like peptide 1 receptor agonist (GLP-1 agonist) for the treatment of type 2 diabetes that can be used once weekly.[1][2]GLP-1 is a hormone that is involved in the normalization of level of glucose in blood (glycemia). The FDA approved dulaglutide for use in the United States in September 2014.[3] The drug is manufactured by Eli Lilly under the brand name Trulicity.[3]

Mechanism of action

Dulaglutide binding to glucagon-like peptide 1 receptor, slows gastric emptying and increases insulin secretion by beta cells in the pancreas. Simultaneously the compound reduces the elevated glucagon secretion by alpha cells of the pancreas, which is known to be inappropriate in the diabetic patient. GLP-1 is normally secreted by L cells of the gastrointestinal mucosa in response to a meal.[4]

Medical uses[

The compound is indicated for adults with type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control. Dulaglutide is not indicated in the treatment of subjects with type 1 diabetes mellitus or patients with diabetic ketoacidosis. Dulaglutide can be used either stand-alone or in combination with other medicines for type 2 diabetes, in particularmetformin, sulfonylureas, thiazolidinediones, and insulin taken concomitantly with meals.[5]

Side effects

The most common side effects include gastrointestinal disorders, such as dyspepsia,decreased appetite, nausea, vomiting, abdominal pain, diarrhea.[6] Some patients may experience serious adverse reactions: acute pancreatitis (symptoms include persistent severe abdominal pain, sometimes radiating to the back and accompanied by vomiting),hypoglycemia, renal impairment (which may sometimes require hemodialysis). The risk of hypoglycemia is increased if the drug is used in combination with sulfonylureasorinsulin.[7][8]

Contraindications

The compound is contraindicated in subjects with hypersensitivity to active principle or any of the product’s components. As a precautionary measure patients with a personal or family history of medullary thyroid carcinoma or affected by multiple endocrine neoplasia syndrometype 2 should not take dulaglutide, because for now it is unclear whether the compound can increase the risk of these cancers.[9]

References

1. JCourtney Aavang Tibble, Tricia Santos Cavaiola, Robert R Henry (2013). “Longer Acting GLP-1 Receptor Agonists and the Potential for Improved Cardiovascular Outcomes: A Review of Current Literature”. Expert Rev Endocrinol Metab 8 (3): 247–259.doi:10.1586/eem.13.20.
2.  “Lilly’s Once-Weekly Dulaglutide Shows Non-Inferiority to Liraglutide in Head-to-Head Phase III Trial for Type 2 Diabetes”. Eli Lilly. Feb 25, 2014.
3.  “FDA approves Trulicity to treat type 2 diabetes” (Press release). FDA. Sep 18, 2014.
4.  Nadkarni P, Chepurny OG, Holz GG (2014). “Regulation of glucose homeostasis by GLP-1″. Prog Mol Biol Transl Sci 121: 23–65. doi:10.1016/B978-0-12-800101-1.00002-8.PMC 4159612. PMID 24373234. Retrieved 2014-09-29.
5.  Terauchi Y, Satoi Y, Takeuchi M, Imaoka T (July 2014). “Monotherapy with the once weekly GLP-1 receptor agonist dulaglutide for 12 weeks in Japanese patients with type 2 diabetes: dose-dependent effects on glycaemic control in a randomised, double-blind, placebo-controlled study”. Endocr. J. PMID 25029955. Retrieved 2014-09-29.
6.  Nauck M, Weinstock RS, Umpierrez GE, Guerci B, Skrivanek Z, Milicevic Z (August 2014). “Efficacy and safety of dulaglutide versus sitagliptin after 52 weeks in type 2 diabetes in a randomized controlled trial (AWARD-5)”. Diabetes Care 37 (8): 2149–58.doi:10.2337/dc13-2761. PMID 24742660.
7.  Amblee A (April 2014). “Dulaglutide for the treatment of type 2 diabetes”. Drugs Today50 (4): 277–89. doi:10.1358/dot.2014.50.4.2132740. PMID 24918645.
8.  Monami M, Dicembrini I, Nardini C, Fiordelli I, Mannucci E (February 2014). “Glucagon-like peptide-1 receptor agonists and pancreatitis: a meta-analysis of randomized clinical trials”. Diabetes Res. Clin. Pract. 103 (2): 269–75.doi:10.1016/j.diabres.2014.01.010.PMID 24485345.
9. Samson SL, Garber A (April 2013). “GLP-1R agonist therapy for diabetes: benefits and potential risks”. Curr Opin Endocrinol Diabetes Obes 20 (2): 87–97.doi:10.1097/MED.0b013e32835edb32. PMID 23403741. Retrieved 2014-09-30.

IDENTIFIERS
CAS NUMBER	923950-08-7
ATC CODE	None
CHEMICAL DATA
FORMULA	C2646H4044N704O836S18
MOL. MASS	59669.81 g/mol

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL  

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO .....FOR BLOG HOME CLICK HERE

Join me on Linkedin

Join me on Facebook FACEBOOK

Join me on twitter

Join me on google plus Googleplus

 amcrasto@gmail.com

 

KEBUZONE…….An antirheumatic agent.

KEBUZONE…….An antirheumatic agent.

Kebuzone (or ketophenylbutazone) is a non-steroidal anti-inflammatory drug.

Structural formula

4-(3-oxobutyl)-1,2-diphenylpyrazolidine-3,5-dione

UNII-4VD83UL6Y6

853-34-9

4-(3-Oxobutyl)-1,2-diphenyl-3,5-pyrazolidinedione

Additional Names: 1,2-diphenyl-4-(g-ketobutyl)-3,5-pyrazolidinedione; 1,2-diphenyl-4-(3¢-oxobutyl)-3,5-dioxopyrazolidine; ketophenylbutazone; KPB

Trademarks: Chebutan; Chepirol; Chetazolidin (Zeria); Chetil; Copirene; Ketason; Ketazone (Beytout); Pecnon (Sanken); Phloguron (Steiner); Recheton

MF: C19H18N2O3

MW: 322.36

Percent Comp: C 70.79%, H 5.63%, N 8.69%, O 14.89%

Properties: Crystals, mp 115.5-116.5° or 127.5-128.5° depending on cryst form.

Melting point: mp 115.5-116.5° or 127.5-128.5° depending on cryst form

Therap-Cat: Antirheumatic.

1. BRN 0308507
2. Chebutan
3. Chepirol
4. Chetazolidin
5. Chetil
6. Copirene
7. EINECS 212-715-7
8. Hichillos
9. Kebuzone
10. Kebuzonum
11. Kebuzonum [INN-Latin]
12. Keobutane-jade
13. Ketason
14. Ketazone
15. Ketophenylbutazone
16. Ketophenylbutazonum
17. KPB
18. Pecnon
19. Quebuzona
20. Quebuzona [INN-Spanish]
21. Recheton
22. UNII-4VD83UL6Y6

Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions.They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.

UV – range

Conditions : Concentration – 1 mg / 100 ml
THE SOLVENT DESIGNATION GRAPHICS	METHANOL	WATER	0.1М HCL	0.1M NAOH
Maximum absorption	244 nm	-	237 nm	262 nm
	448	-	404	617
e	14440	-	13020	19890

IR – spectrum

WAVELENGTH (ΜM)
WAVE NUMBER (CM -1 )

Reference

• UV and IR Spectra. H.-W. Dibbern, R.M. Muller, E. Wirbitzki, 2002 ECV
• NIST/EPA/NIH Mass Spectral Library 2008
• Handbook of Organic Compounds. NIR, IR, Raman, and UV-Vis Spectra Featuring Polymers and Surfactants, Jr., Jerry Workman. Academic Press, 2000.
• Handbook of ultraviolet and visible absorption spectra of organic compounds, K. Hirayama. Plenum Press Data Division, 1967.

Brief background information

SALT	ATC	FORMULA	MM	CAS
-	M01AA06	C 19 H 18 N 2 O 3	322.36 g / mol	853-34-9

4-(3-oxobutyl)-1,2-di(phenyl)pyrazolidine-3,5-dione
CLINICAL DATA
LEGAL STATUS	?
IDENTIFIERS
CAS NUMBER	853-34-9
ATC CODE	M01AA06
PUBCHEM	CID 3824
CHEMSPIDER	3692
UNII	4VD83UL6Y6
KEGG	D01567
CHEBI	CHEBI:31749
CHEMICAL DATA
FORMULA	C19H18N2O3
MOL. MASS	322.35782 g/mol

Application

• anti-inflammatory
• antirheumatic
• Synthesis pathway

SYNTHESIS OF A)
SYNTHESIS B)

Trade names

COUNTRY	TRADE NAME	MANUFACTURER
Germany	Kebuzon	Steiner
France	Ketazon	Beytout
Italy	Chetopir	Sarm
Ukraine	no	no

Formulations

• ampoules of 1 g / 5 ml;
• 250 mg capsule

Reference

1. Synthesis of a)
   • Denss, R. et al .: Helv. Chim. Acta (HCACAV) 40, 402 (1957).
   1. material:
      • Kühn, M .: J. Prakt. Chem. (JPCEAO) 156 (II), 103 (1940).
2. Synthesis b)
   • AT 198 263 (Synfarma; appl. 1955).

References: Prepn: Deuss et al., US 2910481 (1959 to Geigy).

Review of pharmacology: Horakova et al.,Pharmacotherapeutica 1950-1959, 335-350 (1963), C.A. 60, 6072g (1964).

Metabolism: Nemecek et al., Arzneim.-Forsch. 16,1339 (1966); Queisnerova, Nemecek,Cesk. Farm. 20, 55 (1971), C.A. 75, 47077u (1971).

Herrenknecht, Christine; Guernet-Nivaud, Elisabeth; Lafont, Olivier; Guernet, Michel; Gueutin, Claire
Canadian Journal of Chemistry, 1988 ,  v. 66, pg. 1199 – 1202

Cizmarik; Lycka
Pharmazie, 1988 ,  v. 43,  11  pg. 794 – 795

Gueutin-Pelinard, Claire; Nivaud, Elisabeth; Boucly, Patrick; Guernet, Michel
Canadian Journal of Chemistry, 1981 ,  v. 59, pg. 759 – 762

Denss et al.
Helvetica Chimica Acta, 1957 ,  v. 40, pg. 402,406

Patent: CS124279 , 1965 ;Chem.Abstr., 1968 ,  v. 69,   52134r

SPOFA; United Pharmaceutical Work Patent: FR1500627 , 1965 ;Chem.Abstr., 1968 ,  v. 69,   96715k

Nippon Shinyaju Co., Ltd. Patent: US5811547 A1, 1998 ;

Fisnerova,L. et al. Collection of Czechoslovak Chemical Communications, 1974 ,  v. 39, pg. 624 – 633

Share this: