Synthesis and biological evaluation of a gamma-cyclodextrin-based formulation of the anticancer agent 5,6,11,12,17,18,23,24-octahydrocyclododeca[1,2-b:4,5-b':7,8-b'':10,11-b''']tetraindole (CTet).

نویسندگان

  • Simone Lucarini
  • Mauro De Santi
  • Francesca Antonietti
  • Giorgio Brandi
  • Giuseppe Diamantini
  • Alessandra Fraternale
  • Maria Filomena Paoletti
  • Andrea Tontini
  • Mauro Magnani
  • Andrea Duranti
چکیده

5,6,11,12,17,18,23,24-Octahydrocyclododeca[1,2-b:4,5-b':7,8-b'':10,11- b''']tetrai ndole (CTet), an indole-3-carbinol (I3C) metabolite endowed with anticancer properties, is poorly soluble in the solvents most frequently used in biological tests. This study indicates that the use of gamma-cyclodextrin (gamma-CD) avoids this problem. Formulated with gamma-CD CTet is a potent inhibitor of DNA synthesis in both estrogen receptor positive (MCF-7) and estrogen receptor negative (MDA-MB-231) human breast cell lines (IC50 = 1.20 +/- 0.04 microM and 1.0 +/- 0.1 microM, respectively).

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis, Antinociceptive, Antiinflammatory and Antiepileptic Evaluation of Some Novel Indeno[1, 2-b] Quinoxalin-11-ylidenamines

       A series of novel indeno[1, 2-b]quinoxalin-11-ylidenamines 2-9 have been synthesized via condensation of indane[1, 2-b]quinoxalin-11-one (1) with various primary aromatic amines in presence of AcOH for 3 h. Compound 1 was synthesized by condensation of indane-1,2,3-trione with benzene-1,2-diamine in presence of AcOH. The synthesized compounds were characterized by IR, 1H-NMR, ...

متن کامل

A Novel Method to Detect β-Cyclodextrin Glucosyl Transferase (β-CGTase) Activity on Polyacrylamide Gels

b-cyclodextrin glucosyl transferase (b-CGTase) hydrolyses starch to produce b-cyclodextrin by transglycosylation (cyclization) activity. The conventional method for detection of b-CGTase activity is based on detecting starch hydrolysis by iodine staining. This method reveals all amylolytic enzymes, but can not discriminate them. In the present study, we introduce a new method for specific detec...

متن کامل

New and Efficient Rout for One Pot Synthesis of acenaphtho[1,2-b] quinoxalines

Acenaphtho derivatives have been reported as antitumor agents. So, the reaction of acenaphthylene-1,2-dione with 3,4-diaminobenzenethiol, and then with the alkyl chloride derivatives for the synthesis of acenaphtho [1,2-b] quinoxalines are reviewed. Excellent yields of the products, short reaction times and simple work-up are attractive features of this suitable protocol.

متن کامل

Evaluation of Some Methods for Preparing Glipizide-β-Cyclodextrin Inclusion Complexes

      Glipizide has been found to form inclusion complexes with β-cyclodextrin (β-CD) in solution and in solid state. The present study was undertaken to determine a suitable method for scaling up glipizide-β-CD inclusion complex formation and to evaluate the effect of some parameters on the efficiency of complexation. The solid inclusion complexes of glipizide and β-CD were prepared at a molar...

متن کامل

Cellulose sulfuric acid catalyzed multicomponent reaction for efficient synthesis of pyrimido and pyrazolo[4,5-b]quinolines under solvent-free conditions

Cellulose sulfuric acid was used as an efficient biopolymer-based catalyst for the synthesis of tetrahydropyrimido[4,5-b]quinoline-2,4,6-triones and hexahydro-2H-pyrazolo[5,4-b]quinoline-6-ones via three component reaction of aldehyde, 5,5-dimethyl-1,3-cyclohexadione and 6-amino-1,3-dimethyluracil or 5-amino-3-methyl-1-phenypyrazole under solvent-free conditions at 90 oC. The major advantages o...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Molecules

دوره 15 6  شماره 

صفحات  -

تاریخ انتشار 2010