PMID- 33631267
OWN - NLM
STAT- MEDLINE
DCOM- 20210806
LR  - 20211204
IS  - 1879-0003 (Electronic)
IS  - 0141-8130 (Linking)
VI  - 178
DP  - 2021 May 1
TI  - Preparation, development and characterization of Leucaena leucocephala 
      galactomannan (LLG) conjugated sinapic acid: A potential colon targeted prodrug.
PG  - 29-40
LID - S0141-8130(21)00423-2 [pii]
LID - 10.1016/j.ijbiomac.2021.02.132 [doi]
AB  - Sinapic acid (SA), a widely prevalent hydroxycinnamic acid, possess numerous 
      biological activities owing to its antioxidant property. The present study was 
      aimed to prepare colon targeted polysaccharidic/polymeric ester prodrug of SA (a 
      microbially triggered system) using Leucaena leucocephala galactomannan (LLG) as 
      a polysaccharidic carrier. The polymeric conjugates of SA-LLG were found to 
      exhibit an increase in % yield and DS with increase in amount of SA and volume of 
      thionyl chloride. The degree of depolymerization of SA-LLG prodrug batches were 
      evaluated using optimized concentration of galactomannase. The SA-LLG prodrug was 
      characterized employing UV and FTIR spectroscopy, (1)H NMR and XRD. In vitro 
      release study of the optimized prodrug batch (SL10) suggested stable nature of 
      SA-LLG conjugate under acidic (pH 1.2) and alkaline conditions (pH 6.8). The 
      treatment of prodrug with galactomannase (15 mg/mL) followed by esterase 
      (10 U/mL) enzyme released approximately 81% of SA after 24 h. The cell viability 
      results revealed that free SA and SA-LLG were found to have similar 
      antiproliferative potential against human colon cancer cell lines (HCT-116 
      cells). Our investigation revealed that polysaccharidic prodrug, SA-LLG, has the 
      potential for colon targeting of SA and thus can be employed for the treatment of 
      Inflammatory Bowel Diseases (IBDs).
CI  - Copyright (c) 2021 Elsevier B.V. All rights reserved.
FAU - Kaur, Jasleen
AU  - Kaur J
AD  - Department of Pharmaceutical Sciences and Drug Research, Punjabi University, 
      Patiala, India.
FAU - Mehta, Vikrant
AU  - Mehta V
AD  - Laboratory of Molecular Medicine, Department of Human Genetics and Molecular 
      Medicine, Central University of Punjab, Bathinda, India.
FAU - Kaur, Gurpreet
AU  - Kaur G
AD  - Department of Pharmaceutical Sciences and Drug Research, Punjabi University, 
      Patiala, India. Electronic address: kaurgpt@gmail.com.
LA  - eng
PT  - Journal Article
DEP - 20210222
PL  - Netherlands
TA  - Int J Biol Macromol
JT  - International journal of biological macromolecules
JID - 7909578
RN  - 0 (Coumaric Acids)
RN  - 0 (Mannans)
RN  - 0 (Prodrugs)
RN  - 11078-30-1 (galactomannan)
RN  - 68A28V6010 (sinapinic acid)
RN  - X2RN3Q8DNE (Galactose)
SB  - IM
MH  - Cell Proliferation/*drug effects
MH  - Coumaric Acids/*chemistry
MH  - Fabaceae/*chemistry
MH  - Galactose/analogs & derivatives
MH  - HCT116 Cells
MH  - Humans
MH  - Mannans/*chemistry
MH  - *Prodrugs/chemical synthesis/pharmacology
OTO - NOTNLM
OT  - Enzymatic degradation
OT  - Esterase
OT  - Galactomannase
OT  - Leucaena leucocephala galactomannan
OT  - Polymeric prodrug
OT  - Sinapic acid
COIS- Declaration of competing interest None.
EDAT- 2021/02/26 06:00
MHDA- 2021/08/07 06:00
CRDT- 2021/02/25 20:10
PHST- 2020/11/11 00:00 [received]
PHST- 2021/02/17 00:00 [revised]
PHST- 2021/02/17 00:00 [accepted]
PHST- 2021/02/26 06:00 [pubmed]
PHST- 2021/08/07 06:00 [medline]
PHST- 2021/02/25 20:10 [entrez]
AID - S0141-8130(21)00423-2 [pii]
AID - 10.1016/j.ijbiomac.2021.02.132 [doi]
PST - ppublish
SO  - Int J Biol Macromol. 2021 May 1;178:29-40. doi: 10.1016/j.ijbiomac.2021.02.132. 
      Epub 2021 Feb 22.