PMID- 35116275
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20220501
IS  - 2219-6803 (Electronic)
IS  - 2218-676X (Print)
IS  - 2218-676X (Linking)
VI  - 10
IP  - 1
DP  - 2021 Jan
TI  - Acetylation may strengthen the antitumor activity of low molecular heparin.
PG  - 461-468
LID - 10.21037/tcr-20-2195 [doi]
AB  - BACKGROUND: To synthesize acetylated low anticoagulant low molecular weight 
      heparin (ALMWH) and to detect its antineoplastic activity. METHODS: We obtained 
      Low anticoagulant low molecular weight heparin (LMWH) by splitting unfractionated 
      heparin (UFH) with sodium periodate oxidation and sodium borohydride reduction, 
      then the LMWH was subjected to acetylate catalyzed by dicyclohexylcarbodiimide 
      and dimethylaminopyridine to produce ALMWH. The anti-proliferative activities 
      were determined on MDA-MB-231 human breast cancer cells in vitro. RESULTS: ALMWH 
      exhibited stranger anti-proliferative activity Compared with LMWH, In the 
      MDA-MB-231 cell line, the growth of MDA-MB-231 cells with IC50 of 22.16 microM at 48 
      h in a concentration-dependent and time-dependent manner, ALMWH produced stronger 
      inhibitory effects especially when it was used in low concentrations. By the use 
      of bulky catalysts, the acetylation site in the molecular chain of low molecular 
      weight heparin with a high selectivity, the synthesis process of Low 
      anticoagulant low molecular weight heparin can be easily controlled. Therefore, 
      large scale industrial production can be carried out. CONCLUSIONS: The 
      synthesized ALMWH possesses a high anti-proliferative activity, Chemical 
      modification of structure can endow LMWH with a high antiproliferative 
      activities. ALMWH is expected to enter clinical trials due to its high 
      druggability. Simultaneously, this study provides a basic method for screening of 
      antineoplastic drug with low toxicity.
CI  - 2021 Translational Cancer Research. All rights reserved.
FAU - Liang, Ying
AU  - Liang Y
AD  - Anhui Engineering Technology Research Center of Biochemical Pharmaceuticals, 
      Bengbu, China.
AD  - School of Pharmacy, Bengbu Medical College, Bengbu Anhui, China.
FAU - Wang, Yuanyuan
AU  - Wang Y
AD  - School of Basic Medical, Bengbu Medical College, Bengbu, China.
FAU - Wang, Guowen
AU  - Wang G
AD  - Department of Thoracic Surgery, the First Affiliated Hospital of Bengbu Medical 
      College, Bengbu, China.
FAU - Wang, Ansheng
AU  - Wang A
AD  - Department of Thoracic Surgery, the First Affiliated Hospital of Bengbu Medical 
      College, Bengbu, China.
FAU - Wang, Kangwu
AU  - Wang K
AD  - Department of Thoracic Surgery, the First Affiliated Hospital of Bengbu Medical 
      College, Bengbu, China.
FAU - Duan, Guixin
AU  - Duan G
AD  - Department of Thoracic Surgery, the First Affiliated Hospital of Bengbu Medical 
      College, Bengbu, China.
LA  - eng
PT  - Journal Article
PL  - China
TA  - Transl Cancer Res
JT  - Translational cancer research
JID - 101585958
PMC - PMC8798754
OTO - NOTNLM
OT  - Acetylated low molecular weight heparin (ALMWH)
OT  - MDA-MB-231 cells
OT  - antitumor
OT  - drug
OT  - heparan sulfate
COIS- Conflicts of Interest: All authors have completed the ICMJE uniform disclosure 
      form (available at http://dx.doi.org/10.21037/tcr-20-2195). The authors have no 
      conflicts of interest to declare.
EDAT- 2022/02/05 06:00
MHDA- 2022/02/05 06:01
PMCR- 2021/01/01
CRDT- 2022/02/04 05:48
PHST- 2020/04/26 00:00 [received]
PHST- 2021/01/02 00:00 [accepted]
PHST- 2022/02/04 05:48 [entrez]
PHST- 2022/02/05 06:00 [pubmed]
PHST- 2022/02/05 06:01 [medline]
PHST- 2021/01/01 00:00 [pmc-release]
AID - tcr-10-01-461 [pii]
AID - 10.21037/tcr-20-2195 [doi]
PST - ppublish
SO  - Transl Cancer Res. 2021 Jan;10(1):461-468. doi: 10.21037/tcr-20-2195.