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Synthesis and Biological Evaluation of Danshensu and Tetramethylpyrazine Conjugates as Cardioprotective Agents.

Abstract Myocardial ischemia is a primary cause of sudden death worldwide. Numerous active ingredients of traditional Chinese medicines including danshensu (DSS) and tetramethylpyrazine (TMP) have been widely used for the treatment of myocardial ischemia. To enhance their therapeutic efficacy and improve their drugability, in this work, we designed new DSS and TMP conjugates. Their water solubility and protective effects were studied in vitro and in experimental animal models. The new compounds demonstrated higher activities than the positive control agents acetylated danshensu and tetramethylpyrazine conjugate (ADTM) and salvianolic acid B (SAB) in preventing cells from oxidative insult. Among the new compounds, 14, bearing two glycine moieties, was more water soluble. In addition, compound 14 was much more potent in preventing cells from oxidative injury, at least 10- and 20-fold as potent as ADTM and SAB, respectively. The protective effects of compound 14 may be attributed to its anti-radical activity and anti-apoptotic activity. These results suggest that compound 14 is a promising candidate for the treatment of myocardial ischemia.
PMID
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Authors

Mayor MeshTerms
Keywords
Journal Title chemical & pharmaceutical bulletin
Publication Year Start




PMID- 28381679
OWN - NLM
STAT- MEDLINE
DA  - 20170406
DCOM- 20170413
LR  - 20170413
IS  - 1347-5223 (Electronic)
IS  - 0009-2363 (Linking)
VI  - 65
IP  - 4
DP  - 2017
TI  - Synthesis and Biological Evaluation of Danshensu and Tetramethylpyrazine
      Conjugates as Cardioprotective Agents.
PG  - 381-388
LID - 10.1248/cpb.c16-00839 [doi]
AB  - Myocardial ischemia is a primary cause of sudden death worldwide. Numerous active
      ingredients of traditional Chinese medicines including danshensu (DSS) and
      tetramethylpyrazine (TMP) have been widely used for the treatment of myocardial
      ischemia. To enhance their therapeutic efficacy and improve their drugability, in
      this work, we designed new DSS and TMP conjugates. Their water solubility and
      protective effects were studied in vitro and in experimental animal models. The
      new compounds demonstrated higher activities than the positive control agents
      acetylated danshensu and tetramethylpyrazine conjugate (ADTM) and salvianolic
      acid B (SAB) in preventing cells from oxidative insult. Among the new compounds, 
      14, bearing two glycine moieties, was more water soluble. In addition, compound
      14 was much more potent in preventing cells from oxidative injury, at least 10-
      and 20-fold as potent as ADTM and SAB, respectively. The protective effects of
      compound 14 may be attributed to its anti-radical activity and anti-apoptotic
      activity. These results suggest that compound 14 is a promising candidate for the
      treatment of myocardial ischemia.
FAU - Wang, Yingfei
AU  - Wang Y
AD  - Institute of New Drug Research and Guangdong Province Key Laboratory of
      Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University
      College of Pharmacy.
FAU - Zhang, Xiaojing
AU  - Zhang X
FAU - Xu, Changjiang
AU  - Xu C
FAU - Zhang, Gaoxiao
AU  - Zhang G
FAU - Zhang, Zaijun
AU  - Zhang Z
FAU - Yu, Pei
AU  - Yu P
FAU - Shan, Luchen
AU  - Shan L
FAU - Sun, Yewei
AU  - Sun Y
FAU - Wang, Yuqiang
AU  - Wang Y
LA  - eng
PT  - Journal Article
PL  - Japan
TA  - Chem Pharm Bull (Tokyo)
JT  - Chemical & pharmaceutical bulletin
JID - 0377775
RN  - 0 (Cardiotonic Agents)
RN  - 0 (Lactates)
RN  - 0 (Pyrazines)
RN  - 4GF33A5PAJ (3,4-dihydroxyphenyllactic acid)
RN  - V80F4IA5XG (tetramethylpyrazine)
SB  - IM
MH  - Animals
MH  - Apoptosis/*drug effects
MH  - Cardiotonic Agents/*chemical synthesis/chemistry/*pharmacology
MH  - Cell Line
MH  - Disease Models, Animal
MH  - Dose-Response Relationship, Drug
MH  - Lactates/chemistry/*pharmacology
MH  - Male
MH  - Molecular Structure
MH  - Myocardial Ischemia/*drug therapy
MH  - Oxidative Stress/drug effects
MH  - Pyrazines/chemistry/*pharmacology
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Solubility
MH  - Structure-Activity Relationship
EDAT- 2017/04/07 06:00
MHDA- 2017/04/14 06:00
CRDT- 2017/04/07 06:00
AID - 10.1248/cpb.c16-00839 [doi]
PST - ppublish
SO  - Chem Pharm Bull (Tokyo). 2017;65(4):381-388. doi: 10.1248/cpb.c16-00839.

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