PMID- 37308719
OWN - NLM
STAT- Publisher
LR  - 20231017
IS  - 1099-1573 (Electronic)
IS  - 0951-418X (Linking)
VI  - 37
IP  - 10
DP  - 2023 Oct
TI  - Bavachinin selectively modulates PPAR gamma and maintains bone homeostasis in Type 2 
      Diabetes.
PG  - 4457-4472
LID - 10.1002/ptr.7912 [doi]
AB  - Full peroxisome proliferator-activated receptor (PPAR) gamma agonists, 
      Thiazolidinediones (TZDs), effectively prevent the process of Type 2 Diabetes 
      Mellitus (T2DM), but their side effects have curtailed use in the clinic, 
      including weight gain and bone loss. Here, we identified that a selective PPAR gamma 
      modulator, Bavachinin (BVC), isolated from the seeds of Psoralea Corylifolia L., 
      could potently regulate bone homeostasis. MC3T3-E1 pre-osteoblast cells and 
      C3H10T1/2 mesenchymal stem cells were assessed for osteogenic differentiation 
      activities, and receptor activator of NF-kappaB ligand (RANKL)-induced RAW 264.7 
      cells were assessed osteoclasts formation. Leptin receptor-deficient mice and 
      diet-induced obesity mice were applied to evaluate the effect of BVC on bone 
      homeostasis in vivo. Compared to full PPAR gamma agonist rosiglitazone, BVC 
      significantly increased the osteogenesis differentiation activities under normal 
      and high glucose conditions in MC3T3-E1 cells. Moreover, BVC could alleviate 
      osteoclast differentiation in RANKL-induced RAW 264.7 cells. In vivo, synthesized 
      BVC prodrug (BN) has been applied to improve water solubility, increase the 
      extent of oral absorption of BVC and prolong its residence time in blood 
      circulation. BN could prevent weight gain, ameliorate lipid metabolism disorders, 
      improve insulin sensitivity, and maintain bone mass and bone biomechanical 
      properties. BVC, a unique PPAR gamma selective modulator, could maintain bone 
      homeostasis, and its prodrug (BN) exhibits insulin sensitizer activity while 
      circumventing the side effects of the TZDs, including bone loss and undesirable 
      weight gain.
CI  - (c) 2023 John Wiley & Sons Ltd.
FAU - Liu, Jingwen
AU  - Liu J
AD  - Experiment Center for Science and Technology, Shanghai University of Traditional 
      Chinese Medicine, Shanghai, People's Republic of China.
FAU - Li, Xiaoye
AU  - Li X
AD  - School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 
      Shanghai, People's Republic of China.
FAU - Wang, Hong
AU  - Wang H
AD  - School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 
      Shanghai, People's Republic of China.
FAU - Ren, Yan
AU  - Ren Y
AD  - Experiment Center for Science and Technology, Shanghai University of Traditional 
      Chinese Medicine, Shanghai, People's Republic of China.
FAU - Li, Yiming
AU  - Li Y
AD  - School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 
      Shanghai, People's Republic of China.
FAU - Guo, Fujiang
AU  - Guo F
AUID- ORCID: 0000-0003-4073-4773
AD  - School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 
      Shanghai, People's Republic of China.
LA  - eng
GR  - 81872763/National Natural Science Fund of China/
PT  - Journal Article
DEP - 20230612
PL  - England
TA  - Phytother Res
JT  - Phytotherapy research : PTR
JID - 8904486
SB  - IM
OTO - NOTNLM
OT  - Bavachinin
OT  - bone homeostasis
OT  - peroxisome proliferator-activated receptor gamma
OT  - thiazolidinediones
EDAT- 2023/06/13 01:13
MHDA- 2023/06/13 01:13
CRDT- 2023/06/12 23:27
PHST- 2023/04/25 00:00 [revised]
PHST- 2023/01/03 00:00 [received]
PHST- 2023/05/19 00:00 [accepted]
PHST- 2023/06/13 01:13 [pubmed]
PHST- 2023/06/13 01:13 [medline]
PHST- 2023/06/12 23:27 [entrez]
AID - 10.1002/ptr.7912 [doi]
PST - ppublish
SO  - Phytother Res. 2023 Oct;37(10):4457-4472. doi: 10.1002/ptr.7912. Epub 2023 Jun 
      12.