التفاصيل البيبلوغرافية
العنوان: |
Synthesis and Evaluation of Galloyl Conjugates of Flavanones as BMP‑2 Upregulators with Promising Bone Anabolic and Fracture Healing Properties |
المؤلفون: |
Alka Raj Pandey (11301319), Divya Rai (11301322), Suriya Pratap Singh (11301325), Ashish Kumar Tripathi (11301328), Anirban Sardar (11301331), Alisha Ansari (7463396), Anjali Mishra (5087813), Sudha Bhagwati (11301334), Rabi Sankar Bhatta (451215), Mohammad Imran Siddiqi (514431), Naibedya Chattopadhyay (137586), Ritu Trivedi (137583), Koneni V. Sashidhara (1338594) |
سنة النشر: |
2021 |
المجموعة: |
Smithsonian Institution: Digital Repository |
مصطلحات موضوعية: |
Biophysics, Biochemistry, Medicine, Cell Biology, Genetics, Physiology, Pharmacology, Biotechnology, Developmental Biology, Cancer, Hematology, Space Science, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, Promising Bone Anabolic, 1 pM, bone formation rate, bone regeneration, fracture site, bone formation, pharmacokinetic studies, OCN, BMP, vehicle-treated rats, gene expression, osteoblast differentiation ability, bone anabolic, fracture defect model, hybridization concept, vivo studies |
الوصف: |
The molecular hybridization concept led us to design a series of galloyl conjugates of flavanones that have potent osteoblast differentiation ability in vitro and promote bone formation in vivo . An array of in vitro studies, especially gene expression of osteogenic markers, evinced compound 5e as the most potent bone anabolic agent, found to be active at 1 pM, which was then further assessed for its osteogenic potential in vivo . From in vivo studies on rat calvaria and a fracture defect model, we inferred that compound 5e , at an oral dose of 5 mg/(kg day), increased the expression of osteogenic genes (RUNX2, BMP-2, Col1, and OCN) and the bone formation rate and significantly promoted bone regeneration at the fracture site, as evidenced by the increased bone volume/tissue fraction compared with vehicle-treated rats. Furthermore, structure–activity relationship studies and pharmacokinetic studies suggest 5e as a potential bone anabolic lead for future osteoporosis drug development. |
نوع الوثيقة: |
article in journal/newspaper |
اللغة: |
unknown |
Relation: |
https://figshare.com/articles/journal_contribution/Synthesis_and_Evaluation_of_Galloyl_Conjugates_of_Flavanones_as_BMP_2_Upregulators_with_Promising_Bone_Anabolic_and_Fracture_Healing_Properties/15380461 |
DOI: |
10.1021/acs.jmedchem.1c00112.s001 |
الاتاحة: |
https://doi.org/10.1021/acs.jmedchem.1c00112.s001 |
Rights: |
CC BY-NC 4.0 |
رقم الانضمام: |
edsbas.6E98AB42 |
قاعدة البيانات: |
BASE |