生物活性可以通过巨大的宏环封装来缓解葡萄糖皮质类药物诱导的骨质疏松症
Yuna Shang1, Qingrun Zhu2, Jiaming Ding3
1Academy of Interdisciplinary Studies on Intelligent Molecules, Tianjin Key Laboratory of Structure and Performance for Functional Molecules, College of Chemistry, Tianjin Normal University, Tianjin 300387, China.
概括
巨大的宏观循环有效地封装了生物活性,提高了它们的稳定性和疗效,用于再生医学. 这种新型的输送系统对治疗骨质疏松症和开发新的基于的药物充满希望.
科学领域:
- 生物材料科学 生物材料科学
- 再生医学是一种再生医学.
- 超分子化学 超分子化学
背景情况:
- 生物活性对于组织工程至关重要,但面临着不稳定性和短半衰期等挑战.
- 现有的输送方法限制了这些的体内和临床应用.
研究的目的:
- 开发一种新的策略,利用巨型宏观循环封装生物活性.
- 为了评估-宏循环复合物的骨再生功效.
主要方法:
- 合成了四[4] (4) 作为一个巨大的宏循环宿主.
- 复杂的血小板衍生生长因子 (PDGF) 模仿 (Nap-FFGVRKKP, P) 具有宏循环 4.
- 通过结合常数和体外/体内生物活性评估复合物形成.
主要成果:
- 四[4] (4) 与P形成了一个稳定的复合体 (Ka = 1.16 × 107 M-1).
- P+4复合物显著促进了骨髓 stromal 细胞 (BMSC) 增殖 (2.27x) 和保护细胞免受德甲诱导的死亡 (76.94%).
- 在体内研究表明,P+4显著增加了骨质疏松症小鼠的骨质量,改善了椎骨厚 (+17.03%) 和骨体积分数 (+40.55%).
结论:
- 使用巨型宏循环进行超分子封装,为生物活性的输送提供了一个通用和有效的策略.
- 这种方法提高了的稳定性和治疗疗效,为再生医学中药物开发开辟了新的途径.
相关概念视频
Osteoclasts in Bone Remodeling
2.9K
Osteoclasts are cells responsible for bone resorption and remodeling. They originate from hematopoietic progenitor cells present in the bone marrow. Numerous progenitor cells fuse to form multinucleated cells, each with 10-20 nuclei. A single osteoclast has a diameter of 150 to 200 µM. These cells have ruffled borders that break down the underlying bone tissue and release minerals such as calcium into the blood in bone resorption. Osteoclasts cling to bones with their ruffled edges during...
2.9K
Hormones and Bone Tissue
2.7K
The endocrine system produces and secretes hormones, which interact with the skeletal system. These hormones control bone growth, maintain bone once it is formed, and remodel it.
Hormones That Influence Osteoblasts and/or Maintain the Matrix
Several hormones are necessary for controlling bone growth and maintaining the bone matrix. The pituitary gland secretes growth hormone (GH), which, as its name implies, controls bone growth. This happens in several ways: first, it triggers chondrocyte...
Hormones That Influence Osteoblasts and/or Maintain the Matrix
Several hormones are necessary for controlling bone growth and maintaining the bone matrix. The pituitary gland secretes growth hormone (GH), which, as its name implies, controls bone growth. This happens in several ways: first, it triggers chondrocyte...
2.7K
Bone Remodeling
38.3K
Bone remodeling is a continuous and balanced process of bone resorption by osteoclasts and bone formation by osteoblasts. In adults, it helps maintain bone mass and calcium homeostasis. While mechanical stress can stimulate turnover as part of the normal maintenance and reparative process, several hormones also regulate bone remodeling.
38.3K
GPCR Desensitization
6.0K
G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
6.0K
Glucagon-like Receptor Agonists
321
Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
321
GPCRs Regulate Adenylyl Cylase Activity
5.5K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
5.5K


