CN-117959269-B - Application of pp' -DDE and homologs thereof in preparation of medicines for treating osteoporosis

Abstract

The invention provides application of pp '-DDE in preparation of a medicament for treating osteoporosis, which takes pp' -DDE and homologs thereof (DDT; op '-DDT; pp' -DDD and the like) as active ingredients, and promotes formation of mineralized nodules of osteoblasts by improving expression of Ocn, alpl, sp molecules and the like in the osteoblasts, so that thickness of cortical bone or femur is increased, osteoporosis symptoms are improved, and the aim of treating osteoporosis is fulfilled.

Inventors

• ZHANG QIAN
• YAN WENLIANG
• XU JIAYANG
• LV ZIQUAN
• Sun Kainong
• CHEN MENG
• Li Rongzi
• WANG JUN
• LI SHIMING
• MIAO JINGYUAN
• REN FAZHENG

Assignees

• 中国农业大学

Dates

Publication Date

20260505

Application Date

20221024

Claims (7)

1. Use of pp '-DDE in the manufacture of an anti-osteoporosis agent characterized by a white solid crystalline or white powder appearance, a chemical formula C 14 H 8 Cl 4 , a molecular weight 318.0, said pp' -DDE having the structure: 。
2. 2. The use according to claim 1, wherein pp' -DDE increases cortical bone thickness.
3. 3. The use according to claim 1, wherein pp' -DDE is capable of increasing femoral bone thickness.
4. 4. The use according to claim 1, wherein pp' -DDE is capable of promoting mineralization of nodules by osteoblasts.
5. 5. The use according to claim 4, characterized in that it is a white solid crystalline or white powder with the chemical formula C 14 H 8 Cl 4 and with the molecular weight 318.0, said use being achieved by increasing the expression of Ocn in osteoblasts.
6. 6. The use according to claim 4, characterized in that it is a white solid crystalline or white powder with the chemical formula C 14 H 8 Cl 4 and the molecular weight 318.0, said use being achieved by increasing the expression of Alpl in osteoblasts.
7. 7. The use according to claim 4, characterized in that it is a white solid crystalline or white powder in appearance, of formula C1 4 H 8 Cl 4 , of molecular weight 318.0, by increasing the expression of Sp7 in osteoblasts.

Description

Application of pp' -DDE and homologs thereof in preparation of medicines for treating osteoporosis Technical Field The invention belongs to the field of biological medicine, and in particular relates to application of pp' -DDE in treatment of osteoporosis related diseases. Background Osteoporosis is one of the common senile chronic diseases, and bone homeostasis is mainly balanced by bone formation by osteoblasts and bone resorption by osteoclasts, and is caused by the fact that the activity of osteoclasts exceeds that of osteoblasts. At present, most of medicines for osteoporosis clinically are medicines for inhibiting bone resorption, and the essential problem of senile osteoporosis is difficult to solve. A few drugs for promoting bone formation such as parathyroid hormone have the defects of joint pain, bone density reduction after stopping drug, possible hypercalcemia and the like, so that searching for a drug administration site capable of enhancing osteoblast function and increasing bone formation is an important aspect of research. Pp ' -DDE, full name pp ' -dichlorodiphenyl-dichloroethylene, also name 44' -DDE, molecular formula C14H8Cl4, molecular weight 318.0, CAS number 72-55-9. The test of the invention shows that the low dosage of pp' -DDE can promote the differentiation of osteoblasts, increase the thickness of cortical bone of a wild type adult mouse and relieve the osteoporosis caused by estrogen deficiency. Disclosure of Invention The present invention provides an anti-osteoporosis agent containing low-concentration pp' -DDE as an active ingredient. The application of pp' -DDE in preparation of anti-osteoporosis drugs provided by the invention can be based on common knowledge of a person skilled in the pharmaceutical field to add auxiliary components such as carriers, excipients, flavoring agents and the like which do not influence the drug efficacy of the drugs. Since the drug can take effect through oral administration, injection, subcutaneous embedding and the like, the dosage forms can be various, including but not limited to powder, granules, tablets, capsules, pills, solutions, suspensions or injection. The structure of pp' -DDE is as follows: In a second aspect, the present invention provides the use of pp' -DDE for the preparation of a formulation for increasing cortical bone thickness, said formulation being based on the general knowledge of a person skilled in the pharmaceutical arts, with the addition of auxiliary ingredients such as carriers, excipients, flavouring agents etc. which do not affect the efficacy of the drug. Since the drug can take effect through oral administration, injection, subcutaneous embedding and the like, the dosage forms can be various, including but not limited to powder, granules, tablets, capsules, pills, solutions, suspensions or injection. The structure of pp' -DDE is as follows: in a third aspect, the present invention provides the use of pp' -DDE for the preparation of a formulation for increasing the thickness of a femoral bone, said formulation being based on the general knowledge of a person skilled in the art of pharmacy, with the addition of auxiliary components, such as carriers, excipients, flavouring agents, etc., which do not affect the efficacy of the drug. Since the drug can take effect through oral administration, injection, subcutaneous embedding and the like, the dosage forms can be various, including but not limited to powder, granules, tablets, capsules, pills, solutions, suspensions or injection. The structure of pp' -DDE is as follows: In a fourth aspect, the present invention provides the use of pp' -DDE for the preparation of a formulation for promoting mineralization of osteoblasts, said formulation being based on the general knowledge of a person skilled in the art of pharmacy, with the addition of auxiliary ingredients such as carriers, excipients, flavouring agents etc. which do not affect the efficacy of the drug. Since the drug can take effect through oral administration, injection, subcutaneous embedding and the like, the dosage forms can be various, including but not limited to powder, granules, tablets, capsules, pills, solutions, suspensions or injection. The structure of pp' -DDE is as follows: In one embodiment, the use is by increasing the expression of Ocn in osteoblasts, in another embodiment by increasing Alpl expression in osteoblasts, and in yet another embodiment by increasing Sp7 expression. In a sixth aspect, the present invention provides the use of pp' -DDE in the preparation of a reagent for promoting expression of Ocn, alpl, sp or other molecules in osteoblasts, said formulation being based on the general knowledge of a person skilled in the pharmaceutical arts, with the addition of auxiliary ingredients such as carriers, excipients, flavouring agents etc. which do not affect the efficacy of the drug. Since the drug can take effect through oral administration, injection, subcutaneous embedding and the li