Development of novel bone targeting peptide–drug conjugate of 13-aminomethyl-15-thiomatrine for osteoporosis therapy

13-Aminomethyl-15-thiomatrine (M19) previously developed by our research group was a promising candidate for novel anti-osteoporosis drug development.

Common osteoporosis drug associated with increased rates of depression and anxiety

Osteoporosis affects over 10 million Americans over 50. Bisphosphonate therapy, mainly alendronate, is amongst the most prescribed treatments for the disease. The use of alendronate and other bisphosphonates has been associated with depressive symptoms in recent case reports. In this study we quantified this association by analyzing over 100,000 adverse events reports from the Food and Drug Administration Adverse Events Reporting System (FAERS) and the World Health Organization’s (WHO) global database for adverse drug reactions, ADRs, VigiAccess. We found that alendronate therapy is significantly associated with depression and anxiety when compared to other first-line osteoporosis treatments. The reported risk of depressive ADRs was found to be over 14-fold greater in patients taking alendronate under the age of 65 and over fourfold greater for patients over 65 compared to the control. Several hypotheses concerning the molecular mechanism of the observed association of alendronate and depressive symptoms were discussed.

Therapeutic Potential, Synthesis, Patent evaluation and SAR studies of thieno[3,2-d]pyrimidine derivatives: Recent updates.

: Thieno[3,2-d]pyrimidine ring framework comprises a significant class of heterocyclics that serve as a promising platform showing different pharmacological activities. The interest in thieno[3,2-d]pyrimidine cores for pharmaceutical products makes this scaffold an exceptionally helpful building block for organic chemistry. This review presents current research on thieno[3,2-d]pyrimidines and elucidates their biological importance in anti-cancer, anti-infectious, anti-convulsant, anti-diabetic, CNS, and osteoporosis drug discoveries. Patents on the thieno[3,2-d]pyrimidines are also elaborated as a piece of useful information. Here we additionally focus on the synthesis of this vital ring and the discovery of new thieno[3,2-d]pyrimidines.

Fabrication of Chemically Linked PEGylated Prodrugs for Hydrogel Carriers

Some hydrophilic drugs (e.g. anti-tumor drug of doxorubicin (DOX) and anti-osteoporosis drug of alendronate sodium (ALN)) have great toxic and adverse effects on the human body. In this paper, two kinds of drug-loaded composite gel systems were prepared via mild and efficient chemical reaction synthesis, hyaluronic acid-linked ALN (HA-ALN) hydrogel and polyethylene glycol-linked DOX (Tetra-PEG-DOX) hydrogel. By characterizing their chemical structures, morphological networks, and ultraviolet absorption behaviors, two different types of drug-loaded composite gels can be constructed well. It is expected to achieve effective drug loading and controlled release. The two drug-loaded gels are applied in the fields of antitumor and anti-osteoporosis and exert their application value in the field of biomedicine.