Current Drug Targets

BACKGROUND: Statins, especially simvastatin promote bone formation by stimulating the activity of osteoblasts and suppressing osteoclast activity via the BMP-Smad signaling pathway. Statins present the liver first-pass metabolism. This study attempts to fabricate and evaluate simvastatin functionalized hydroxyapatite encapsulated in poly(lactic-co-glycolic) acid (PLGA) nanoparticles (HSIM-PLGA NPs) administered subcutaneously with sustained release properties for effective management of osteoporosis...

BACKGROUND: Antibiotic-resistant microorganisms (ARMS) are the leading cause of socio-economic loss in the world, with historical evidence linking them to increased mortality and morbidity. METHODOLOGY: In this systematic review, we highlight a new treatment approach for antibiotic-resistant infections using 'Extracellular vesicle (EVs)-based therapy,' also known as cell- and drug-free therapy. Here, we categorize and summarize studies on EVs derived from various human sources, such as tissues, bodily fluids, or their condition media, emphasizing their anti-infective properties in the treatment of various infections...

Sodium-glucose cotransporter 2 (SGLT2) inhibitors are a new type of oral hypoglycemic drugs that exert a hypoglycemic effect by blocking the reabsorption of glucose in the proximal renal tubules, thus promoting the excretion of glucose from urine. Their hypoglycemic effect is not dependent on insulin. Increasing data shows that SGLT2 inhibitors improve cardiovascular outcomes in patients with type 2 diabetes. Previous studies have demonstrated that SGLT2 inhibitors can reduce pathological myocardial hypertrophy with or without diabetes, but the exact mechanism remains to be elucidated...

Stimulator of interferon genes (STING) plays a vital role in the human innate immune system. Aberrant expression of STING has been proven to be associated with several diseases, such as STING-associated vasculopathy with onset in infancy, Aicardi-Goutieres syndrome, and systemic lupus erythematosus. Therefore, inhibition of the STING signaling pathway can also be expected to provide effective therapeutic strategies for treating specific inflammatory and autoimmune diseases. However, the development of STING inhibitors is still in its infancy...

No abstract text is available yet for this article.

Brain-related disorders are one of the world's most important and complex health problems today. These brain-related disorders are responsible for a massive number of morbidities and death all around the world. However, researchers have devoted a large amount of time to investigating these diseases and found positive results; nevertheless, there are currently quite a few medications available to treat them. Emodin (EM), a polyphenol compound, has many health benefits. It is a biologically active monomer derived from rhubarb root that exhibits anti-inflammation, anti-oxidation, anticancer, and neuroprotective properties...

BACKGROUND: Cancer is a life-threatening disease worldwide, but proper treatment has not yet been developed. Many therapies are available to treat cancer disorders, like chemotherapy, surgery, hormone therapy, and immunotherapy. Chemotherapy often relies on a combination of harmful, highly toxic platinum-based compounds. Also, there are chances of poor distribution of chemotherapeutic agents and cytotoxic to most cells which leads to damage to other healthy cells, also, there are chances of resistance...

INTRODUCTION: Glioblastoma multiforme (GBM) has a poor prognosis, with current treatments providing no advantage in terms of survival. Certain new immunotherapy methods, such as peptide vaccines, have been used in clinical trials. In this meta-analysis, the effectiveness of peptide vaccinations on the survival rate of GBM patients was studied. METHOD: A comprehensive search was carried out using three electronic databases: PubMed, Scopus, and ISI. The purpose of this research was to assess overall survival (OS)...

No abstract text is available yet for this article.

BACKGROUND: Hepatocellular carcinoma (HCC) is associated with a high mortality rate due to early recurrence and its metastasis features. To this day, effective treatment options for metastatic HCC remain a major challenge to patient treatment. Flavokawain B (FKB) is a naturally occurring chalcone molecule capable of providing effective therapy against this life-threatening disease. OBJECTIVE: This study investigated the anti-metastatic effects of FKB on the growth and development of metastatic HCC...

Osteoporosis is one of the skeletal diseases of major health concern worldwide. Homeostasis of bone occurs with the help of cells, namely, osteoblasts and osteoclasts. Physiological and pathological conditions involve the death of the cells by apoptosis, autophagy, and necrosis. Apoptosis is a key factor in the growth, development, and maintenance of the skeleton. Apoptosis is generated by two pathways: the intrinsic (mitochondria) and extrinsic (death receptor) pathways. Osteoblast apoptosis is governed by the factors like B cell lymphoma 2 (Bcl-2) family proteins, extracellular signal-regulated kinase (ERK), mitogen-activated protein kinases (MAPK), phosphoinositide-3-kinase/ protein kinase B (PI3-K/Akt), Janus kinase 2 (JAK2), bone morphogenetic protein (BMP), and bone matrix protein...

Microtubules are a well-known target in cancer chemotherapy because of their critical role in cell division. Chromosome segregation during mitosis depends on the establishment of the mitotic spindle apparatus through microtubule dynamics. The disruption of microtubule dynamics through the stabilization or destabilization of microtubules results in the mitotic arrest of the cells. Microtubule-targeted drugs, which interfere with microtubule dynamics, inhibit the growth of cells at the mitotic phase and induce apoptotic cell death...

BACKGROUND: The poor water solubility of an active pharmaceutical ingredient leads to a lower dissolution profile that in turn results in poor bioavailability of drugs. Various approaches like solid dispersion, nano-technology, complexation, and micronization techniques, etc. are frequently used by pharmaceutical researchers to overcome these issues. In this context, crystal engineering emerges as a viable technique. OBJECTIVE: This review endeavors to cover the latest developments in the field of solubility enhancement using crystal engineering techniques...

BACKGROUND: Human African trypanosomiasis (HAT) is a parasitic infection that may lead to death if left untreated. This disease is caused by a protozoan parasite of the genus Trypanosoma and is transmitted to humans through tsetse fly bites. The disease is widespread across Sub-Saharan Africa, with 70% of cases in recent reports in the Democratic Republic of the Congo and an average of less than 1000 cases are declared annually. Since there is no appropriate treatment for HAT, steroidal and triterpenoid saponins have been reported to be effective in in vitro studies and might serve as scaffolds for the discovery of new treatments against this disease...

No abstract text is available yet for this article.

Some diseases caused by trypanosomatid parasites, like Leishmaniasis, Chagas Disease, and Human African Trypanosomiasis (HTA), are challenging to manage, mainly concerning pharmacological therapy because they are associated with vulnerable populations. Unfortunately, there is a lack of significant investments in the search for new drugs. Therefore, one of the strategies to aid the discovery of new drugs is to identify and inhibit molecular targets essential to the parasite's survival, such as the proteasome, which degrades most proteins in the parasite cells...

BACKGROUND: Skin aging is a natural process resulting from intrinsic (hormonal and genetic) and extrinsic (environmental) factors. Photoaging occurs due to prolonged exposure of the skin to ultraviolet radiation, accounting for 80% of facial aging. INTRODUCTION: Characteristics of aging skin include reduced elasticity, the appearance of fine wrinkles, uneven tone, and dryness. Clinical signs of photoaging involve the presence of deeper wrinkles, rough texture, dyschromia and a greater loss of elasticity compared to chronological aging...

BACKGROUND: Tropolone and thailandepsin B are naturally occurring substances that are primarily isolated from fungi and plants, although they can also be found in certain bacteria. Tropolones belong to an important class of aromatic compounds with a seven-membered non-benzenoid ring structure. Thailandepsins are a group of natural products that were initially discovered in the culture broth of the Gram-negative bacterium Burkholderia thailandensis. Tropolone-based structures have been identified in over 200 natural compounds, ranging from simple tropolone derivatives to complex multicyclic systems like pycnidione and pyrerubrine A...

The extensive development in the strains of resistant bacteria is a potential hazard to public health worldwide. This necessitates the development of newer agents with the antibacterial property having new mechanisms of action. Mur enzymes catalyze the steps related to the biosynthesis of peptidoglycan, which constitutes a major part of the cell wall in bacteria. Peptidoglycan increases the stiffness of the cell wall, helping it to survive in unfavorable conditions. Therefore, the inhibition of Mur enzymes may lead to novel antibacterial agents that may help in controlling or overcoming bacterial resistance...

Gelatin is an attractive material for drug delivery and tissue engineering applications due to its excellent biocompatibility and biodegradability, which has been utilized as cell, drug, and gene carriers. Gelatin is less immunogenic compared to collagen and its precursor and retains informational signals, such as RGD (Arg-Gly-Asp) sequence, thus promoting cell adhesion and proliferation. To tune the mechanical strength and bioactivity, gelatin can be easily modified via chemical reactions and physical methods to obtain various derivatives...