The Pharmacological Implications of Flavopiridol: An Updated Overview.

Flavopiridol is a flavone synthesized from the natural product rohitukine, which is derived from an Indian medicinal plant, namely Dysoxylum binectariferum Hiern. A deeper understanding of the biological mechanisms by which such molecules act may allow scientists to develop effective therapeutic strategies against a variety of life-threatening diseases, such as cancer, viruses, fungal infections, parasites, and neurodegenerative diseases. Mechanistic insight of flavopiridol reveals its potential for kinase inhibitory activity of CDKs (cyclin-dependent kinases) and other kinases, leading to the inhibition of various processes, including cell cycle progression, apoptosis, tumor proliferation, angiogenesis, tumor metastasis, and the inflammation process. The synthetic derivatives of flavopiridol have overcome a few demerits of its parent compound. Moreover, these derivatives have much improved CDK-inhibitory activity and therapeutic abilities for treating severe human diseases. It appears that flavopiridol has potential as a candidate for the formulation of an integrated strategy to combat and alleviate human diseases. This review article aims to unravel the potential therapeutic effectiveness of flavopiridol and its possible mechanism of action.

Wogonin, as a potent anticancer compound: From chemistry to cellular interactions.

Chinese native medicine Scutellaria baicalensis Georgi, also referred to as Chinese skullcap or Huang-Qin, is frequently used to treat cancer, viral infections, and seizures. This plant's abundance of flavones (wogonoside) and their related aglycones (wogonin) is responsible for many of its pharmacologic effects. A significant ingredient in S. baicalensis that has been the subject of the most research is wogonin. Numerous preclinical investigations revealed that wogonin suppresses tumor growth by cell cycle arrest, stimulating cell death and preventing metastasis. This review focuses on a complete overview of published reports that suggest chemopreventive action of wogonin and the mechanistic insights behind these neoplastic activities. It also emphasizes the synergistic improvements made by wogonin in chemoprevention. The factual data in this mini-review stimulate additional research on chemistry and toxicological profile of wogonin to confirm its safety issues. This review will encourage researchers to generalize the merits of wogonin to be used as potential compound for cancer treatment.

Genistein: a promising modulator of apoptosis and survival signaling in cancer.

Genistein, a commonly occurring isoflavone, has recently gained popularity owing to its ever-expanding spectrum of pharmacological benefits. In addition to health benefits such as improved bone health and reduced postmenopausal complications owing to its phytoestrogen properties, it has been widely evaluated for its anti-cancer potential. Several studies have established the potential for its usage in the management of breast, lung, and prostate cancers, and its usage has significantly evolved from early applications in traditional systems of medicine. This review offers an insight into its current status of usage, the chemistry, and pharmacokinetics of the molecule, an exploration of its apoptotic mechanisms in cancer management, and opportunities for synergism to improve therapeutic outcomes. In addition to this, the authors have presented an overview of recent clinical trials, to offer an understanding of contemporary studies and explore prospects for a greater number of focused trials, moving forward. Advancements in the application of nanotechnology as a strategy to improve safety and efficacy have also been highlighted, with a brief discussion of results from safety and toxicology studies.

Progressive supranuclear palsy responding to intravenous thiamine: superimposed Wernicke's encephalopathy?

Progressive supranuclear palsy (PSP) may be a risk factor for thiamine deficiency. The classic symptoms of PSP (postural instability, supranuclear vertical gaze palsy and dementia) overlap with the clinical triad of Wernicke's encephalopathy (cognitive impairment, gait problems and ocular abnormality). Therefore, superimposed thiamine deficiency in patients with PSP may aggravate the pre-existing symptoms of PSP. Here, we are reporting a 64-year-old woman having supranuclear ocular palsy, gait instability and dementia for the past 2-3 years. The patient fulfilled the diagnostic criteria of PSP. In parallel, she fulfilled the Caine's criteria of Wernicke's encephalopathy. Her serum thiamine level was low. Supplementation of thiamine led to marked improvement in the symptoms which had been present for many years. These symptoms were originally presumed to be due to PSP. This case highlights the needs to identify superimposed thiamine deficiency in patients with PSP.

Vitamin D Deficiency in Patients With Chronic Tension-Type Headache: A Case-Control Study.

OBJECTIVE: To see the interrelation between chronic tension-type headache (CTTH) and serum vitamin D levels. BACKGROUND: Several studies have suggested an association between chronic pain and vitamin D deficiency. Anecdotal evidence suggests that vitamin D deficiency may be associated with tension-type headache and migraine. METHODS: This case-control study was carried out to examine the association between CTTH and serum 25-hydroxy vitamin (25(OH) D) levels. One hundred consecutive adult (>18 years) patients with CTTH and 100 matched healthy controls were enrolled. RESULTS: The serum 25(OH) D levels were significantly lower in CTTH patients than in the controls (14.7 vs 27.4 ng/mL). The prevalence of vitamin D deficiency (serum 25 (OH) D < 20 ng/mL) was greater in patients with CTTH (71% vs 25%). CTTH patients had a significantly high prevalence of musculoskeletal pain (79% vs 57%), muscle weakness (29%vs 10%), muscle tenderness score (7.5 vs 1.9), and bone tenderness score (3.0 vs 0.8) in comparison to controls. CTTH patients with vitamin D deficient group (<20 ng/mL) had a higher prevalence of musculoskeletal pain (58% vs 31%), muscle weakness (38%vs 7%), muscle and bone tenderness score, associated fatigue (44% vs 17%) and more prolonged course (15.5 months vs 11.2 months). A strong positive correlation was noted between serum vitamin D levels and total muscle tenderness score (R2 = 0. 7365) and total bone tenderness score (R2 = 0. 6293). CONCLUSION: Decreased serum 25(OHD) concentration was associated with CTTH. Intervention studies are required to find out if supplementation of vitamin D is effective in patients with CTTH.

Selenium containing imidazolium salt in designing single source precursors for silver bromide and selenide nano-particles.

The AgBr and Ag(2)Se nanoparticles (NPs) have been synthesized for the first time from two single source precursors ([Ag(2)(L)(2)Br(2)] (1) and [Ag(L-HBr)(2)]BF(4) (2) respectively) designed using the same ligand 3-benzyl-1-(2-phenylselanyl-ethyl)-3H-imidazolium bromide (L). The ODE-ODA-OA (1 : 1 : 2) and TOP-OA (1 : 2) are most suitable solvents for thermolysis of 1 and 2 respectively, resulting in the NPs. The composition of the solvent used in thermolysis affects the purity of NPs. The bonding of L in 1 is unique, as it has a pre-carbene site intact.