Pharmacological safety of dimethoxy curcumin-human serum albumin conjugate for potential therapeutic purpose.

Medicinal properties of curcumin are widely published. Previously, researchers used curcuminoid mixture comprising three chemical forms, out of which, the highest quantity is the most active molecule-dimethoxy curcumin (DMC). Reduced bioavailability, poor aqueous solubility, and quick hydrolytic degradation of DMC have projected challenges limiting its therapeutic value. However, selective conjugation of DMC with human serum albumin (HSA) enhances drug stability and solubility by several folds. Studies using animal models demonstrated potential anti-cancer/anti-inflammatory effects of DMCHSA; both studies showed results of local administration in peritoneal cavity and rabbit knee joint. DMC has prospects as intravenous therapeutic agent because carrier is HSA. However, before in vivo testing, important preclinical data required are toxicological safety and bioavailability of soluble forms of DMC. This study evaluated absorption, distribution, metabolism, and excretion of DMCHSA. Imaging technology and molecular analysis proved bio-distribution. The study also assessed the pharmacological safety of DMCHSA in mice in terms of its acute and sub-acute toxicity, complying with regulatory toxicology. Overall, the study demonstrated the safety pharmacology of DMCHSA upon intravenous infusion. This is a novel study establishing the safety of highly soluble and stable formulation of DMCHSA, qualifying it for intravenous administration and further efficacy evaluation in suitable disease models.

Incidence and Clinical Presentation of Temporo-Mandibular Joint Disorders and their Association with Psychological Distress and Para-Functional Habits in a Non-Patient Population.

Purpose: The study aims at finding the incidence of temporo-mandibular joint disorders (TMDs) in a non-patient population and relates their association with psychological distress and parafunctional habits. Materials and Methods: A DC/TMD questionnaire and DASS-21 scale survey were completed by selected participants followed by clinical examination of TMDs symptoms in sample population. Results: A study sample of 855 participants revealed 36.65% population with various TMDs symptoms, while 63.5% population had no TMDs symptoms. 50.8% study participants were men, and 49.2% were women. Of all affected population, 16.2% had pain-related TMDs, 12.39% had intra-articular TMDs symptoms, and 8.07% had TMJ pain associated with pain or dysfunction. For all TMDs symptoms groups, the strongest correlations were for depression, while no significant associations were observed with parafunctional habits in all groups. Conclusions: Overall psychological distress and anxiety increased the prospects of TMDs symptoms. Clinical factors like muscle tenderness, crossbite and deep vertical overlap seem to be significant etiological factors, while angle molar relationship and parafunctional habits do not seem to be significant etiologic factors in TMDs.

Transition metal dichalcogenide (TMDs) electrodes for supercapacitors: a comprehensive review.

As globally, the main focus of the researchers is to develop novel electrode materials that exhibit high energy and power density for efficient performance energy storage devices. This review covers the up-to-date progress achieved in transition metal dichalcogenides (TMDs) (e.g. MoS2, WS2, MoSe2,and WSe2) as electrode material for supercapacitors (SCs). The TMDs have remarkable properties like large surface area, high electrical conductivity with variable oxidation states. These properties enable the TMDs as the most promising candidates to store electrical energy via hybrid charge storage mechanisms. Consequently, this review article provides a detailed study of TMDs structure, properties, and evolution. The characteristics technique and electrochemical performances of all the efficient TMDs are highlighted meticulously. In brief, the present review article shines a light on the structural and electrochemical properties of TMD electrodes. Furthermore, the latest fabricated TMDs based symmetric/asymmetric SCs have also been reported.

Exploring the magic bullets to identify Achilles' heel in SARS-CoV-2: Delving deeper into the sea of possible therapeutic options in Covid-19 disease: An update.

The symptoms associated with Covid-19 caused by SARS-CoV-2 in severe conditions can cause multiple organ failure and fatality via a plethora of mechanisms, and it is essential to discover the efficacious and safe drug. For this, a successful strategy is to inhibit in different stages of the SARS-CoV-2 life cycle and host cell reactions. The current review briefly put forth the summary of the SARS-CoV-2 pandemic and highlight the critical areas of understanding in genomics, proteomics, medicinal chemistry, and natural products derived drug discovery. The review further extends to briefly put forth the updates in the drug testing system, biologics, biophysics, and their advances concerning SARS-CoV-2. The salient features include information on SARS-CoV-2 morphology, genomic characterization, and pathophysiology along with important protein targets and how they influence the drug design and development against SARS-CoV-2 and a concerted and integrated approach to target these stages. The review also gives the status of drug design and discovery to identify the drugs acting on critical targets in SARS-CoV-2 and host reactions to treat Covid-19.

Structural, electrical properties and dielectric relaxations in Na+-ion-conducting solid polymer electrolyte.

In this paper, we have studied the structural, microstructural, electrical, dielectric properties and ion dynamics of a sodium-ion-conducting solid polymer electrolyte film comprising PEO8-NaPF6+ x wt. % succinonitrile. The structural and surface morphology properties have been investigated, respectively using x-ray diffraction and field emission scanning electron microscopy. The complex formation was examined using Fourier transform infrared spectroscopy, and the fraction of free anions/ion pairs obtained via deconvolution. The complex dielectric permittivity and loss tangent has been analyzed across the whole frequency window, and enables us to estimate the DC conductivity, dielectric strength, double layer capacitance and relaxation time. The presence of relaxing dipoles was determined by the addition of succinonitrile (wt./wt.) and the peak shift towards high frequency indicates the decrease of relaxation time. Further, relations among various relaxation times ([Formula: see text]) have been elucidated. The complex conductivity has been examined across the whole frequency window; it obeys the Universal Power Law, and displays strong dependency on succinonitrile content. The sigma representation ([Formula: see text]) was introduced in order to explore the ion dynamics by highlighting the dispersion region in the Cole-Cole plot ([Formula: see text]) in the lower frequency window; increase in the semicircle radius indicates a decrease of relaxation time. This observation is accompanied by enhancement in ionic conductivity and faster ion transport. A convincing, logical scheme to justify the experimental data has been proposed.

Chebulagic acid from Terminalia chebula enhances insulin mediated glucose uptake in 3T3-L1 adipocytes via PPARγ signaling pathway.

The thiazolidinedione (TZDs) class of drugs are very effective for the treatment of type 2 diabetes mellitus (T2DM). But due to the adverse effects of synthetic TZDs, their use is strictly regulated. The therapeutic actions of TZDs are mediated via modulation of peroxisome proliferator-activated receptor gamma (PPARγ). Naturally occurring PPARγ modulators are more desirable as they lack the serious adverse effects caused by TZDs. This has prompted the exploitation of medicinal plants used in traditional medicine, for their potential PPARγ activity. In the present work, we studied chebulagic acid (CHA) isolated from fruits of Terminalia chebula with respect to its effect on adipogenesis, glucose transport, and endocrine function of adipocyte. The mRNA expression profile of PPARγ target gene CCAAT/enhancer-binding protein alpha (C/EBP-α) was analyzed by qRT-PCR. The putative binding mode and the potential ligand-target interactions of CHA, with PPARγ was analyzed using docking software (Autodock and iGEMDOCKv2). The results showed that CHA enhances PPARγ signaling and adipogenesis dose dependently but in a moderate way, less than rosiglitazone. GLUT4 expression and adiponectin secretion was increased by CHA treatment. The mRNA expression of PPARγ target gene C/EBP-α was increased in CHA -treated adipocytes. The comparison of results of various parameters of adipogenesis, insulin sensitivity, endocrine function and molecular docking experiments of roziglitazone and chebulagic acid indicate that the latter behaves like partial PPARγ agonist which could be exploited for phytoceutical development against T2DM.