Social networking: An analysis of health-related social support messages posted in a Facebook group for Kashmiri women.

The support groups within social networking sites such as Facebook have become a popular platform for various kinds of conversation and social support including health, especially among women. The aim of this study was to explore and analyze the types of health-related social support messages posted in a month by Kashmiri women in a Facebook group and the most common health topics for which social support was sought. A total of 302 health-related posts were selected for analysis. The results revealed that of various health-related social support posts in the group, informational support messages were posted more frequently and most requested information was related to pregnancy.

Glycol Chitosan-Poly(lactic acid) Conjugate Nanoparticles Encapsulating Ciprofloxacin: A Mucoadhesive, Antiquorum-Sensing, and Biofilm-Disrupting Treatment Modality for Bacterial Keratitis.

Bacterial keratitis (BK) causes visual morbidity/blindness if not treated effectively. Here, ciprofloxacin (CIP)-loaded nanoparticles (NPs) using glycol chitosan (GC) and poly(lactic acid) (PLA) conjugate at three different ratios (CIP@GC(PLA) NPs (1:1,5,15)) were fabricated. CIP@GC(PLA) NPs (1:1) were more effective than other tested ratios, indicating the importance of optimal hydrophobic/hydrophilic balance for corneal penetration and preventing bacterial invasion. The CIP@GC(PLA) (NPs) (1:1) realized the highest association with human corneal epithelial cells, which were nonirritant to the hen's egg-chorioallantoic membrane test (HET-CAM test) and demonstrated significant antibacterial response in the in vitro minimum inhibitory, bactericidal, live-dead cells, zone of inhibition, and biofilm inhibition assays against the keratitis-inducing pathogen Pseudomonas aeruginosa. The antiquorum sensing activity of GC has been explored for the first time. The NPs disrupted the bacterial quorum sensing by inhibiting the production of virulence factors, including acyl homoserine lactones, pyocyanin, and motility, and caused significant downregulation of quorum sensing associated genes. In the in vivo studies, CIP@GC(PLA) NPs (1:1) displayed ocular retention in vivo (∼6 h) and decreased the opacity and the bacterial load effectively. Overall, the CIP@GC(PLA) NP (1:1) is a biofilm-disrupting antiquorum sensing treatment regimen with clinical translation potential in BK.

Rubus moluccanus L.: a valuable medicinal plant of traditional system of medicine.

Rubus moluccanus L., commonly known as Molucca bramble or broad-leaf bramble is a member of family Rosaceae which occurs mainly in tropical Asia and Australia. It has applications in indigenous medicines and is used in the treatment of number of ailments like headache, diarrhoea, dysentery, abdominal pain, nocturnal micturition of children and enhancement of female fertility. This plant is a rich and valuable source of bioactive flavonoids, terpenes and other chemical compounds. The presence of these active chemical compounds exerts antibacterial, antifungal, antihelminthic and antioxidant activities. Regardless of its use in various diseases and disorders, the information about this plant is scanty. So the present review assessed and summarised the knowledge on taxonomy, morphology, geographical distribution, nutritional value, ethnobotany, phytochemistry and biological activities of R. moluccanus.

Polymeric graphene oxide nanoparticles loaded with doxorubicin for combined photothermal and chemotherapy in triple negative breast cancer.

Combining photothermal and chemotherapy is an emerging strategy for tumor irradiation in a minimally invasive manner, utilizing photothermal transduction agents and anticancer drugs. The present work developed a 2D carbon nanomaterial graphene oxide (GO)-based nanoplatform that converted to 3D colloidal spherical structures upon functionalization with an amphiphilic polymer mPEG-PLA (1, 0.5/1/2) and entrapped doxorubicin (Dox) physically. The Dox@GO(mPP) (1/0.5) NPs displayed the least particle size (161 nm), the highest stability with no aggregation, the highest Dox loading (6.3 %) and encapsulation efficiency (70 %). The therapeutic efficacy was determined in vitro and in vivo using murine (4 T1) and human triple-negative breast cancer cells (MDA-MB-231), and 4 T1-Luc-tumor bearing mouse models. The results demonstrated that the Dox@GO(mPP) (1/0.5) NPs treatment with laser (+L) (808 nm) was highly efficient in inducing apoptosis, cell cycle arrest (G2/M) phase, significant cytotoxicity, mitochondrial membrane depolarization, ROS generation, and photothermal effect leading to a higher proportion of cell death than free Dox, and Dox@GO(mPP) (1/0.5) NPs (-L). The anticancer studies in mice harboring the 4 T1-Luc tumor showed that combination of Dox@GO(mPP) (1/0.5) NPs (+L) effectively reduced tumor development and decreased lung metastasis. The developed nanoplatform could be a promising combination chemo-photothermal treatment option for triple-negative breast cancer.

Impact of exercise training duration on obesity and cardiometabolic biomarkers: a systematic review.

Introduction: Physical exercise deters the risk and reduce the adjusted Odds Ratio related to obesity and cardiometabolic diseases but the amount of physical exercise required for initiating those potential advantageous developments in the human body for normal obese individuals is still debatable and thus made many face the health burden during pandemic, despite of their claiming to be physically active. Objective: The primary aim of this review was to find an ideal duration and form of exercise that could help reduce the risk of cardiometabolic diseases and its complications for subjects with obesity and deranged cardiometabolic risk markers. Method: Electronic database PubMed/MedLine, Scopus and PEDro for available literature on Experimental studies and RCT on exercise prescription and its effect on anthropometric measurements as well as key biomarkers in obese individuals, 451 records were procured, 47 full text articles were identified to assess eligibility criteria out of which 19 were finally included in the review. Results: There exists a strong association between cardiometabolic profile and physical activity, poor diet, sedentary lifestyle and continuous exercises for longer duration can lead to reduction in obesity and subjects with cardiometabolic diseases. Conclusion: Various confounding factors that may affect the outcome of physical activity training have not been considered in a standard format by all the authors in the articles reviewed. There was variation in duration of physical activity and energy expenditure required for inducing the changes in different cardiometabolic biomarkers.

Novel Functionalized Spiro [Indoline-3,5'-pyrroline]-2,2'dione Derivatives: Synthesis, Characterization, Drug-Likeness, ADME, and Anticancer Potential.

A highly stereo-selective, one-pot, multicomponent method was chosen to synthesize the novel functionalized 1, 3-cycloaddition spirooxindoles (SOXs) (4a-4h). Synthesized SOXs were analyzed for their drug-likeness and ADME parameters and screened for their anticancer activity. Our molecular docking analysis revealed that among all derivatives of SOXs (4a-4h), 4a has a substantial binding affinity (∆G) -6.65, -6.55, -8.73, and -7.27 Kcal/mol with CD-44, EGFR, AKR1D1, and HER-2, respectively. A functional study demonstrated that SOX 4a has a substantial impact on human cancer cell phenotypes exhibiting abnormality in cytoplasmic and nuclear architecture as well as granule formation leading to cell death. SOX 4a treatment robustly induced reactive oxygen species (ROS) generation in cancer cells as observed by enhanced DCFH-DA signals. Overall, our results suggest that SOX (4a) targets CD-44, EGFR, AKR1D1, and HER-2 and induces ROS generation in cancer cells. We conclude that SOX (4a) could be explored as a potential chemotherapeutic molecule against various cancers in appropriate pre-clinical in vitro and in vivo model systems.

Hypoxia alleviating platinum(IV)/chlorin e6-based combination chemotherapeutic-photodynamic nanomedicine for oropharyngeal carcinoma.

Hypoxia is an important pathological hallmark of the tumor microenvironment, associated with metabolic alterations, cell proliferation, aggressiveness, metastasis, and therapy resistance in cancers. Hypoxia impedes the outcome of photodynamic therapy (PDT), which is largely dependent on molecular oxygen to generate cytotoxic 1O2. Here, a near-infrared light activatable, oxygen-generating nanomicellar PDT-chemotherapy system (mPPCPN Ms) constituted of amphiphilic mPEG-PLA, photosensitizer Ce6, and tetravalent platinum prodrug Pt(IV)-diazide was developed for oral squamous cell carcinoma. The polymer conjugate self-assemble to nanosize (115 ± 2.35 nm) micelles, which, upon irradiation (660 nm laser), activated Ce6, and photodecomposed to produce cytotoxic Pt(II), azidyl radical, and molecular oxygen. The strategically fabricated PDT-chemotherapy produced a strong antitumor response in vitro using oral squamous cell carcinoma and in vivo in oral cancer-xenografted mouse models, revealing its significant potential in chemo-photodynamic combination therapy with the benefit of reversing hypoxia.

Isatin Conjugates as Antibacterial Agents: A Brief Review.

Pathogenic bacteria, with their innate resistance to drugs, pose a constant threat to human health and well-being and put a persistent strain on the health care system. Development of more effective and safer novel antibacterial drugs is warranted to counter the menace unleashed by pathogenic bacteria. Integration of privileged pharmacophores from various bioactive molecules into a single template is a promising strategy to obtain new leads with unique mechanisms of action to overcome drug resistance. In the past few years, numerous isatin-based hybrid molecules were screened and their pharmacological properties were explored in efforts to develop novel therapeutics. The results of screening show that isatin conjugates exhibit promising activity against a broad range of highly pathogenic gram-positive and gram-negative bacteria and can serve as important leads in the discovery of highly potent broad spectrum antibacterial drugs. Herein, we review the antibacterial bioactive profile of a variety of hybrid isatin derivatives, including isatin-azole, isatin-quinoline/ quinolone, isatin-furan/coumarin, isatin-hydrazone/(thio)semicarbazone, isatin dimers, and isatin- indole hybrids.

Nanotherapeutic Intervention in Photodynamic Therapy for Cancer.

The clinical need for photodynamic therapy (PDT) has been growing for several decades. Notably, PDT is often used in oncology to treat a variety of tumors since it is a low-risk therapy with excellent selectivity, does not conflict with other therapies, and may be repeated as necessary. The mechanism of action of PDT is the photoactivation of a particular photosensitizer (PS) in a tumor microenvironment in the presence of oxygen. During PDT, cancer cells produce singlet oxygen (1O2) and reactive oxygen species (ROS) upon activation of PSs by irradiation, which efficiently kills the tumor. However, PDT's effectiveness in curing a deep-seated malignancy is constrained by three key reasons: a tumor's inadequate PS accumulation in tumor tissues, a hypoxic core with low oxygen content in solid tumors, and limited depth of light penetration. PDTs are therefore restricted to the management of thin and superficial cancers. With the development of nanotechnology, PDT's ability to penetrate deep tumor tissues and exert desired therapeutic effects has become a reality. However, further advancement in this field of research is necessary to address the challenges with PDT and ameliorate the therapeutic outcome. This review presents an overview of PSs, the mechanism of loading of PSs, nanomedicine-based solutions for enhancing PDT, and their biological applications including chemodynamic therapy, chemo-photodynamic therapy, PDT-electroporation, photodynamic-photothermal (PDT-PTT) therapy, and PDT-immunotherapy. Furthermore, the review discusses the mechanism of ROS generation in PDT advantages and challenges of PSs in PDT.

Current trends in the use of human serum albumin for drug delivery in cancer.

INTRODUCTION: Human serum albumin is the most abundant transport protein in plasma, which has recently been extensively utilized to form nanoparticles for drug delivery in cancer. The primary reason for selecting albumin protein as drug delivery cargo is its excellent biocompatibility, biodegradability, and non-immunogenicity. Moreover, the albumin structure containing three homologous domains constituted of a single polypeptide (585 amino acid) incorporates various hydrophobic drugs by non-covalent interactions. Albumin shows active tumor targeting via their interaction with gp60 and SPARC proteins abundant in the tumor-associated endothelial cells and the tumor microenvironment. AREAS COVERED: The review discusses the importance of albumin as a drug-carrier system, general procedures to prepare albumin NPs, and the current trends in using albumin-based nanomedicines to deliver various chemotherapeutic agents. The various applications of albumin in the nanomedicines, such as NPs surface modifier and fabrication of hybrid/active-tumor targeted NPs, are delineated based on current trends. EXPERT OPINION: Nanomedicines have the potential to revolutionize cancer treatment. However, clinical translation is limited majorly due to the lack of suitable nanomaterials offering systemic stability, optimum drug encapsulation, tumor-targeted delivery, sustained drug release, and biocompatibility. The potential of albumin could be explored in nanomedicines fabrication for superior treatment outcomes in cancer.

Multifunctional graphene oxide nanoparticles for drug delivery in cancer.

Recent advancements in nanotechnology have enabled us to develop sophisticated multifunctional nanoparticles or nanosystems for targeted diagnosis and treatment of several illnesses, including cancers. To effectively treat any solid tumor, the therapy should preferably target just the malignant cells/tissue with minor damage to normal cells/tissues. Graphene oxide (GO) nanoparticles have gained considerable interest owing to their two-dimensional planar structure, chemical/mechanical stability, excellent photosensitivity, superb conductivity, high surface area, and good biocompatibility in cancer therapy. Many compounds have been functionalized on the surface of GO to increase their biological applications and minimize cytotoxicity. The review presents an overview of the physicochemical characteristics, strategies for various modifications, toxicity and biocompatibility of graphene and graphene oxide, current trends in developing GO-based nano constructs as a drug delivery cargo and other biological applications, including chemo-photothermal therapy, chemo-photodynamic therapy, bioimaging, and theragnosis in cancer. Further, the review discusses the challenges and opportunities of GO, GO-based nanomaterials for the said applications. Overall, the review focuses on the therapeutic potential of strategically developed GO nanomedicines and comprehensively discusses their opportunities and challenges in cancer therapy.

When muscle quivers and undulates.

We describe a patient who presented with fatigue and pulling sensation in his lower limbs. He had continuous muscle contractions over his trunk (myokymia) which pointed towards the diagnosis of Isaacs syndrome which was confirmed by strongly positive CASPR2 antibodies in blood.

Root-Knot Disease Suppression in Eggplant Based on Three Growth Ages of Ganoderma lucidum.

This investigation presents a novel finding showing the effect of culture filtrates (CFs) of macrofungi, Ganoderma lucidum, against Meloidogyne incognita evaluated in vitro and in planta. To determine the nematicidal activity, juveniles of M. incognita were exposed to Ganoderma CFs of three different ages (Two, four and eight weeks old) of pileus and stipe at different concentrations, i.e., 100%, 50%, 10% and 1% for different time intervals (12, 24, 48 and 72 h). Ganoderma species were examined morphologically based on external appearance and analytically using SEM. The ethanolic samples of basidiocarp were prepared and analyzed for in vitro nematicidal assay and different bioactive compounds. The in vitro experiment results revealed that among all three ages of pileus and stipe, two-week-old pileus and stipe exhibited great nematotoxic potency and caused 83.8% and 73.8% juveniles' mortality at 100% concentration after 72 h of exposure time, respectively. Similarly, the two-week-old pileus and stipe showed the highest egg hatching inhibition of 89.2% and 81.0% at the 100% concentration after five days. The eight-week-old pileus and stipe were not more effective than the two- and four-week-old pileus and stipe. The metabolites were characterized using GC-MS, including sugar alcohol, steroids, silanes, glucosides, pyrones, ester, oleic acid, phthalic acid, linoleic acid, palmitates and ketones. The in planta study conducted in the greenhouse demonstrated that the root dip treatment for 30 min with Ganoderma CFs curtailed the infection level of M. incognita and promoted the eggplant plant growth. The maximum percent increase in plant length, plant fresh weight, plant dry weight, total chlorophyll, carotenoids and yield/plant was obtained at 100% conc. of fungus CFs, whereas a reduction was observed in nematode infestation parameters. It was concluded from the study that Ganoderma CFs can be explored as an effective and eco-friendly antinemic biocontrol agent in fields infected with root-knot nematodes.

Green Nanotechnology: Plant-Mediated Nanoparticle Synthesis and Application.

The key pathways for synthesizing nanoparticles are physical and chemical, usually expensive and possibly hazardous to the environment. In the recent past, the evaluation of green chemistry or biological techniques for synthesizing metal nanoparticles from plant extracts has drawn the attention of many researchers. The literature on the green production of nanoparticles using various metals (i.e., gold, silver, zinc, titanium and palladium) and plant extracts is discussed in this study. The generalized mechanism of nanoparticle synthesis involves reduction, stabilization, nucleation, aggregation and capping, followed by characterization. During biosynthesis, major difficulties often faced in maintaining the structure, size and yield of particles can be solved by monitoring the development parameters such as temperature, pH and reaction period. To establish a widely accepted approach, researchers must first explore the actual process underlying the plant-assisted synthesis of a metal nanoparticle and its action on others. The green synthesis of NPs is gaining attention owing to its facilitation of the development of alternative, sustainable, safer, less toxic and environment-friendly approaches. Thus, green nanotechnology using plant extract opens up new possibilities for the synthesis of novel nanoparticles with the desirable characteristics required for developing biosensors, biomedicine, cosmetics and nano-biotechnology, and in electrochemical, catalytic, antibacterial, electronics, sensing and other applications.

Oxaliplatin delivery via chitosan/vitamin E conjugate micelles for improved efficacy and MDR-reversal in breast cancer.

A bioinspired chitosan/vitamin E conjugate (Ch/VES, 1:4) was synthesized, optimized based on chitosan's molecular weight (15, 300 kDa), and was assembled to entrap oxaliplatin (OXPt). 1H NMR, infrared spectroscopy, chromatography, X-ray photoelectron spectroscopy, X-ray diffraction, drug release, hemolysis, and stability studies were performed to characterize OXPt@Ch/VES micelles. The therapeutic efficacy of the micelles was tested in vitro in ER+/PR+/HER2- and triple-negative sensitive/resistant breast cancer cells, MCF-7 and MDA-MB-231 via cellular uptake, cytotoxicity, nuclear staining, DNA fragmentation, mitochondrial membrane potential, ROS generation, apoptosis, and cell cycle assays and in vivo using 4T1(Luc)-tumor-bearing mice. OXPt@Ch/VES Ms exhibited decreased IC50 towards MCF-7, MDA-MB-231 (sensitive/resistant) than OXPt. OXPt@Ch/VES Ms caused extensive DNA damage, mitochondrial depolarization, apoptosis, and cell-growth arrest (G2/M). OXPt@Ch/VES Ms treatment retarded tumor growth significantly, prolonged survival, and decreased nephrotoxicity than OXPt. The OXPt@Ch/VES Ms could serve as a potential nanomedicine to overcome conventional OXPt-mediated drug resistance/nephrotoxicity in breast cancer.

Isolation, Identification, and Biocontrol Potential of Entomopathogenic Nematodes and Associated Bacteria against Virachola livia (Lepidoptera: Lycaenidae) and Ectomyelois ceratoniae (Lepidoptera: Pyralidae).

Virachola livia (Lepidoptera: Lycaenidae) and Ectomyelois ceratoniae (Lepidoptera: Pyralidae) are the key pests of pomegranates in Saudi Arabia that are managed mainly using broad-spectrum pesticides. Interactions between the entomopathogenic nematodes (EPNs) Steinernematids, and Heterorhabditids, and their entomopathogenic bacterial symbionts (EPBs) have long been considered monoxenic 2-partner associations responsible for killing insects and, therefore, are widely used in insect pest biocontrol. However, there are limited reports identifying such organisms in Taif, Saudi Arabia. The current study aimed to identify the EPNs and their associated bacteria isolated from Taif, Saudi Arabia, and evaluate their biocontrol potential on third instar larvae of V. livia and E. ceratoniae under laboratory conditions. A total of 35 EPN isolates belonging to Steinernema (20) and Heterorhabditis (15) were recovered from 320 soil samples. Twenty-six isolates of symbiotic or associated bacteria were isolated from EPNs and molecularly identified as Xenorhabdus (6 isolates), Photorhabdus (4 isolates), Pseudomonas (7), or Stenotrophomonas (9). A pathogenicity assay revealed that Steinernema spp. were more virulent than Heterorhabditis spp. against the two pomegranate insects, with LC50 values of 18.5 and 13.6 infective juveniles (IJs)/larva of V. livia for Steinernema spp. and 52 and 32.4 IJs/larva of V. livia for Heterorhabditis spp. at 48 and 72 h post-treatment, respectively. Moreover, LC50 values of 9 and 6.6 IJs/larva (Steinernema spp.) and 34.4 and 26.6 IJs/larva (Heterorhabditis spp.) were recorded for E. ceratoniae larvae at 48 and 72 h post-treatment. In addition, the EPB Stenotrophomonas maltophilia CQ1, isolated from Steinernema spp., surpassed Pseudomonas mosselii SJ10, associated with Heterorhabditis spp., in their ability to kill V. livia or E. ceratoniae larvae within 6 h post-application, resulting in 100% mortality in both insects after 24 and 48 h of exposure. We conclude that either application of EPNs' IJs or their associated EPBs could serve as potential biocontrol agents for V. livia and E. ceratoniae.

Effect of Individual, Simultaneous and Sequential Inoculation of Pseudomonas fluorescens and Meloidogyne incognita on Growth, Biochemical, Enzymatic and Nonenzymatic Antioxidants of Tomato (Solanum lycopersicum L.).

This study was conducted on tomato (Solanum lycopersicum cv. K-21) to investigate the bioprotective nature of Pseudomonas fluorescens and its interactive effects with Meloidogyne incognita in terms of growth biomarkers, changes in biochemical attributes and modulation in antioxidant enzymes of the tomato plant. In this study, we grew tomato plants with M. incognita and P. fluorescens in separate pots, simultaneously and sequentially (15 days prior or post) after 15 days of seed sowing. The sequential inoculation of Mi15→Pf maximally increased the root-knot index and decreased the nematode population. It was also noted that inoculation suppressed the plant growth biomarkers in comparison to control. However, maximum suppression in nematode reproduction and increment in growth and physiological attributes were observed when P. fluorescens was applied 15 days prior to the nematode (Pf15→Mi) as compared to control. All the treatments showed an increase in antioxidant enzymes. Expression of phenol content and defensive enzymes such as peroxidase (POX) and superoxide dismutase (SOD) increased, in contrast to a significant reduction in malondialdehyde (MDA) and hydrogen peroxide (H2O2) contents when compared with the untreated inoculated plants. However, the highest levels of POX and SOD, and a lowest of phenol, MDA and H2O2 were displayed in the treatment Pf15→Mi, followed by Mi+Pf and Mi15→Pf.

New insights on the utilization of ultrasonicated mustard seed cake: chemical composition and antagonistic potential for root-knot nematode, Meloidogyne javanica.

This study focused, for the first time, on the effect of ultrasonic features on the extraction efficiency of secondary metabolites in mustard seed cake (MSC). The nematostatic potential of sonicated seed cake was examined against the second-stage juveniles (J2s) of root-knot nematode, Meloidogyne javanica. The results show that a 35 ppm (parts per million) concentration of a sonicated extract (SE) sample of MSC caused 65% J2s mortality at 18 h exposure period in vitro. It also significantly suppressed the root-knot index (RKI=0.94) in tomato roots. The lethal concentration values for SE were 51.76, 29.79, and 13.34 ppm, respectively, at 6, 12, and 18 h of the exposure period, and the lethal concentration values for the non-sonicated extract (NSE) sample were 116.95, 76.38, and 55.59 ppm, respectively, at similar exposure time. Sinapine and gluconapin were identified as the major compounds in ultrasonic-assisted MSC. Because of the high extraction efficiency of metabolites in the SE, all treatments of SE were shown to be antagonistic to J2s. Thus, this study of ultrasonication activity-based profiling of MSC may help generate target-based compounds at a scale relevant to the control of disease caused by nematodes in economic crops.

Exosomes Harnessed as Nanocarriers for Cancer Therapy - Current Status and Potential for Future Clinical Applications.

Exosomes are nano structured (50-90 nm) vesicles that originate from endosomal compartment of eukaryotic cells and are secreted into extracellular matrix. In recent years, there has been increased interest in exploring exosomes for diagnostic and therapeutic applications. Like many other diseases, e.g., neurodegenerative disorders, autoimmune diseases exosomes have a considerable significance in cancer too. Exosomes are known to prevail in large numbers and carry unique cargos in different types of cancers and thus are proving as versatile entities in understanding their biology of cancers and utilized as efficient diagnostic biomarkers in identification of cancer type. In addition to diagnostic applications, there has been an increased interest in recent years to exploit exosomes as carriers for delivery of therapeutic agents to target sites as well. This is indebted to their exceptional non-immunogenic and biomimetic properties that prompted researchers to use exosomes as carriers for delivery of therapeutic agents, e.g., drugs, genes and peptides. Exosomes also circumvent many drawbacks associated with other lipid or polymeric nanocarriers, e.g., low circulation time, lipid toxicities, long term stability, etc. However, in spite of many favorable aspects of exosome based therapy, there have been a number of challenges too. This review will focus on the current status of the exosome based drug therapy for cancer, the challenges faced and its potential for future clinical use.

Steroidal thiazolidinone derivatives: Design, synthesis and their molecular interaction with human serum albumin.

A series of steroidal thiazolidinone derivatives have been synthesized through one-pot multicomponent reaction involving steroidal ketone, thiosemicarbazide/methyl-thiosemicarbazide and DMAD in presence of AlCl3 as a Lewis acid catalyst. Among all the synthesized steroidal thiazolidinone derivatives, compound 7-9 (ST 7-9) were investigated for their in vitro molecular interaction with human serum albumin. Intrinsic fluorescence spectroscopy, constant wavelength synchronous fluorescence spectroscopy, circular dichroism and UV-visible absorption techniques have been exploited to characterize the binding phenomena in phosphate buffer solution at pH 7.4. The experimental results indicated that ST 7-9 bind to HSA and the intrinsic fluorescence of HSA was quenched through static quenching mechanism. The binding parameters were calculated and the binding constants obtained were 1.44 × 105 M-1 for ST 7, 0.84 × 105 M-1 for ST 8 and 1.06 × 105 M-1 for ST 9. Circular dichroism analysis confirms that the presence of ST 7-9, altered the secondary structure of HSA due to partial unfolding of the polypeptide chain. Furthermore, hemolytic activity assay demonstrated that the synthesized steroidal thiazolidinone derivatives have good compatibility towards human red blood cells. Finally, molecular docking studies revealed that the steroidal thiazolidinones can bind in the hydrophobic cavity of HSA, by hydrophobic and hydrogen bonding interaction. These results provided valuable information about the binding mechanism of ST 7-9 with HSA and play a pivotal role in the development of steroidal heterocycle inspired compounds.