PREDICTION OF ACTIVITY SPECTRA OF SUBSTANCES ASSISTED PREDICTION OF BIOLOGICAL ACTIVITY SPECTRA OF POTENTIAL ANTI-ALZHEIMER'S PHYTOCONSTITUENTS

Objective: To predict the biological activity of certain phytoconstituents for their anti-AD effects.Methods: Several phytoconstituents were selected on the basis of reported literature. The anti-AD activities of selected phytoconstituents were predicted by employing canonical simplified molecular-input line-entry system obtained from PubChem using PASS online.Results: Several phytoconstituents were predicted to have effects better than marketed drugs under some or the other out of the chosen six areas of pharmacological intervention. On the other hand, several new avenues were predicted in which the in vitro and in vivo evaluation of the phytoconstituents can be made on the basis of PASS predicted activities.Conclusion: PASS is an important tool for virtually screening the compounds of interest for the biological activities of interest. This helps the researchers to streamline the research. However, PASS has its own share of limitations amidst a multitude of merits

PHYTO-PHARMACOLOGICAL PROPERTIES OF SIDA CORDIFOLIA: A REVIEW OF FOLKLORE USE AND PHARMACOLOGICAL ACTIVITIES

ABSTRACTPlants have been considered to be useful as a medicine for treating different ailments and improving health conditions, since ancient times. Theplants as herbal drugs lay down an important foundation of different, well recognized, ancient, and traditional healthcare systems in India as well asother parts of the world. In India, plants constitute an important and indispensable role in different ancient healthcare systems such as Ayurveda,Siddha, Unani, Naturopathy, and Homeopathy. In Ayurveda system of medicine, one of the Rasayana plants having a great medicinal importance isSida cordifolia belonging to the family Malvaceae. It is an annual undershrub found throughout the tropical and subtropical regions of India. It hasbeen used since ancient times for various ailments in Ayurveda system of medicine. It has numerous folklore uses in different pathological conditions.The plant also reported to possess a number of important pharmacological activities. The present review focused on all these folklore use of this herbalong with its reported pharmacological activities.Keywords: Sida cordifolia, Ayurveda, Parkinson's disease, Analgesic, Anti-inflammatory

HUMAN PAPILLOMAVIRUS AND ITS NATURE OF INFECTION: AN OVERVIEW

Human papillomavirus (HPV) belonging to Papillomaviridae (family of Papillomavirus). HPV infection causes various types of disorders and diseases including cervical, vaginal, anal, penile, oropharyngeal, and lung cancer also cancer in head and neck along with some malignant and benign warts. HPV also found to be responsible for respiratory papillomatosis. Epidermodysplasia verruciformis, an orphan disease termed as tree man disease, is also occurred by the HPV infection. Vaccines show benefit nowadays. Some surgery and adjuvant therapy is also showing response in the treatment of HPV caused cancers. In this abstract, we summarized the types, structures, genomic organization, mode of transmission of the virus along with type of infections, and protection and modern treatment approaches

PREDICTION OF ANTI-PARKINSON POTENTIAL OF PHYTOCONSTITUENTS USING PREDICTION OF ACTIVITY SPECTRA OF SUBSTANCES SOFTWARE

Objective: Neurodegenerative disorders are group of diseased conditions in which there is loss of neuron cells occur. The main objective of this study to find/search out the phytochemical with the help of prediction of activity spectra of substances (PASSs), those show maximum activity over the selected targets of the Parkinson's disease (PD).Methods: PASSs is a valuable software which is used in this study, to predict the anti-Parkinson activity of different compounds. Canonical simplified molecular-input line-entry system is used for the prediction of anti-Parkinson activity which is obtained from PubChem website. The predicted activity also compared with marketed compound like levodopa.Results: From the study, it was found that resveratrol was the only compound which has the activity on all the selected targets. On the other hand, stemazole and celastrol were found to have the least active compounds as both have the activity only on a single target.Conclusion: In this research work, we tried to compile the information regarding the PASS predicted anti-Parkinson activity of some important phytoconstituents. We found that resveratrol can be a target for further investigation in the development of drug therapy for PD

IDENTIFICATION OF POSSIBLE MOLECULAR TARGETS OF POTENTIAL ANTI-PARKINSON DRUGS BY PREDICTING THEIR BINDING AFFINITIES USING MOLECULAR DOCKING TECHNIQUE

Objective: Mechanistic study of newly reported anti-Parkinson agents by molecular docking to predict possible target.Methods: Structures of newer drugs known anti-Parkinson agents were drawn using ChemBioDraw 2D software. Thereafter, they were converted to 3D structures using ChemBioDraw 3D software in which they were subjected to energy minimization using the MM2 method and then saved as PDB extension files, which can be accessed using the AutoDock Vina (ADT) interface. ADT 1.5.6 software version was used for molecular docking study.Results: Various molecular targets were selected (D2/D3, D2, A2A, and MAO-B) and studied for Pardoprunox, Istradefylline, Rasagiline, and Bromocriptine. Pardoprunox, Istradefylline, and Bromocriptine had more affinity with their corresponding receptor with −6.9, −8.5, and −9.4 kcal/mol binding affinity, respectively, except Rasagiline, who has less affinity with its corresponding receptor (−6.4kcal/mol) and shown better affinity with 3pbl receptor (−6.7 kcal/mol).Conclusion: Pardoprunox, Istradefylline, and Bromocriptine were found to act on D2/D3 (3pbl), A2A (3pwh), and D2 (4yyw), respectively, whereas Rasagiline found to be act on D2/D3 (3pbl) receptor. The results help in prediction of mechanism and interaction to various Parkinson's disease targets

Diabetes Insipidus: Types, Diagnosis and Management

Diabetes insipidus (DI) is an acquired or hereditary water imbalance disorder characterized by polydipsia and polyuria. It is a condition that involves the excretion of dilute urine in large volumes. The illness can strike at any age, with males and females have identical rates of occurrence of the disease. The two main mechanisms responsible for diabetes insipidus are either insufficient release or production of ADH (antidiuretic hormone) from the hypothalamus (central diabetes insipidus) or ADH resistance in which the kidneys are unable to respond to ADH (nephrogenic diabetes insipidus). Another form of DI is transient diabetes insipidus commonly known as gestational diabetes insipidus that occurs in the second/third trimester of pregnancy due to increased levels of placental vasopressinase that occurs progressively during pregnancy and increases metabolic clearance of vasopressin. The fourth type of DI is primary polydipsia, characterized by elevated levels of water intake that physiologically lower vasopressin and may be psychogenic, iatrogenic or dipsogenic. Signs and symptoms of DI often include water electrolyte-imbalance, excessive or severe thirst, frequent and excessive urination, fatigue, dehydration, and weight loss. Diabetes insipidus (DI) should be distinguished from primary polydipsia, and whether it is caused by a central, nephrogenic, or gestational cause. This distinction is critical since incorrect treatment can result in serious repercussions. Diagnosis of DI includes measurement of plasma sodium and osmolality, baseline copeptin, hypertonic saline stimulation and arginine stimulation test. The treatment for DI includes the use of drugs such as desmopressin, thiazide diuretics, indomethacin and amiloride

Structure and expression analysis of early auxin-responsive Aux/IAA gene family in rice (Oryza sativa)

Auxin exerts pleiotropic effects on plant growth and development by regulating the expression of early auxin-responsive genes of auxin/indoleacetic acid (Aux/IAA), small auxin-up RNA, and GH3 classes. These genes have been studied extensively in dicots like soybean and Arabidopsis. We had earlier characterized a cDNA of the first monocot member of Aux/IAA family from rice. The achievement of the large scale rice genome sequencing combined with the availability of full-length cDNA sequences from Knowledge-based Oryza Molecular Biological Encyclopedia provided us the opportunity to draw up the first comprehensive list of Aux/IAA genes in a monocot. By screening the available databases, we have identified 31 Aux/IAA genes having high sequence identity within the conserved domains I, II, III, and IV. The genomic organization as well as chromosomal location of all the Oryza sativa indoleacetic acid (OsIAA) genes is reported. The rice Aux/IAA proteins can be classified in two groups (A and B) on the basis of their phylogenetic relationship with Arabidopsis Aux/IAA proteins. An evolutionary pattern of the rice Aux/IAA genes has been discussed by analyzing their structure (exon/intron organization) and duplications. Interestingly, the duplication of rice Aux/IAA genes was found to be associated with chromosomal block duplication events in rice. The in-silico analysis has been complemented with real-time polymerase chain reaction analysis to quantify transcript levels of all Aux/IAA family members. OsIAA genes showed differential and overlapping organ-specific expression patterns in light- and dark-grown seedlings/plants. Although auxin enhanced the transcript abundance of most of the OsIAA genes, the effect was more pronounced on OsIAA9, 14, 19, 20, 24, and 31. These results provide a foundation for future studies on elucidating the precise role of rice Aux/IAA genes in early steps of auxin signal transduction

Hypoxia-inducible factor (HIF): fuel for cancer progression

Hypoxia is an integral part of the tumor microenvironment, caused primarily due to rapidly multiplying tumor cells and a lack of proper blood supply. Among the major hypoxic pathways, HIF-1 transcription factor activation is one of the widely investigated pathways in the hypoxic tumor microenvironment (TME). HIF-1 is known to activate several adaptive reactions in response to oxygen deficiency in tumor cells. HIF-1 has two subunits, HIF-1β (constitutive) and HIF-1α (inducible). The HIF-1α expression is largely regulated via various cytokines (through PI3K-ACT-mTOR signals), which involves the cascading of several growth factors and oncogenic cascades. These events lead to the loss of cellular tumor suppressant activity through changes in the level of oxygen via oxygen-dependent and oxygenindependent pathways. The significant and crucial role of HIF in cancer progression and its underlying mechanisms have gained much attention lately among the translational researchers in the fields of cancer and biological sciences, which have enabled them to correlate these mechanisms with various other disease modalities. In the present review, we have summarized the key findings related to the role of HIF in the progression of tumors

Targeting eosinophils in respiratory diseases: Biological axis, emerging therapeutics and treatment modalities

Eosinophils are bi-lobed, multi-functional innate immune cells with diverse cell surface receptors that regulate local immune and inflammatory responses. Several inflammatory and infectious diseases are triggered with their build up in the blood and tissues. The mobilization of eosinophils into the lungs is regulated by a cascade of processes guided by Th2 cytokine generating T-cells. Recruitment of eosinophils essentially leads to a characteristic immune response followed by airway hyperresponsiveness and remodeling, which are hallmarks of chronic respiratory diseases. By analysing the dynamic interactions of eosinophils with their extracellular environment, which also involve signaling molecules and tissues, various therapies have been invented and developed to target respiratory diseases. Having entered clinical testing, several eosinophil targeting therapeutic agents have shown much promise and have further bridged the gap between theory and practice. Moreover, researchers now have a clearer understanding of the roles and mechanisms of eosinophils. These factors have successfully assisted molecular biologists to block specific pathways in the growth, migration and activation of eosinophils. The primary purpose of this review is to provide an overview of the eosinophil biology with a special emphasis on potential pharmacotherapeutic targets. The review also summarizes promising eosinophil-targeting agents, along with their mechanisms and rationale for use, including those in developmental pipeline, in clinical trials, or approved for other respiratory disorders