scholarly journals Elagolix Sodium: Novel GnRH Antagonist for the Treatment of Endometriosis

2021 ◽  
pp. 1-3
Author(s):  
Rohit Bhatia

Endometriosis is a category of lesions and fibroids which occur in the innermost lining of the uterus that is the endometrial layer and spreads to the other parts of the neighboring tissues. It is characterized by inflammation, pelvic pain, menstrual bleeding, and Dysmenorrhea. Endometriosis exists in 3 forms based on its spreadability. i.) superficial peritoneal lesions ii.) deep infiltrating lesion and iii.) cyst. Traditional treatments involve are NSAIDS, Oral contraceptives, Aromatase inhibitors, and GnRH agonists. Elagolix emerges out to be the latest potent drug that acts by inhibiting the GnRH receptor. Unlike other allopathy medicine, it is not an asymptomatic pain reliever but acts on the root cause of the disease. FDA has approved it for specific treatment of endometriosis in July 2018. It is believed that endometriosis occurs by an increase in the production of estrogen. Elagolix competitively binds to the GnRH receptors and prevents the binding of the Gonadotropin hormone flowing through blood capillaries from the Hypothalamus to the pituitary gland and thereby stops the formation of Oestrogen in the reproductive system which ultimately ceases in the proliferation of endometrial layers and tissue spread. In estrogen biosynthesis, the aromatase P450 enzyme plays a vital role. Elagolix belongs to BCS class III and available in the oral dosage form of 150, 200mg. It is rapidly absorbed and Cmax reaches within 1hour. The plasma protein binding is 80%. In this review, various aspects related to Elagolix sodium have been summarised, which include pathophysiology, Mode of Action, Structure-activity relationship, Pharmacokinetics, pharmacodynamics, and clinical studies with minimal side effects.

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3287 ◽  
Author(s):  
Berin Karaman Mayack ◽  
Wolfgang Sippl ◽  
Fidele Ntie-Kang

Natural products have been used for the treatment of human diseases since ancient history. Over time, due to the lack of precise tools and techniques for the separation, purification, and structural elucidation of active constituents in natural resources there has been a decline in financial support and efforts in characterization of natural products. Advances in the design of chemical compounds and the understanding of their functions is of pharmacological importance for the biomedical field. However, natural products regained attention as sources of novel drug candidates upon recent developments and progress in technology. Natural compounds were shown to bear an inherent ability to bind to biomacromolecules and cover an unparalleled chemical space in comparison to most libraries used for high-throughput screening. Thus, natural products hold a great potential for the drug discovery of new scaffolds for therapeutic targets such as sirtuins. Sirtuins are Class III histone deacetylases that have been linked to many diseases such as Parkinson`s disease, Alzheimer’s disease, type II diabetes, and cancer linked to aging. In this review, we examine the revitalization of interest in natural products for drug discovery and discuss natural product modulators of sirtuins that could serve as a starting point for the development of isoform selective and highly potent drug-like compounds, as well as the potential application of naturally occurring sirtuin inhibitors in human health and those in clinical trials.


2021 ◽  
Vol 2 (2) ◽  
pp. 61
Author(s):  
Diksha Koul ◽  
Jasmine K. Khosla ◽  
Ravi S. Manhas ◽  
Devtulya Chander ◽  
Asha Chaubey

Background: COVID-19 pandemic has forced the human population to rethink over the lifestyle and food habits being followed by them. During the current scenario, when cases of more virulent new strain are emerging and specific treatment are still underway, we must look back to the Darvin’s theory of “Survival of the fittest” and in order to sustain the pandemic, we must follow the rule “Prevention is better than cure”. Traditional Medicinal System can bring possible solution including prevention and control of COVID-19. Humic substances have been used for antiviral activities, signifying that it has potential applications in the management and prevention of infectious diseases. Summary: Present article is focused on the assessment of the naturally occurring humic substances, which are major constituents of Shilajit, being used in traditional system of medicine and can be used against for the prevention of COVID-19. Key message: Humic substances not only improve the immune system, but also have anti-inflammatory, antioxidant and antiviral activities against human RNA viruses. Therefore, while the entire world is preparing to deal with alarming threat of community spread of COVID-19, Humic substances may play a vital role in improving the innate immunity for prevention and management of SARS-CoV-2 infection


Author(s):  
Ruma Dey ◽  
Chakraborty Swagata ◽  
Das Aparajita

Importance of Agni has been mentioned univocally in almost all classical treatises in Ayurveda. It has also been mentioned that hypo-functioning Agni is the root cause of every diseases. Agni plays a vital role in maintaining health and balancing the equilibrium of Dosa, Dhatu and Mala. So, to bring the function of Agni to normalcy, besides maintaining proper diet and regimen, Deepaniya drugs are advised. Ten members of Deepaniya mahakashaya are discussed here critically based on their Rasapanchak i.e., Rasa, Guna, Virya, Vipaka and Karma. In this review article a comparative study has been done on Deepaniya mahakashaya as mentioned in Charaka Samhita and discussed in relation to Bhavaprakash Nighantu, Dhanwantari Nighantu, Raj Nighantu and Kaiyadev Nighantu. Along with this, the functions of the drugs mentioned in these classics in the light of modern perspectives are also discussed critically.


2021 ◽  
Vol 22 (22) ◽  
pp. 12263
Author(s):  
Anam Naseer ◽  
Snober Shabnam Mir ◽  
Krisztina Takacs-Vellai ◽  
Aamir Nazir

Age-associated neurodegenerative diseases are known to have “impaired protein clearance” as one of the key features causing their onset and progression. Hence, homeostasis is the key to maintaining balance throughout the cellular system as an organism ages. Any imbalance in the protein clearance machinery is responsible for accumulation of unwanted proteins, leading to pathological consequences—manifesting in neurodegeneration and associated debilitating outcomes. Multiple processes are involved in regulating this phenomenon; however, failure to regulate the autophagic machinery is a critical process that hampers the protein clearing pathway, leading to neurodegeneration. Another important and widely known component that plays a role in modulating neurodegeneration is a class of proteins called sirtuins. These are class III histone deacetylases (HDACs) that are known to regulate various vital processes such as longevity, genomic stability, transcription and DNA repair. These enzymes are also known to modulate neurodegeneration in an autophagy-dependent manner. Considering its genetic relevance and ease of studying disease-related endpoints in neurodegeneration, the model system Caenorhabditis elegans has been successfully employed in deciphering various functional outcomes related to critical protein molecules, cell death pathways and their association with ageing. This review summarizes the vital role of sirtuins and autophagy in ageing and neurodegeneration, in particular highlighting the knowledge obtained using the C. elegans model system.


2021 ◽  
Vol 12 (1S) ◽  
pp. 173-183
Author(s):  
Mohamad Afif Hamdi Mohamad Sobri ◽  
Saiful Iskandar Khalit ◽  
Syazreen Syima Sharifuddin

Water is an essential nutrient in the human body and it plays a vital role. Water is required to work in every system in the body, from cells and tissues to vital organs. About 70% of human-used freshwater goes to cultivation. The study aimed to assess water quality and identify the water category of Besut Campus Lake A. Water Quality Index (WQI) related to this study because it is standard used to classify the class of the water body. Water sampling was done at three sampling stations in two different locations and were sampled from February 2021 until March 2021. According to HACH and American Public Health Associations (APHA) methods, ten water quality parameters were analysed based on in situ and ex situ analysis. The values of pH, TDS, Temp, TSS and AN had been classified under Class I referred to National Water Quality Standard (NWQS). At the same time, DO and BOD were classified under Class II. And COD had been classified under Class III according to NWQS classification. Based on WQI, the water quality status in Campus Besut Lake was classified under Class II with a value of 85.742. It had been considered as Clean which is suitable for recreational activities and safe for body contact as well.


People from all walks of life suffer from stress in one-way or the other. Employees stress is the growing concern for organizations in today’s environment. When stress becomes excessive it often affects work performance, which has significantly lead to burnout and turnover. It is necessary to recognize and address the causes of stress and effectively manage prolonged stress. Since it should be an ethical and legal decision for an organization in managing stress. Stress is expression of individual mental and physical reaction to stressor. The objective is to analyze various pressures that trigger job stress, identifying the causes and outcome, stress is not always negative it may also bring the best out of an individual at times, excessive stress may result into burnout. HR can play an active role in managing it. As outlined in the previous sentences that the level of stress at work place should be controlled since, too much of stress leads to burnout, HR can play a very vital role in the organization to curb the level of stress by reducing and identifying the root cause of the stressor by implementing stress audit program by measuring the stress in-terms of cost which will help to quantify the decrease in level of job performance.


2019 ◽  
Vol 2 ◽  
pp. 62-66
Author(s):  
HEMADRI K. SAO ◽  
ABHISHEK K. BHARDWAJ ◽  
GAURAV AGRAWAL

Observation of present scenario indicates that the root cause of widely spread sufferings, distress and mental problems is certainly the distorted, directionless & unfocused thinking. Those who are unable to manage themselves, always live in stress, that in its consequences leads the person towards mental disorders. For mental and physical fitness level one would have to learn the art of self-management; but it is possible only after knowing the self and refining it. Understanding one’s own self and refining would require proper training, guidance and therapy. As there are not enough skillful guides, so one to one guidance is not possible. The solution for this is called “Swadhyaya chikitsa”. It can play a vital role as a therapy. In modern psychology the assumptions of humanistic and existential (phenomenology) therapies come very close to it. It includes the cognitive restructuring in its process of therapy, but this therapy goes beyond normal cognitive therapy as the insights developed here are far more stable and naturally implemented.


Author(s):  
Padmaja Y. Samant ◽  
Juhi Jayadev Puri

Background: The burden of HIV and AIDS comes with social, monetary and health related consequences. HIV is reported to be a pandemic, but the maximum burden of the disease is in the low and middle income \ countries. In obstetric context, sociodemographic factors influence health seeking, compliance and adherence to the advised regimen. These determine vertical transmission. Present study was undertaken to study the demographic characteristics among pregnant and postpartum HIV positive women, to study the high risk obstetric conditions, morbidities and obstetric outcome, among the women, to study the neonatal outcomes among HIV reactive women and to study the postnatal choices and compliance in these women.Methods: The study was conducted after approval from the institutional ethics committee. All antenatal patients delivering at the institute in the one and a half year of study duration, who consented to be a part of the study, were enrolled in the study. The mother-baby pair was followed up for six weeks postpartum.Results: Eighty patients formed the study cohort as per the inclusion criteria. 44% belonged to the age group of 26-30 years. 56.2% had attended up to secondary schooling, 55% belonged to class III of the Kuppuswamy socio-economic class, 96.2% were married. 91.2% were homemakers. 41.8% spouses were seropositive, 25.3% spouses were not willing to be tested. 75% were registered pregnancies out of which 56% had registered before 20 weeks of gestation. 25% of neonates weighed between 2.7-2.9 kg closely followed by those more than 3 kg. Fifty-four patients opted for top feeding (66.7%). Seven mother-baby pair did not follow-up.Conclusions: Social class and educational status play a vital role in establishing awareness and ensuring the antenatal care and compliance. Empathetic, inclusive and responsive by health care providers in convincing women to get tested goes a long way.


Energies ◽  
2021 ◽  
Vol 14 (4) ◽  
pp. 790
Author(s):  
Shabana Urooj ◽  
Fadwa Alrowais ◽  
Ramya Kuppusamy ◽  
Yuvaraja Teekaraman ◽  
Hariprasath Manoharan

In the present scenario the depletion of conventional sources causes an energy crisis. The energy crisis causes load demand with respect to electricity. The use of renewable energy sources plays a vital role in reducing the energy crisis and in reduction of CO2 emission. The use of solar energy is the major source of power in generation as this is the root cause for the development of wind, tides, etc. However, due to climatic condition the availability of PV sources varies from time to time. Hence it is essential to track the maximum source of energy by implementing different types of MPPT algorithms. However, use of MPPT algorithms has the limitation of using the same during partial shadow conditions. The issue of tracking power under partial shadow conditions can be resolved by implementing an intelligent optimization tracking algorithm which involves a computation process. Though many of nature’s inspired algorithms were present to address real world problems, Mirjalili developed the dragonfly algorithm to provide a better optimization solution to the issues faced in real-time applications. The proposed concept focuses on the implementation of the dragonfly optimization algorithm to track the maximum power from solar and involves the concept of machine learning, image processing, and data computation.


Author(s):  
Berin Karaman Mayack ◽  
Wolfgang Sippl ◽  
Fidele Ntie-Kang

Natural products have been used for the treatment of human diseases since ancient history. Over time, due to the lack of precise tools and techniques for the separation, purification, and structural elucidation of active constituents in natural resources there has been a decline in financial support and efforts in characterization of natural products. Advances in the design of chemical compounds and the understanding of their functions is of pharmacological importance for the biomedical field. However, natural products regained attention as sources of novel drug candidates upon recent developments and progress in technology. Natural compounds were shown to bear an inherent ability to bind to biomacromolecules and cover an unparalleled chemical space in comparison to most libraries used for high-throughput screening. Thus, natural products hold a great potential for the drug discovery of new scaffolds for therapeutic targets such as Sirtuins. Sirtuins are Class III histone deacetylases that have been linked to many diseases such as Parkinson`s disease, Alzheimer’s disease, type II diabetes, and cancer linked to aging. In this review, we examine the revitalization of interest in natural products for drug discovery and discuss natural product modulators of Sirtuins that could serve as a starting point for the development of isoform selective and highly potent drug-like compounds.


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