scholarly journals Bioinformatics inspiring peptides from toxins as a new alternative in obesity treatment

2021 ◽  
Vol 10 (14) ◽  
pp. e432101422057
Author(s):  
Ana Paula de Aráujo Boleti ◽  
Thiago Antonio Almeida Rodrigues ◽  
Maria Eduarda Freitas Biembengute ◽  
Lincoln Takashi Hota Mukoyama ◽  
Ludovico Migliolo
Keyword(s):  
Side Effects ◽  
Rational Design ◽  
Malignant Tumors ◽  
Treatment Options ◽  
High Body Mass Index ◽  
Lifestyle Changes ◽  
The Body ◽  
Bioactive Molecules ◽  
Nutritional Disorder ◽  
Treatment Of Obesity

Obesity is a nutritional disorder caused by the excessive accumulation of white adipose tissue (WAT) in the body, which is characterized by a high body mass index and interferes with the body's energy balance. Obesity is a major risk factor for a number of different diseases, such as type 2 diabetes, cardiovascular disease, hypertension, fatty liver disease and some malignant tumors. The treatment of obesity primarily focuses on diet and physical exercise; when lifestyle changes fail, drugs and surgery will be considered as treatment options. At present, a number of so‑called anti‑obesity drugs have been developed, which affect digestion and absorption. These drugs can produce significant weight loss in the individual; however, some patients are unwilling to receive this type of treatment, due to side effects such as insomnia, hypertension and dizziness. This perspective shows that rational design is an alternative methodology based on native bioactive molecules for the development of analogous compounds, improved from the point of view of efficiency and side effects. We also show that the modification of peptides from animal toxins can be an interesting alternative in the treatment of obesity, since peptides from toxins have already shown significant anti-inflammatory effects.

Quinoline: an attractive scaffold in drug design

2021 ◽  
Vol 21 ◽  
Author(s):  
Lucas F. E. Moor ◽  
Thatyana R. A. Vasconcelos ◽  
Raisa da R. Reis ◽  
Ligia S. S. Pinto ◽  
Thamires M. da Costa
Keyword(s):  
Side Effects ◽  
Drug Design ◽  
Heterocyclic Compounds ◽  
Rational Design ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Bioactive Molecules ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range

: Quinoline and its derivatives comprise an important group of heterocyclic compounds that exhibits a wide range of pharmacological properties such as antibacterial, antiviral, anticancer, antiparasitic, anti-Alzheimer and anticholesterol. In fact, the quinoline nucleus is found in the structure of many drugs and in rational design in medicinal chemistry for the discovery of novel bioactive molecules. Persistent efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. This review highlights some discoveries on the development of quinoline-based compounds in recent years (2013-2019) focusing on their biological activities, including anticancer, antitubercular, antimalarial, anti-ZIKV, anti-DENV, anti-Leishmania and anti-Alzheimer’s disease.

scholarly journals Synthesis and Evaluation of Chalcone-Quinoline Based Molecular Hybrids as Potential Anti-Malarial Agents

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 4093
Author(s):  
Bonani Vinindwa ◽  
Godwin Akpeko Dziwornu ◽  
Wayiza Masamba
Keyword(s):  
Drug Discovery ◽  
Side Effects ◽  
Rational Design ◽  
Bioactive Molecules ◽  
Molecular Hybridization ◽  
Hybrid Compound ◽  
Expected Outcome ◽  
New Chemical Entities ◽  
Ic50 Values ◽  
Molecular Hybrids

Molecular hybridization is a drug discovery strategy that involves the rational design of new chemical entities by the fusion (usually via a covalent linker) of two or more drugs, both active compounds and/or pharmacophoric units recognized and derived from known bioactive molecules. The expected outcome of this chemical modification is to produce a new hybrid compound with improved affinity and efficacy compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profiles, different and/or dual modes of action, reduced undesired side effects and ultimately lead to new therapies. In this study, molecular hybridization was used to generate new molecular hybrids which were tested against the chloroquine sensitive (NF54) strain of P. falciparum. To prepare the new molecular hybrids, the quinoline nucleus, one of the privileged scaffolds, was coupled with various chalcone derivatives via an appropriate linker to produce a total of twenty-two molecular hybrids in 11%–96% yield. The synthesized compounds displayed good antiplasmodial activity with IC50 values ranging at 0.10–4.45 μM.

Virtue of Nanotechnology in Confronting Obesity: Recent Advances

2020 ◽  
Vol 10 ◽  
Author(s):  
Jashanpreet Singh Sandhu ◽  
Rina Das ◽  
Dinesh Kumar Mehta ◽  
Meenakshi Dhanawat
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Treatment Options ◽  
Sleep Apnoea ◽  
Western World ◽  
Nano Technology ◽  
Recent Developments ◽  
Delivery Strategies ◽  
Treatment Of Obesity ◽  
Health Complications

Background: Obesity has been a serious health issue over the last decades both in the affluent western world and developing countries. Obesity is linked with major health complications such as diabetes, cardiac disorder, cancer, hypertension, sleep apnoea, etc. Available treatments such as bariatric surgery and pharmacotherapy are often accompanied by adverse side effects and poor patient compliance. Nanotechnology is a discipline that is concerned with material characteristics at nanoscale, and offers novel techniques for disease detection, management, and prevention. Objectives: Recent progress in the field of obesity research at its interface with nanotechnology is our focus. Nanomedicine has greatly enhanced the health status of the people suffering from obesity as it provides non-obtrusive techniques for the management and treatment of obesity. Methods: Literature survey was performed using PubMed, Science Direct, and Web of Science search engines with- terms nanotechnology, nanomedicine and obesity. The research was focused primarily on articles published between the years 2000 and 2019. Results: We have described original and innovative approaches in developments of nano-technology based drug delivery strategies. Nanotechnology has been widely proposed to combine herbal medicine for the treatment of obesity, because nano-structured systems might be able to potentiate the action of plant extracts, reducing the required dose and side effects, and improving activity. This will offer a wide era of treatment options which will directly improve the patient’s compliance. Conclusion: This review surveys recent developments of nanotechnology‐based drug delivery strategies are highlighted, and discussed for obesity treatment with an emphasis on the enhanced therapeutic efficiency and minimized side effects. The insights for future development related to the management of obesity are also discussed.

scholarly journals Patient and provider differences in the treatment of opioid-induced constipation: a qualitative study

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Michelle S. Keller ◽  
Alma Jusufagic ◽  
Brennan M. R. Spiegel
Keyword(s):  
Quality Of Life ◽  
Side Effects ◽  
Cancer Pain ◽  
Treatment Options ◽  
Daily Basis ◽  
Lifestyle Changes ◽  
Treatment Preferences ◽  
Structured Interviews ◽  
Related Quality

Abstract Background Patients using opioids to treat chronic non-cancer pain often experience side effects that may affect health-related quality of life (HRQOL). These side effects include opioid-induced constipation (OIC), sedation, dizziness, and nausea. OIC can significantly affect HRQOL for patients on a daily basis. However, it is not well understood whether patients and clinicians view OIC management similarly. Aims In this study, we sought to elucidate the decision-making process around managing OIC by assessing patient and provider treatment preferences, experiences, and communication regarding this condition. Methods We conducted semi-structured interviews with 33 clinicians, and held three focus groups with patients who were currently using or had used opioids for chronic non-cancer pain. We then analyzed transcribed interviews using descriptive qualitative methods based on grounded theory methodology. Results Clinicians recognized OIC as a concern but prioritized pain management over constipation. They focused on medication-based treatments for OIC, but also recommended lifestyle changes (e.g., diet) and reducing opioids to relieve symptoms. Patients reported using over-the-counter treatments, but the majority focused on diet-related constipation management. Patients reported not receiving adequate information from clinicians about OIC and relevant treatments. Cost of treatment was a major concern for both patients and clinicians. Conclusions Assessing experiences with and preferences for OIC treatment, including cost, ease of access, and side effects, could improve patient-provider communication and HRQOL. Quality improvement efforts can target uncovered misalignments between patients and clinicians to improve communication about opioid medication adverse effects and relevant treatment options, which may help improve quality of life for patients with chronic pain.

scholarly journals Hyperuricaemia and gout

2020 ◽  
pp. 95-100
Author(s):  
A Kopke ◽  
OBW Greeff
Keyword(s):  
Uric Acid ◽  
Side Effects ◽  
Treatment Options ◽  
The Body ◽  
Acute Gout ◽  
Tophaceous Gout ◽  
Life Threatening ◽  
Inflammatory Drugs ◽  
Urate Crystals

Gout is a painful, inflammatory disease that affects more men than women. The incidence of gout has increased substantially over the past few decades, as evidenced by information from the Rochester project. Some of the risk factors for the development of gout include: increased ethanol intake, high dietary purine consumption, obesity and the use of certain drugs, such as diuretics. Another important risk factor for the development of gout is hyperuricaemia. Hyperuricaemia results from an imbalance between the rate of production and excretion of uric acid in the body. An excess of uric acid thus builds up in the body, supersaturating body fluids and leading to the formation of monosodium urate crystals. These crystals accumulate in tissue and around joints, leading to an acute gout attack. Gout can be divided into four phases, namely asymptomatic hyperuricaemia, acute gout attacks or recurrent gout, intercritical gout and chronic tophaceous gout. Various treatment options are available for gout, and the treatment for each gout patient is determined by the stage of the disease. Nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, corticotropin and colchicine are used for the treatment of acute gout attacks. Allopurinol and probenecid are used for long-term hypouricaemic therapy, while NSAIDs and colchicine are prescribed for the prophylaxis of future gout attacks. All of these treatments have side-effects, ranging from mild to life-threatening in nature. There is a need for novel gout therapies that have fewer side-effects but are still as effective.

Evaluation of the hormonal and biochemical changes in obese and non-obese PCOS Iraqi women before and after vitamin D supplementation

2019 ◽  
Vol 9 (o3) ◽  
Author(s):  
Suaad Muhssen Ghazi ◽  
Fatin Shallal Farhan
Keyword(s):  
Vitamin D ◽  
Serum Vitamin ◽  
Follicular Development ◽  
High Body Mass Index ◽  
Vitamin D Supplementation ◽  
The Body ◽  
Obese People ◽  
Serum Vitamin D ◽  
Before And After ◽  
Granulose Cells

Vitamin D deficiency is common in women with polycystic ovarian syndrome. Vitamin D plays an important physiologic role in reproductive functions of ovarian follicular development and luteinization through altering anti-müllerian hormone signaling, follicular stimulating hormone activity and progesterone production in human granulose cells. Vitamin D is precipitated in adipose fat tissues, making it notable to be used for the body as a result; obese people with high body mass index are already highly expected to have low levels of serum vitamin D.

Efficacy and safety of oral dapsone in acne vulgaris – experience of a tertiary care teaching hospital in central Lahore

2020 ◽  
Vol 14 (2) ◽  
pp. 87-90
Author(s):  
Sadaf Amin Chaudhry ◽  
Nadia Ali Zafar ◽  
Rabia Hayat ◽  
Ayesha Noreen ◽  
Gulnaz Ali ◽  
...  
Keyword(s):  
Side Effects ◽  
Therapeutic Option ◽  
Acne Vulgaris ◽  
Treatment Options ◽  
Tertiary Care ◽  
Poor Response ◽  
Global Assessment Scale ◽  
Severe Acne ◽  
Hematologic Profile

Background: Acne is the eighth most prevalent disease affecting 9.4% of the population worldwide and its prevalence in our country is estimated to be around 5%. Severe inflammatory acne is most likely to leave scars and in order to prevent facial disfigurement due to acne scarring, early treatment is desirable. Various treatment options have been formulated for acne, and are tailored according to the severity of the disease. Numerous clinical trials have been conducted till now, to determine the usefulness and side effect profile of such therapies, making acne treatment a highly studied area in dermatology. Objective of this study is to highlight the fact that oral Dapsone could be used as a cheaper alternate to isotretinoin in recalcitrant severe acne, especially in females where retinoids are sometimes contraindicated. Patients and methods: 51 patients, suffering from severe nodulocystic acne, fulfilling the criteria, were enrolled from the Department of Dermatology, Sir Ganga Ram Hospital, Lahore. All the study patients were given oral Dapsone 50mg for initial two weeks and then 100mg daily for the next 10 weeks along with oral cimetidine and topical clindamycin application twice daily. Investigator Global Assessment Scale (IGAS) was employed to measure effectiveness. The treatment was considered ʽeffectiveʹ if the patient achieves 2 or more than 2-grade improvement or almost clear or clear skin at the end of 12 weeks according to IGAS scale. The lesion counts were also done before the start of therapy (day 1) and at every two weeks follow up for 12 weeks. The change in lesion count observed between the baseline number and that seen at follow up visits was also used to evaluate the effectiveness of oral Dapsone. Safety was analyzed by fortnightly visits of the patients to look for any undesirable side effects and monitoring of the hematologic profile of the patients. Final follow up was done at the end of 16 weeks. Results: The study was conducted on 51 patients, with a ratio of 1:3 for males and females and a mean age of 25.2 years (SD ±5.81). At 12th week, patients had significant reduction in their acne lesions; with 7 patients (13.7%) showing completely clear skin, 17 patients (33.3%) had almost clear skin, 5 patients (9.8%) had 3-grade improvement. Twelve patients (23.5%) had 2-grade improvement from baseline score and only 2 patients (3.9%) had 1-grade improvement from baseline. Based on percentage reduction of lesions, excellent response was seen in 32 patients (62.7%), good response in 9 patients (17.6%), moderate response in 2 patients (3.9%), while no patient showed poor response. Dapsone was discontinued in 8 patients due to derangement of hematologic profile. Conclusion: Oral Dapsone, when given carefully, is a very effective therapeutic option in severe recalcitrant acne, with limited side effects.

Biocompatible Polymers and their Potential Biomedical Applications: A Review

2019 ◽  
Vol 25 (34) ◽  
pp. 3608-3619 ◽  
Author(s):  
Uzma Arif ◽  
Sajjad Haider ◽  
Adnan Haider ◽  
Naeem Khan ◽  
Abdulaziz A. Alghyamah ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Biomedical Applications ◽  
Living System ◽  
Health Condition ◽  
The Body ◽  
Biocompatible Polymers ◽  
Nano Technology ◽  
Artificial Grafts ◽  
Immunological Reactions

Background: Biocompatible polymers are gaining great interest in the field of biomedical applications. The term biocompatibility refers to the suitability of a polymer to body and body fluids exposure. Biocompatible polymers are both synthetic (man-made) and natural and aid in the close vicinity of a living system or work in intimacy with living cells. These are used to gauge, treat, boost, or substitute any tissue, organ or function of the body. A biocompatible polymer improves body functions without altering its normal functioning and triggering allergies or other side effects. It encompasses advances in tissue culture, tissue scaffolds, implantation, artificial grafts, wound fabrication, controlled drug delivery, bone filler material, etc. Objectives: This review provides an insight into the remarkable contribution made by some well-known biopolymers such as polylactic-co-glycolic acid, poly(ε-caprolactone) (PCL), polyLactic Acid, poly(3- hydroxybutyrate-co-3-hydroxyvalerate) (PHBV), Chitosan and Cellulose in the therapeutic measure for many biomedical applications. Methods: : Various techniques and methods have made biopolymers more significant in the biomedical fields such as augmentation (replaced petroleum based polymers), film processing, injection modeling, blow molding techniques, controlled / implantable drug delivery devices, biological grafting, nano technology, tissue engineering etc. Results: The fore mentioned techniques and other advanced techniques have resulted in improved biocompatibility, nontoxicity, renewability, mild processing conditions, health condition, reduced immunological reactions and minimized side effects that would occur if synthetic polymers are used in a host cell. Conclusion: Biopolymers have brought effective and attainable targets in pharmaceutics and therapeutics. There are huge numbers of biopolymers reported in the literature that has been used effectively and extensively.

Using Naïve Bayes Algorithm to Estimate the Response to Drug in Lung Cancer Patients

2019 ◽  
Vol 21 (10) ◽  
pp. 734-748 ◽  
Author(s):  
Baoling Guo ◽  
Qiuxiang Zheng
Keyword(s):  
Lung Cancer ◽  
Side Effects ◽  
Cancer Patients ◽  
Drug Response ◽  
Treatment Options ◽  
Clinical Manifestations ◽  
Treatment Strategies ◽  
Cancer Resistance ◽  
Lung Cancer Patients ◽  
Bayes Algorithm

Aim and Objective: Lung cancer is a highly heterogeneous cancer, due to the significant differences in molecular levels, resulting in different clinical manifestations of lung cancer patients there is a big difference. Including disease characterization, drug response, the risk of recurrence, survival, etc. Method: Clinical patients with lung cancer do not have yet particularly effective treatment options, while patients with lung cancer resistance not only delayed the treatment cycle but also caused strong side effects. Therefore, if we can sum up the abnormalities of functional level from the molecular level, we can scientifically and effectively evaluate the patients' sensitivity to treatment and make the personalized treatment strategies to avoid the side effects caused by over-treatment and improve the prognosis. Result & Conclusion: According to the different sensitivities of lung cancer patients to drug response, this study screened out genes that were significantly associated with drug resistance. The bayes model was used to assess patient resistance.

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