scholarly journals Simulation of Physicochemical and Pharmacokinetic Properties of Vitamin D3 and Its Natural Derivatives

2020 ◽  
Vol 13 (8) ◽  
pp. 160
Author(s):  
Subrata Deb ◽  
Anthony Allen Reeves ◽  
Suki Lafortune

Vitamin D3 is an endogenous fat-soluble secosteroid, either biosynthesized in human skin or absorbed from diet and health supplements. Multiple hydroxylation reactions in several tissues including liver and small intestine produce different forms of vitamin D3. Low serum vitamin D levels is a global problem which may origin from differential absorption following supplementation. The objective of the present study was to estimate the physicochemical properties, metabolism, transport and pharmacokinetic behavior of vitamin D3 derivatives following oral ingestion. GastroPlus software, which is an in silico mechanistically-constructed simulation tool, was used to simulate the physicochemical and pharmacokinetic behavior for twelve vitamin D3 derivatives. The Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) Predictor and PKPlus modules were employed to derive the relevant parameters from the structural features of the compounds. The majority of the vitamin D3 derivatives are lipophilic (log P values >5) with poor water solubility which are reflected in the poor predicted bioavailability. The fraction absorbed values for the vitamin D3 derivatives were low except for calcitroic acid, 1,23S,25-trihydroxy-24-oxo-vitamin D3, and (23S,25R)-1,25-dihydroxyvitamin D3-26,23-lactone each being greater than 90% fraction absorbed. Cytochrome P450 3A4 (CYP3A4) is the primary hepatic enzyme along with P-glycoprotein involved in the disposition of the vitamin D derivatives. Lipophilicity and solubility appear to be strongly associated with the oral absorption of the vitamin D3 derivatives. Understanding the ADME properties of vitamin D3 derivatives with the knowledge of pharmacological potency could influence the identification of pharmacokinetically most acceptable vitamin D3 derivative for routine supplementation.

2021 ◽  
Vol 9 (B) ◽  
pp. 1596-1601
Author(s):  
Lamiaa K. Elsayyad ◽  
Alaa Shafie ◽  
Mazen Almehmadi ◽  
Amal F. Gharib ◽  
Ahmad El Askary ◽  
...  

BACKGROUND: Low Vitamin D levels associated with obesity have reached an epidemic level all over the world. It has been supposed that the low serum level of Vitamin D3 in obese subjects may be due to an increase in the uptake of Vitamin D3 by adipose tissue. AIM: The current study aimed to investigate the effect of a specially designed exercise program for boosting lipolysis on the Vitamin D level in obese children. METHODS: Thirty obese male children participated in the study. Their age was ranged from 9 to 11 years. The participants were assigned to two groups, Group I (GI) who received endurance exercise (ENE) only and Group II (GII) who received the specially designed exercise for increasing lipolysis (ENE preceded by resistance exercise). Free fatty acids (FFA), glycerol, and 25(OH)D were assessed before and immediately after exercise. RESULTS: FFA and glycerol showed a significant increase in both groups following exercise, while 25(OH)D showed a significant increase only in GII. GII showed significantly higher levels of FFA, glycerol, and 25(OH)D following exercise when it was compared to GI. CONCLUSION: The application of resistance training before ENE could improve the Vitamin D status through increasing the lipolytic activities more than the application of endurance exercise alone.


Nutrients ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 2602
Author(s):  
Luis G. Vargas Buonfiglio ◽  
Oriana G. Vanegas Calderon ◽  
Marlene Cano ◽  
Jacob E. Simmering ◽  
Philip M. Polgreen ◽  
...  

Background: It is widely unknown why respiratory infections follow a seasonal pattern. Variations in ultraviolet B (UVB) light during seasons affects cutaneous synthesis of vitamin D3. Serum vitamin D concentration influences the expression of airway surface liquid (ASL) antimicrobial peptides such as LL-37. Objective: We sought to determine the effect of seasons on serum vitamin D levels and ASL antimicrobial activity. Methods: Forty participants, 18–60 years old, were randomized 1:1 to receive 90 days of 1000 IU vitamin D3 or placebo. We collected ASL via bronchoscopy and measured serum 25(OH) vitamin D from participants before and after intervention across seasons. We measured ASL antimicrobial activity by challenging samples with bioluminescent Staphylococcus aureus and measured relative light units (RLUs) after four minutes. We also investigated the role of LL-37 using a monoclonal neutralizing antibody. Results: We found that participants, prior to any intervention, during summer–fall (n = 20) compared to winter–spring (n = 20) had (1) decreased live bacteria after challenge (5542 ± 175.2 vs. 6585 ± 279 RLU, p = 0.003) and (2) higher serum vitamin D (88.25 ± 24.25 vs. 67.5 ± 45.25 nmol/L, p = 0.026). Supplementation with vitamin D3 increased vitamin D levels and restored ASL antimicrobial activity only during the winter–spring. The increased ASL antimicrobial activity seen during the summer–fall was abrogated by adding the LL-37 neutralizing antibody. Conclusion: ASL kills bacteria more effectively during the summer–fall compared to the winter–spring. Supplementation of vitamin D during winter–spring restores ASL antimicrobial activity by increasing the expression of antimicrobial peptides including LL-37.


2020 ◽  
Vol 7 (6) ◽  
pp. 971
Author(s):  
Divya V. Patil ◽  
Tarun Kumar Dutta

Background: Vitamin D, a fat-soluble vitamin is produced when ultraviolet rays from sunlight strike the skin. Literature data supports, there is a relationship between low vitamin D and pathogenesis of cardiovascular diseases and arterial hypertension. It had been seen that lower circulating 25(OH)D levels were associated with higher blood pressures. Aim was to study the correlation between serum vitamin D3 levels and blood pressure in patients with essential hypertension and normotensive individuals.Methods: An observational study was conducted on 60 individuals in the OPD at MGMCRI between January 2018 and December 2018. Based on history and blood pressure values (JNC 7), the population was divided into cases and controls in accordance with the age and sex. Serum Vitamin D levels were measured by chemiluminescence assay and classified into deficiency (<20ng/ml), insufficiency (20-30ng/ml) and sufficiency (30-100ng/ml). Statistical analysis was done using independent t test, one way ANOVA and correlation.Results: Among the hypertensive individuals, 90% were Vitamin D deficient and 10% had insufficiency. The mean Serum Vitamin D level in essential hypertension was 14.6±4.401 (p value <0.001). Serum Vitamin D levels were affected significantly by increasing BMI (p value <0.001) and less sunlight exposure (p value <0.001) among both cases and controls. There was also a significant negative correlation between serum vitamin D levels and systolic blood pressure (p <0.001).Conclusions: Isolated systolic hypertension was associated with lower serum Vitamin D levels. Obesity and reduced sunlight exposure are factors associated with lower serum Vitamin D levels.


2020 ◽  
Vol 90 (3-4) ◽  
pp. 346-352
Author(s):  
Vincenzo Pilone ◽  
Salvatore Tramontano ◽  
Carmen Cutolo ◽  
Federica Marchese ◽  
Antonio Maria Pagano ◽  
...  

Abstract. We aim to assess the prevalence of vitamin D deficiency (VDD) in patients scheduled for bariatric surgery (BS), and to identify factors that might be associated with VDD. We conducted a cross-sectional observational study involving all consecutive patients scheduled for BS from 2017 to 2019. The exclusion criteria were missing data for vitamin D levels, intake of vitamin D supplements in the 3 months prior to serum vitamin D determination, and renal insufficiency. A total of 206 patients (mean age and body mass index [BMI] of 34.9 ± 10.7 years, and 44.3 ± 6.99 kg/m2, respectively) met the inclusion criteria and were enrolled for data analysis. VDD (<19.9 ng/mL), severe VDD (<10 ng/mL), and vitamin D insufficiency (20–29.9 ng/mL) were present in 68.8 %, 12.5 %, and 31.2 % of patients, respectively. A significant inverse correlation was found between vitamin D levels and initial BMI, parathyroid hormone, and homeostatic model assessment of insulin resistance (r = −0.280, p < 0.05; r = −0.407, p = 0.038; r = −0.445, p = 0.005), respectively. VDD was significantly more prevalent in patients with higher BMI [−0.413 ± 0.12, CI95 % (−0.659; −0.167), p = 0.006], whereas no significant association between hypertension [−1.005 ± 1.65, CI95 % (−4.338; 2.326), p = 0.001], and diabetes type 2 (T2D) [−0.44 ± 2.20, CI95 % (−4.876; 3.986), p = 0.841] was found. We observed significant association between female sex and levels of vitamin D [6.69 ± 2.31, CI95 % (2.06; 11.33), p = 0.006]. The present study shows that in patients scheduled for BS, VDD deficiency is common and was associated with higher BMI, and female sex.


Author(s):  
Sanjeeva Kumar Goud T ◽  
Rahul Kunkulol

The present study was aimed to study the effect of Sublingual Vitamin D3 on Serum Vitamin D level in Vitamin D deficiency patients. This was a cross-sectional and interventional study. All the Vitamin D deficiency patients of age 18-60years and either gender, willing to participate in the study were included. Patients who had greater than 20 ng/ml were excluded from the study. The total number of participants in our study was 200, out of these 111 males and 89 females, the mean age in our study was 51.07 ± 7.39Yrs. All volunteers were given sublingual vitamin D3 (60,000IU) in six doses every fifteen days of follow up for 3 months. The subject’s serum 25(OH)D levels were estimated before and after the treatment of sublingual vitamin D3. There was a statistically significant difference in serum vitamin D3 level before 16.61±6.71 ng/ml and after 35.80±7.80 ng/ml after treatment with Sublingual Vitamin D3. Six doses of 60,000IU of Vitamin D3 sublingual route having improved the role of serum 25(OH)D levels in the treatment of Vitamin D3 deficiency patients.Keywords: Vitamin D3; Sublingual route


Background: The risk factors for asthma exacerbations are well understood. However, the effect of vitamin D levels on number of asthma exacerbations per year is not clearly studied. The objective of the study was to find out the association of serum vitamin D levels and asthma risk factors on asthma exacerbations. Methods: In this study, ninety-nine subjects from 5 to 15 years of age were recruited at an episode of acute exacerbation. It was a cross sectional study and carried out from 2012 to 2015. Pulmonary function test was done by spirometry. Asthma exacerbation was labeled when forced expiratory volume/ forced vital capacity (FEV1/FVC) ratio was less than 80% (American Thoracic Society). Global Initiative for Asthma (GINA) guidelines were used to classify asthma into mild, moderate and severe persistent asthma. Serum vitamin D levels were measured by chemiluminescence method. Pearson Chi-square test was applied and p value (p<0.05) was considered as statistically significant. Results: Children who had exposure to animal dander had significantly lower asthma exacerbations per year (p-value <0.046). There was no significant association between vitamin D levels and number of exacerbations per years (p-value <0.099). Asthma was prevalent in girls of low socioeconomic status (SES) compared to males. However, there was no significant association between smoke, exercise, home environment, food allergies, weather, pollen and dust with asthma exacerbations. Conclusion: Low levels of vitamin D were not associated with increased number of asthma exacerbations per year. However, children exposed to animal dander had lesser number of exacerbations per year (p-value <0.046). Keywords: Asthma; Vitamin D; Children; Exacerbations, Risk factors.


Pathology ◽  
2021 ◽  
Vol 53 ◽  
pp. S40
Author(s):  
Michael B. Theophilos ◽  
Catherine Lynch ◽  
Jasmina Nguyen ◽  
Ken A. Sikaris

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