Synthesis Of Vitamin Research Articles

Charactirestics of vitamin D level in patients with atopic dermatitis

The peculiarity of the skin is that it acts not only as a place of synthesis of vitamin D, but also as an organ targeted for its biologically active form. The aim of our study was to analyze the level of vitamin D in patients with atopic dermatitis. There were examined 48 people aged between 18 to 55 years; they are residents of Vinnytsia and Vinnytsia region. Serum levels of vitamin D, total IgE and eosinophilic cationic protein (ECP) were determined in the subjects. The average level of vitamin D in the serum of patients with atopic dermatitis was 19.2 [11.3-25.4] ng/ml, which corresponded to a deficiency. Among those surveyed, vitamin D deficiency was found in 68.4±4.7% (n=26) while vitamin D insufficiency in 31.6±4.5% (n=12). The severe course of the disease prevailed among patients aged 18-40 years (63.33±8.79) % more than in the age group of 41 years and older, (36.67±8.8%, p<0.05; OR=2.98, S=0.53, 95% SI:1.04-8.52). The proportion of people with vitamin D deficiency and moderate severity of atopic dermatitis was 62.5% (n=10) with a median level of 14 [8.3–19] ng/ml, and patients with severe atopic dermatitis made up 90.9% (n=20) (χ²=4.6; p=0.023), in which the median level of vitamin D was 14 [8.3-19] ng/ml. Serum vitamin D levels were in the zone of deficiency in patients with moderate and severe atopic dermatitis. Vitamin D deficiency was significantly more common in the group of patients with elevated levels of allergic inflammation markers. A positive correlation of medium strength between the level of vitamin D and ECP in the serum of patients with atopic dermatitis (rs=0.53, p<0.001), was revealed.

Analysis of Cholesterol from the Liver Using Gas Chromatography-Mass Spectrometry.

Cholesterol is an essential lipid molecule for several biological functions including the proper functioning of cell membranes, lipoproteins, and lipid rafts, as well as the synthesis of bile acids, vitamin D, and steroid hormones. Cholesterol can be extracted from liver tissue by multiple methods of lipid extraction. Subsequently, gas chromatography-mass spectrometry (GC-MS) can be used to obtain the highest level of sensitivity and selectivity in the analysis of cholesterol. This chapter describes two methods of lipid extraction for liver tissue, Bligh and Dyer and methyl tertiary butyl ether (MTBE), followed by an analysis with GC-MS.

Previtamin D action spectrum: Challenging CIE towards a standard

In 2006, CIE published a technical report on an action spectrum for the production of previtamin D3 in human skin. CIE procedure is to publish guidelines (e.g., an action spectrum) and let the community test them before moving to define a standard. The CIE previtamin D3 action spectrum has been in use for 15 years, and challenged on several occasions; a number of alternative action spectra have been suggested. To date (2021) no alternative action spectrum has shown clear advantages over the CIE version when tested against experimental outcomes. Thus, the CIE action spectrum remains widely used, but not fully accepted as best representing the photobiology in human skin leading to synthesis of vitamin D. We report on a CIE workshop designed to address the challenges to the CIE action spectrum, and explore alternative action spectra. The workshop concluded that the CIE action spectrum probably requires amendment, with several candidates for consideration in determining any changes. However, until there is a clear alternative, the CIE action spectrum should remain in use whilst ensuring full spectral information about sources of ultraviolet radiation. Thus, results are comparable between studies and can be recalculated to an updated action spectrum if necessary.

An examination of vitamin D levels as a mediator in the association of ambient air pollution and incident type 2 diabetes mellitus in India

Background & Aim: Recent evidence suggests a role for air pollution and low vitamin D levels in enhancing the risk of diabetes. In India, both air pollution and a high prevalence of vitamin D deficiency exist alongside a high burden of diabetes. Particulate matter also reduces penetration of UVB light into earth’s atmosphere resulting in reduced synthesis of cutaneous vitamin D. We hypothesized that air pollution as measured by PM2.5 is associated with vitamin D levels as measured by 25-OHD in the body, which may mediate association between PM2.5 and incident type 2 diabetes mellitus. Methods: We used a nested prospective case-control study in the Center for Cardiometabolic Risk Reduction in South Asia cohort study in Delhi and Chennai. Cases (n=506) defined as those with incident diabetes mellitus, were matched with healthy controls/non-diabetics (n=506). Multivariable regression analyses were performed to evaluate the associations between varying lag exposures of PM2.5 and incident diabetes. We estimated the mediating effects of vitamin D levels associated with PM2.5 exposure on incident diabetes through causal mediation analyses and boot strapping. Results: 92.4% and 89.9% of cases and controls were vitamin D insufficient (< 30 ng/ml), respectively. We observed statistically significant negative correlation [-0.41 95%CI: -0.35, -0.46] between vitamin D levels and PM2.5 for all the lag periods (1-day, 7-day, 30-day, and 90-day) studied. The association between short-term exposure to PM2.5 and incident diabetes were evident among people who were obese, had higher waist-hip-ratio, and elevated triglyceride levels. The mediating role of low vitamin D was not supported by our dataset. Conclusions: Air pollution appears to interfere with vitamin D synthesis from natural sources. We, however, did not find evidence to support a mediating role of vitamin D on the association between PM2.5 and incident diabetes. Keywords: Air pollution, diabetes mellitus, vitamin D, mediation analysis

Vitamine D voor kinderen in Vlaanderen

Vitamin D for children in Flanders Vitamin D plays a pivotal role in calcium/phosphate homeostasis and a subsequent healthy bone metabolism. In addition, vitamin D potentially has many other functions like a role in the regulation of the immune system. Across Europe, there is consensus to supplement infants under 1 year of age with (at least) 400 IU of vitamin D. However, there is no consensus regarding vitamin D supplementation for older children (as well as the desired levels of 25-OH vitamin D). Endogenous synthesis of vitamin D in the skin takes place under the influence of UVB sunlight. Therefore, in healthy fair-skinned children who spend sufficient time outdoors, a supplement is not necessary, yet harmless. The number of children at risk of deficiency has increased. Risk factors for vitamin D deficiency are dark skin, veiling, the use of complete sun-blocking agents and spending most time indoors. A uniform and straightforward recommendation could increase compliance. Therefore, the Vitamin D working group of the Flemish Association of Pediatricians confirms the recommendation of a universal supplementation of at least 400 IU per day for all children from birth until 6 years. In children with risk factors, this daily supplementation is advised until 18 years of age (and older) and an even higher supplemental dose could be considered. Dosing of serum 25-OH vitamin D as a screening test in healthy children is not recommended. This article should be considered as a narrative review with conclusions based on expert opinion, due to the limited evidence on this topic.

Impact of maternal dietary carbohydrate intake and vitamin D-related genetic risk score on birth length: the Vitamin D Pregnant Mother (VDPM) cohort study

BackgroundOur objectives were to investigate the relationship between maternal vitamin D status and IGF-1 levels in healthy Minangkabau pregnant mothers and their impact on newborn anthropometry outcomes and to examine whether this relationship was modified by dietary intake using a nutrigenetic approach.MethodsHealthy singleton pregnant mother and infant pairs (n = 183) were recruited. We created three genetic risk scores (GRSs): a six-SNP GRS based on six vitamin D-related single nucleotide polymorphisms (SNPs) involved in the synthesis of vitamin D (vitamin D-GRS), a two-SNP GRS using SNPs in VDR genes (VDR-GRS) and a four-SNP GRS using SNPs from DHCR7, GC, CYP24A1 and CYP2R1 genes (non-VDR GRS). The effect of the GRSs on IGF-1, vitamin D and newborn anthropometry and the interaction between the GRSs and dietary factors were tested using linear regression analysis.ResultsThe vitamin D- and non-VDR GRSs were significantly associated with lower 25(OH)D concentration (p = 0.005 and p = 0.001, respectively); however, there was no significant association with IGF-1, and newborn anthropometry outcomes. However, there was a significant interaction of VDR-GRS with carbohydrate intake on birth length outcome (Pinteraction = 0.032). Pregnant mothers who had higher carbohydrate intake (405.88 ± 57.16 g/day) and who carried ≥ 2 risk alleles of VDR-GRS gave birth to babies with significantly lower birth lengths compared to babies born to mothers with < 2 risk alleles (p = 0.008).ConclusionThis study identified a novel interaction between VDR-GRS and carbohydrate intake on birth length outcome. These findings suggest that reducing the intake of carbohydrates during pregnancy, particularly for those who have a higher genetic susceptibility, might be an effective approach for preventing foetal growth abnormalities.

Vitamin D Target Genes in Dental Health

INTRODUCTION: Vitamin D is an important molecule which plays pivotal role in overall human health and metabolism. This vitamin acts as both vitamin as well as hormone, and thus, dual nature of this vitamin makes it as one of the important chemicals required for the overall health, harmonious growth, and development. Recently, this vitamin is gaining large attention in dentistry, and it is becoming master regulator of dental health. It is well studied that vitamin D plays major role in calcium absorption for bone and teeth mineralisation, it acts as odontogenic inducer of differentiation of human dental pulp cells and in tooth development. STUDY SELECTION, DATA, AND SOURCES: Vitamin D regulates various signalling pathways in dental network and plays a beneficial role. Synthesis of vitamin D takes place in multiple steps in human body. The natural form of vitamin D is fat soluble in nature and is produced in the skin from 7-dehydrocholesterol molecules. Natural Sunlight through its ultraviolet B (UVB) energy converts the precursor7-dehydrocholesterol molecules to vitamin D3. Advanced and unhealthy lifestyle of modern times has led to the deficiency of vitamin D and metabolic syndrome. CONCLUSIONS: Deficiency of vitamin D also leads to various dental problems including dental caries, gingivitis, and periodontal disease. In this short review, we are discussing the role of vitamin D and importance of its target genes in dental health. CLINICAL RELEVANCE: Vitamin D has a major role in managing the oral health this article updates the clinician with the different genes which are responsible for the regulation of vitamin D in different tissues.

ORAL LEUKOPLAKIA WITH AND WITHOUT MALIGNANT TRANSFORMATION ARE METABOLICALLY DISTINCT

<h3>Objectives</h3> To compare the metabolic profile of oral leukoplakia with and without malignant transformation. <h3>Study Design</h3> We evaluated samples of untransformed oral leukoplakia (<i>n</i> = 15) and those that underwent malignant transformation (<i>n</i> = 5) by high-performance liquid chromatography-mass spectrometry-based untargeted metabolomics. Univariate and multivariate statistical methods were applied to detect potentially discriminating compounds between groups. The mummichog and gene set enrichment analysis algorithms were associated to predict the enriched biological pathways. <h3>Results</h3> Seventy-two compounds were statistically significant (<i>P</i> < .05) for discriminating our study groups. Multivariate statistical analysis demonstrated the distinct metabolic profile of the samples, revealing a trend for the separation of transformed and untransformed oral leukoplakias. The main enriched pathways were related to lipid metabolism, synthesis of proinflammatory molecules, and retinoic and vitamin E metabolism. <h3>Conclusions</h3> The current results suggest untargeted metabolomics' potential to discriminate malignantly transformed leukoplakias from untransformed ones. Statistical analysis showed compounds that may characterize each evaluated group. Also, the enriched metabolic pathways were consistent with carcinogenesis-related processes. Further evaluation of the significantly altered compounds may be promising for developing a biomarker panel for the early diagnosis of leukoplakia with an increased risk of malignant progression.

Synthesis and preparation of vitamin A coupled butein-loaded solid lipid nanoparticles for liver fibrosis therapy in rats

The development of a therapeutic system for hepatic fibrosis has become a research hotspot to date. Butein, a simple chalcone derivative, displays anti-fibrotic effects through different pathways. However, impurities, low solubility, and low concentration in the target tissue hinder therapy with herbal ingredients. Hepatic stellate cells (HSCs), the vitamin A (VA) storage cells, as the main contributors to liver fibrogenesis, are not readily accessible to drugs owing to their anatomical location. Targeted delivery of therapeutics to the activated HSCs is therefore critical for successful treatment.For these reasons, the current study aimed at increasing butein delivery to the liver. Hence, high purity butein was synthesized in three steps. A novel VA-Myrj52 ester conjugate was also synthesized using all-trans retinoic acid and a hydrophilic emulsifier (Myrj52) as a targeting agent. Next, butein was encapsulated inside the novel VA-modified solid lipid nanoparticles (VA-SLNs) and studied in vitro and in vivo.According to our evaluations, negatively charged SLNs with a mean diameter of 150 nm and entrapment efficacy of 75 % were successful in liver fibrosis amelioration.Intraperitoneal (i.p.) injection of VA-SLNs in fibrotic rats, for four weeks long, reduced serum AST and ALT by 58% (P, 0.001) and 72% (P, 0.05), respectively, concerning the CCl4 group. Additionally, histologic damage score decline and normalization of tissue oxidative stress markers collectively confirmed the efficacy of formulations in hepatic fibrosis and kidney damage amelioration.

RETRACTED: Histological, ultrastructural and immunohistochemical studies on the ameliorative role of Cinnamon zeylanicum against high cholesterol diet-induced hypercholesterolemia in the kidney of adult male albino rats

Cholesterol is an important type of lipid as it is involved in the structure of cell membrane, synthesis of steroid hormones, bile acid and vitamin D. Many diseases affect various mammalian organs, including the kidney, as a result of high cholesterol levels (hypercholesterolemia). Cinnamon zeylanicum (C. zeylanicum) proves its efficiency as it has anti-inflammatory and antioxidant prosperities. This study aimed to investigate the possible ameliorative role of C. zeylanicum on hypercholesterolemia-induced the renal toxicity in albino rats. Forty adult male albino rats were equally divided into four groups. The first group served as the control one. The second group was supplemented with C. zeylanicum powder (15% w/w) with the standard diet. The third group was fed high cholesterol diet (HCD) to induce acute hypercholesterolemia. The fourth group was fed HCD provided with C. zeylanicum powder (15% w/w). At the end of the experiment (8th weeks), kidneys were removed and prepared for histological, immunohistochemical and ultrastructure studies. Rats-fed HCD showed degenerated glomeruli and tubular cells with vacuolated or coagulated cytoplasm and pyknotic nuclei. Moreover, the renal cortex ultrastructural examination showed degenerated podocytes, parietal and mesangial cells, as well as the proximal and distal tubular cells appeared with rarified cytoplasm, degenerated mitochondria, large fat vacuoles and complete damaged microvilli. The same group showed a significant increase in the expression of desmin and inducible nitric oxide synthase. On the other hand, animals fed HCD provided with C. zeylanicum showed an obvious improvement in the observed histological, ultrastructural and immunohistochemical changes. The architecture of the renal cortex appeared mostly similar to the control one. This study concluded that C. zeylanicum has a promising role in treating the nephron-toxicity of HCD due to its natural constituent that is responsible for its pharmaceutical effects.

Industrial Synthesis of Vitamin E

Industrial Synthesis of Vitamin E

Sunscreen- The facts must known

Sunlight is the most important natural source of energy for all living creatures. Sunlight stimulates hormone production, allows synthesis of vitamin D, promotes skin cell regeneration and contributes to an overall sense of well being of an individual. Sunscreens are agents that alter the effects of UV radiation on the skin by absorption or reflection of part of the incident radiation. It protects the skin from carcinogenic effects of burning rays.

Novel approach to A-ring synthon for Pd-catalyzed synthesis of 1α-hydroxylated vitamin D metabolites

A novel approach to an A-ring synthon for Pd-catalyzed synthesis of 1α-hydroxylated vitamin D metabolites is described. Key step is an asymmetric glyoxylate ene reaction to access a highly diastereomerically pure α-hydroxy ester. Subsequent stereospecific transformation to an anti-1,3-diol and appropriate chemical modifications at both ends of the acyclic precursor leads to a diastereomerically and enantiomerically pure silylated anti-1,3-diol enyne, serving as a versatile A-ring synthon for its use in vitamin D synthesis.

How Vitamin D Levels of Children Changed During COVID-19 Pandemic: A Comparison of Pre-pandemic and Pandemic Periods

Objective:The synthesis of vitamin D is related to sun exposure, thus the restrictions during the Coronavirus disease-2019 (COVID-19) pandemic may have affected the levels of vitamin D in all age groups. The aim of this study was to evaluate vitamin D levels of healthy children and adolescents during the first year of the pandemic.Methods:The study group included healthy children and adolescents who were admitted for general check-ups and evaluated with 25(OH)D levels. Then, it was divided into two groups: Group 1 “pre-pandemic”, and Group 2 “pandemic”. Vitamin D levels were recorded from the hospital database and were compared according to age groups, gender, and the season, retrospectively.Results:The study group [mean age=90.29±59.45 median age=79 interquartile range (IQR): 102 months, male/female: 1409/1624] included 3033 children and adolescents (Group 1/Group 2 n=1864/1169). Although the mean 25(OH)D levels among preschool children did not differ between groups, the vitamin D levels of school-aged children and adolescents were significantly lower in the pandemic period than in the pre-pandemic period [Group 1 median=16.50 (IQR: 10.5) vs Group 2 median=15.9 (IQR: 11.3) in 6-12 age group (p=0.026); Group 1 median=13.30 (IQR: 10.2) vs Group 2 median=11.20 (IQR: 9.7) in 12-18 age group (p=0.003)]. Moreover, the 25(OH)D levels of adolescents showed seasonal variance with lower levels in winter, and unexpectedly, in summer.Conclusion:Pandemic-related restrictions have caused significant decreases in vitamin D levels of school-aged children and adolescents. We suggest that children and adolescents should be given vitamin D supplementation in order to maintain sufficient levels of vitamin D during the pandemic.

Regioselective hydrogenation of alkenes over atomically dispersed Pd sites on NHC-stabilized bimetallic nanoclusters

<h2>Summary</h2> A catalyst containing atomically dispersed Pd sites on N-heterocyclic carbene (NHC)-stabilized Au nanoclusters, with the precise formula of PdAu₉(NHC^Bn)₇X₂ (NHC^Bn is dibenzylbenzimidazolin-2-ylidene, X is Br or Cl), has been developed for the regioselective hydrogenation of alkenes. Each Pd site is encircled by an Au₉ ring protected by seven NHC and two halide ligands. Such an encirclement arrangement and open stereochemical framework endow the single Pd atom with the power to activate molecular hydrogen and catalyze the hydrogenation of alkenes efficiently. Interestingly, it otherwise exhibits much lower activity toward the crowded alkenes, owing to the inherent and highly stringent steric requirement of NHC ligands, as also visualized by the theory. As such, these clusters are demonstrated to be a highly efficient (653 h⁻¹ of turnover frequency) and highly selective (97%) catalyst in the regioselective hydrogenation of linalool, an important synthetic perfume and a key intermediate in the synthesis of vitamin A.

High sodium reduced the expression of PTH1R and Klotho by inhibiting 1,25(OH)2D3 synthesis in cultured proximal tubule epithelial cells.

BackgroundThe proximal tubule is the sensing site of sodium and phosphate and the main place for the synthesis and metabolism of 1,25(OH)2D3. We aimed to investigate the effects of high sodium on the synthesis and function of active vitamin D and local phosphate regulation in proximal tubular epithelial cells.MethodsHuman proximal tubule epithelial (HK-2) cells were treated with different concentrations of sodium/phosphate. The expression of 1α-OHase and 24-OHase was determined. Liquid chromatography/mass spectrometry (LC/MS) and enzyme-linked immunosorbent assay (ELISA) were used to detect the levels of 1,25(OH)2D3. RNA sequencing and bioinformatics analysis was used to probe into the possible pathways. Chromatin samples were immunoprecipitated with antibodies against parathyroid receptor 1 (PTH1R) and Klotho.ResultsWe found that high sodium decreased the expression of 1,25(OH)2D3 by reducing 1α-OHase and 24-OHase, reduced the expression of PTH1R and Klotho, and increased the intracellular calcium concentration. These effects were reversed by sodium phosphate transporter inhibitor, sodium hydrogen transporter inhibitor, and a chelator of the extracellular calcium, whereas enhanced by ouabain. Vitamin D receptor (VDR) agonists significantly increased the recruitment of VDR to the vitamin D response element (VDRE) of PTH1R and Klotho promoter, thus increasing the expression of PTH1R and Klotho.ConclusionsHigh sodium can decrease the synthesis of active vitamin D in the proximal tubules, affect the gene regulation of 1,25(OH)2D3/VDR, and significantly reduce the expression of PTH1R and Klotho. It revealed the influence of a high-sodium diet on mineral metabolism and the core role of vitamin D in kidney mineral metabolism.

Synthesis of Deuterium-Labeled Vitamin D Metabolites as Internal Standards for LC-MS Analysis.

Blood levels of the vitamin D3 (D3) metabolites 25-hydroxyvitamin D3 (25(OH)D3), 24R,25-dihydroxyvitamin D3, and 1α,25-dihydroxyvitamin D3 (1,25(OH)2D3) are recognized indicators for the diagnosis of bone metabolism-related diseases, D3 deficiency-related diseases, and hypercalcemia, and are generally measured by liquid-chromatography tandem mass spectrometry (LC-MS/MS) using an isotope dilution method. However, other D3 metabolites, such as 20-hydroxyvitamin D3 and lactone D3, also show interesting biological activities and stable isotope-labeled derivatives are required for LC-MS/MS analysis of their concentrations in serum. Here, we describe a versatile synthesis of deuterium-labeled D3 metabolites using A-ring synthons containing three deuterium atoms. Deuterium-labeled 25(OH)D3 (2), 25(OH)D3-23,26-lactone (6), and 1,25(OH)2D3-23,26-lactone (7) were synthesized, and successfully applied as internal standards for the measurement of these compounds in pooled human serum. This is the first quantification of 1,25(OH)2D3-23,26-lactone (7) in human serum.

Revolution of vitamin E production by starting from microbial fermented farnesene to isophytol

Vitamin E is one of the most widely used vitamins. In the classical commercial synthesis of vitamin E (α-tocopherol), the chemical synthesis of isophytol is the key technical barrier. Here, we establish a new process for isophytol synthesis from microbial fermented farnesene. To achieve an efficient pathway for farnesene production, Saccharomyces cerevisiae was selected as the host strain. First, β-farnesene synthase genes from different sources were screened, and through protein engineering and system metabolic engineering, a high production of β-farnesene in S. cerevisiae was achieved (55.4 g/L). This farnesene can be chemically converted into isophytol in three steps with approximately 92% yield, which is economically equal to that from the best total chemical synthesis. Furthermore, we co-produced lycopene and farnesene to reduce the cost of farnesene. A factory based on this new process was successfully operated in Hubei Province, China, in 2017, with an annual output of 30,000 tons of vitamin E. This new process has completely changed the vitamin E market due to its low cost and safety.

Synthesis of Polyene Bioactive Natural Products: FR252921 and Vitamin A.

A formal synthesis of FR252921, a potent macrocyclic immunosuppressive agent, and a six-step synthesis of vitamin A have been demonstrated. The application of a ruthenium-catalyzed step-economic and environmentally benign strategy for the highly stereo- and chemoselective construction of valuable polyene motifs of FR252921 and vitamin A highlights the syntheses. The key features for the synthesis FR252921 include preparation of the triene moiety followed by two consecutive peptide couplings of the three fragments.

Design, Green Synthesis and Tailoring of Vitamin E TPGS Augmented Niosomal Nano-Carrier of Pyrazolopyrimidines as Potential Anti-Liver and Breast Cancer Agents with Accentuated Oral Bioavailability.

VEGF plays a crucial role in cancer development, angiogenesis and progression, principally liver and breast cancer. It is vital to uncover novel chemical candidates of VEGFR inhibitors to develop more potent anti-breast and anti-liver cancer agents than the currently available candidates, sorafenib and regorafenib, that face resistance obstacles and severe side effects. Herein, nine pyrazolopyrimidine derivatives were designed, synthesized as sorafenib and regorafenib analogues and screened for their in vitro cytotoxic and growth inhibition activities against four human cancer cell lines, namely breast cancer (Michigan Cancer Foundation-7 (MCF-7), hepatocellular carcinoma (HCC) type (HepG2), lung carcinoma (A-549) and human colorectal carcinoma-116 (HCT-116)). Among the tested compounds, compounds 1, 2a, 4b and 7 showed the uppermost cytotoxic activities against all aforementioned cell lines with IC50 estimates varying from 6 to 50 µM, among which compound 7 showed the best inhibitory activity on all tested compounds. Stunningly, compound 7 showed the best significant inhibition of the VEGFR-2 protein expression level (72.3%) as compared to the control and even higher than that produced with sorafenib and regorafenib (70.4% and 55.6%, respectively). Modeling studies provided evidence for the possible interactions of the synthesized compounds with the key residues of the ATP binding sites on the hinge region and the “DFG out” motif of VEGFR-2 kinase. Collectively, our present study suggests that pyrazolopyrimidine derivatives are a novel class of anti-cancer drug candidates to inhibit VEGF-VEGFR function. Aspiring to promote constrained aqueous solubility, hence poor oral bioavailability of the developed lead molecule, 7 and 2a-charged D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) surface-coated niosomes were successfully constructed, adopting a thin film hydration technique striving to overcome these pitfalls. A 23 full factorial design was involved in order to investigate the influence of formulation variables: type of surfactant, either Span 60 or Span 40; surfactant:cholesterol ratio (8:2 or 5:5) along with the amount of TPGS (25 mg or 50 mg) on the characteristics of the nanosystem. F2 and S2 were picked as the optimum formula for compounds 2a and 7 with desirability values of 0.907 and 0.903, respectively. In addition, a distinguished improvement was observed in the compound’s oral bioavailability and cytotoxic activity after being included in the nano-TPGS-coated niosomal system relative to the unformulated compound. The nano-TPGS-coated niosomal system increased the hepatocellular inhibitory activity four times fold of compound 7a (1.6 µM) and two-fold of 2a (3 µM) relative to the unformulated compounds (6 µM and 6.2 µM, respectively).