scholarly journals In vivo and in silico investigations of the toxicological and analgesic properties of unprocessed Aloe vera gel in experimental rat models

2018 ◽  
Vol 70 (4) ◽  
pp. 727-735 ◽  
Author(s):  
Subhashis Paul ◽  
Arnab Chakraborty ◽  
Debabrata Modak ◽  
Arnab Sen ◽  
Soumen Bhattacharjee

Aloe vera is a commonly used plant in both food and medicine industry. The potential toxicological side-effects of prolonged intake of Aloe extract have not been evaluated in detail. This work presents an in-depth toxicological study of the crude unprocessed A. vera gel in experimental rats. Acute and sub-chronic toxicity was evaluated in a 1 to 28-day long feeding schedule of the aqueous homogenized gel material. Hemoglobin, total protein, high density lipoprotein (HDL), low density lipoprotein (LDL), cholesterol, triglyceride, serum creatinine, serum alanine transaminase (SGPT), aspartate transaminase (SGOT) and alkaline phosphatase were examined and kidney and liver histology was performed. In the acute toxicity test, the behavioral aspects were also considered. A molecular docking assay was performed to investigate the binding affinities of pure A. vera compounds with liver and kidney toxicological marker enzymes, in order to assess the probable mode of action of selected Aloe constituents. Solubility factors for the active constituents were also studied to determine their possible miscibility with body fluids. The results from in vivo tests provided no major toxicological indications. Crude Aloe gel consumption up to 4 g/kg body weight (b.w.) showed no toxicological side effects. From the structural standpoint, Aloe-based bioactive molecules, such as Aloe-emodin, acetophenone, ?-sitosterol, cholestenol and squalene showed promising binding affinity to qualify as alternative and complementary medicines. The synergistic roles of all A. vera constituents remain to be validated in human disease models.

Author(s):  
Khadijah S. Balamash ◽  
Mona S. Al-ddyni

Background: Atorvastatin (ATV), a lipid lowering agent, has low solubility and poor dissolution affects its oral bioavailability. Nanoemulsion (NE) has been developed to improve the delivery of therapeutic agents. This study was aimed to assess the ability of the NE in enhancing ATV bioavailability and minimizing its side effects in hyperlipidemic rats.Methods: Thirty-five rats divided into seven groups were utilized in this study. Hyperlipidemia was induced by feeding rats high fat diet (HFD) for 3 months. The antihyperlipidemic activity of 10 and 20 mg/kg of ATV loaded in two different delivery systems; nanoemulsion (10% and 20% ATV-LNE) or in water (10% and 20% ATV-sol), were investigated. At the end of the experiment, body weight, serum and plasma biochemical parameters (lipid profile, glucose, insulin, liver and kidney functions, oxidative stress markers were assessed. Liver and kidney were histopathologically examined. The physical characteristics of NE were determined by the Zetasizer (the z-average diameter and zeta potential).Results: 20% ATV-LNE had the smallest nanoparticles (38.12±6.71nm) whereas it had the largest zeta negative potential of -26.8±4.16mV. The serum biochemical results and the histopathological examination revealed that treatment with 20% ATV-LNE improved the lipid profile by significantly increasing HDL and decreasing cholesterol and low-density lipoprotein. Both 10 and 20% ATV-LNE reduced serum glucose level compared to other used formulas.Conclusions: NE formulas have the potential to improve the bioavailability and efficacy of ATV and reduce its side effects.


2016 ◽  
Vol 13 (3) ◽  
pp. 471-480 ◽  
Author(s):  
Lonette Wallis ◽  
Maides Malan ◽  
Chrisna Gouws ◽  
Dewald Steyn ◽  
Suria Ellis ◽  
...  

Circulation ◽  
1996 ◽  
Vol 94 (7) ◽  
pp. 1698-1704 ◽  
Author(s):  
Klaus Juul ◽  
Lars B. Nielsen ◽  
Klaus Munkholm ◽  
Steen Stender ◽  
Børge G. Nordestgaard

1986 ◽  
Vol 234 (1) ◽  
pp. 245-248 ◽  
Author(s):  
W Jessup ◽  
G Jurgens ◽  
J Lang ◽  
H Esterbauer ◽  
R T Dean

The incorporation of the lipid peroxidation product 4-hydroxynonenal into low-density lipoprotein (LDL) increases the negative charge of the particle, and decreases its affinity for the fibroblast LDL receptor. It is suggested that this modification may occur in vivo, and might promote atherogenesis.


1994 ◽  
Vol 35 (4) ◽  
pp. 669-677
Author(s):  
H.N. Hodis ◽  
D.M. Kramsch ◽  
P. Avogaro ◽  
G. Bittolo-Bon ◽  
G. Cazzolato ◽  
...  

Metabolites ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 223
Author(s):  
Roberta D’Assante ◽  
Mariarosaria De Luca ◽  
Sergio Ferraro ◽  
Andrea Ferraro ◽  
Antonio Ruvolo ◽  
...  

Hypercholesterolemia represents a serious public health problem as it significantly increases the risk of developing cardiovascular diseases. Its treatment with statin is limited by costs, side effects, and drugs interactions. Nutraceuticals appear to have an important metabolic effect on cholesterol reduction as well as on body weight and glycemia. The aim of this study was to evaluate the effect of a nutraceutical combination (Melasterol) in eighty-seven patients with acquired hypercholesterolemia. Clinically relevant parameters were collected at baseline and after three and six months of Melasterol treatment, one tablet per day. The primary endpoint was the change in cholesterol and triglyceride levels. Six months of treatment resulted in a 19.2% decrease in total cholesterol, accompanied by a 19.8% decrease in low-density lipoprotein (LDL) and a 23% reduction in triglycerides (p < 0.001) but not in high-density lipoprotein (HDL) levels (p > 0.05). These results were paralleled by a significative blood glucose (108.3 ± 21.3 vs. 98.4 ± 18.6 mg/dL p < 0.001) and body mass index (BMI) reduction (27.8 ± 4.4 vs. 27.0 ± 4.2 mg/dL, p < 0.001). A subgroup of 12 patients performed flow-mediated dilation, with values increasing by 1.8% (p < 0.05). No significant side effects were reported. Besides its cholesterol-lowering effect, Melasterol was associated with a significant improvement in other relevant metabolic parameters such as BMI and glycemia.


2021 ◽  
Vol 7 (9) ◽  
pp. eabf4398
Author(s):  
M. Kim ◽  
M. Jeong ◽  
S. Hur ◽  
Y. Cho ◽  
J. Park ◽  
...  

Ionizable lipid nanoparticles (LNPs) have been widely used for in vivo delivery of RNA therapeutics into the liver. However, a main challenge remains to develop LNP formulations for selective delivery of RNA into certain types of liver cells, such as hepatocytes and liver sinusoidal endothelial cells (LSECs). Here, we report the engineered LNPs for the targeted delivery of RNA into hepatocytes and LSECs. The effects of particle size and polyethylene glycol–lipid content in the LNPs were evaluated for the hepatocyte-specific delivery of mRNA by ApoE-mediated cellular uptake through low-density lipoprotein receptors. Targeted delivery of RNA to LSECs was further investigated using active ligands. Incorporation of mannose allowed the selective delivery of RNA to LSECs, while minimizing the unwanted cellular uptake by hepatocytes. These results demonstrate that engineered LNPs have great potential for the cell type–specific delivery of RNA into the liver and other tissues.


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