Aside from awesome logistical problems, “mandatory for everyone” means the planners have no wiggle room. It becomes difficult to make adjustments in the face of public opposition

PMID: 

Antibiotics (Basel). 2020 Apr 20 ;9(4). Epub 2020 Apr 20. PMID: 32325952

Abstract Title: 

In Vitro Antimicrobial Activity of Frankincense Oils fromGrown in Different Locations of the Dhofar Region (Oman).

Abstract: 

Frankincense essential oils fromhave been commonly used to treat microbial infections from as early as the 11th century. The main feature of the plant is its gum resin, from which it is possible to obtain essential oils. In the present study, we focused on the comparative study of the oils extracted from the resins of three differentcultivars (Najdi, Sahli and Houjri). From each of frankincense resin three successive essential oil samples (Grade 1, Grade 2, Grade 3) were obtained. Houjri gum resin gave the lowest percentage (5%) of total essential oil content but showed the maximum number of volatile components in all three grades. Najdi Grade 2 essential oil showed a minimum inhibitory concentration (MIC) of 52 mg/mL toward relevant pathogensand, and samples from Grade 2 of Sahily and Houjiri were particularly active against a dermatological strain, displaying MIC values of 0.264 and 0.66 mg/mL, respectively. Data obtained from in vitro studies showed that all essential oils had a significant antifungal effect againstand, showing MIC values ranging from 54.56 to 0.246 mg/mL. This work aims to increase the number of substances available in the fight against pathogens and to combat the phenomenon of antibiotic resistance, encouraging the use of alternative resources, especially in non-clinical settings (farms, food processing, etc.).

read more

PMID: 

World J Gastroenterol. 2020 Apr 14 ;26(14):1601-1612. PMID: 32327909

Abstract Title: 

Silymarin, boswellic acid and curcumin enriched dietetic formulation reduces the growth of inherited intestinal polyps in an animal model.

Abstract: 

BACKGROUND: Some substances of plant origin have been reported to exert an effect in reducing intestinal neoplasm development, especially in animal models. Adenomatous polyposis coli multiple intestinal neoplasia – Apcis the most studied murine model of genetic intestinal carcinogenesis.AIM: To assess whether an enriched nutritional formulation (silymarin, boswellic acid and curcumin) with provenandanti-carcinogenetic properties may prevent inherited intestinal cancer in animal model.METHODS: Forty adenomatous polyposis coli multiple intestinal neoplasia – Apcmice were used for the study of cancer prevention. They were divided into two groups: 20 assumed standard and 20 enriched diet. At the 110d animals were sacrificed. In each group, four subgroups received intraperitoneal bromodeoxyuridine injection at different times (24, 48, 72 and 96 h before the sacrifice) in order to assess epithelial turnover. Moreover, we evaluated the following parameters: Intestinal polypoid lesion number and size on autoptic tissue, dysplasia and neoplasia areas by histological examination of the whole small intestine, inflammation by histology and cytokine mRNA expression by real-time polymerase chain reaction, bromodeoxyuridine and TUNEL immuno-fluorescence for epithelial turnover and apoptosis, respectively. Additionally, we performed western blotting analysis for the expression of estrogen alpha and beta receptors, cyclin D1 and cleaved caspase 3 in normal and polypoid tissues.RESULTS: Compared to standard, enriched diet reduced the total number (203416) and the mean± SD/animal (12.6 ± 5.026.0± 8.8;

read more

PMID: 

Biomolecules. 2020 May 12 ;10(5). Epub 2020 May 12. PMID: 32408614

Abstract Title: 

Triterpenic Acids as Non-Competitiveα-Glucosidase Inhibitors fromwith Structure-Activity Relationship: In Vitro and In Silico Studies.

Abstract: 

Fourteen triterpene acids, viz., three tirucallane-type (-), eight ursane-type (-), two oleanane-type (,) and one lupane type (), along with boswellic aldehyde (),α-amyrine (), epi-amyrine (), straight chain acid (), sesquiterpene () and two cembrane-type diterpenes (,) were isolated, first time, from the methanol extract ofresin. Compound () was isolated for first time as a natural product, while the remaining compounds (‒) were reported for first time fromThe structures of all compounds were confirmed by advanced spectroscopic techniques including mass spectrometry and also by comparison with the reported literature. Eight compounds (-and) were further screened for in vitroα-glucosidase inhibitory activity. Compounds-andshowed significant activity againstα-glucosidase with ICvalues ranging from 9.9-56.8μM. Compound(IC= 9.9± 0.48 μM) demonstrated higher inhibition followed by(IC= 14.9± 1.31 μM),(IC= 20.9± 0.05 μM) and(IC= 56.8± 1.30 μM), indicating that carboxylic acid play a key role in α-glucosidase inhibition. Kinetics studies on the active compounds-andwere carried out to investigate their mechanism (mode of inhibition and dissociation constants). All compounds were found to be non-competitive inhibitors withvalues in the range of 7.05± 0.17-51.15 ± 0.25 µM. Moreover, in silico docking was performed to search the allosteric hotspot for ligand binding which is targeted by our active compounds investigates the binding mode of active compounds and it was identified that compounds preferentially bind in the allosteric binding sites of α-glucosidase. The results obtained from docking study suggested that the carboxylic group is responsible for their biologic activities. Furthermore, the α-glucosidase inhibitory potential of the active compounds is reported here for the first time.

read more

PMID: 

Iran J Basic Med Sci. 2020 Mar ;23(3):277-286. PMID: 32440312

Abstract Title: 

Genusas a new candidate for neurodegenerative disorders.

Abstract: 

Neurodegenerative diseases, characterized by progressive loss of neurons, share common mechanisms such as apoptotic cell death, mitochondrial dysfunction, inflammation, and oxidative stress. Genusis a genus in the Burseraceae family. It comprises several species traditionally used for treatment of chronic inflammatory diseases, cerebral edema, chronic pain syndrome, gastrointestinal diseases, tumors, as well as enhancing intelligence. Many studies have been carried out to discover therapeutic approaches for neurodegenerative diseases such as Alzheimer's diseases, Parkinson's disease, Huntington's disease, multiple sclerosis and amyotrophic lateral sclerosis, stroke, and concomitant cognitive deficits. However, no curative treatment has been developed. This paper provides an overview of evidence about the potential of the Boswellia species and their main constituents, boswellic acids, as modulators of several mechanisms involved in the pathology of the neurodegenerative diseases., animal, and clinical studies have confirmed that Boswellia species contain bioactive components that may enhance cognitive activity and protect against neurodegeneration. They exert the beneficial effects via targeting multiple pathological causes by antioxidative, anti-inflammatory, antiamyloidogenic, and anti-apoptotic properties. The Boswellia species, having neuroprotective potential, makes them a promising candidate to cure or prevent the neurodegenerative disorders.

read more

PMID: 

J Nat Prod. 2020 May 22 ;83(5):1461-1472. Epub 2020 Apr 29. PMID: 32347726

Abstract Title: 

Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.

Abstract: 

The overexpression of the ATP-binding cassette (ABC) transporter ABCG2 has been linked to clinical multidrug resistance in solid tumors and blood cancers, which remains a significant obstacle to successful cancer chemotherapy. For years, the potential modulatory effect of bioactive compounds derived from natural sources on ABCG2-mediated multidrug resistance has been investigated, as they are inherently well tolerated and offer a broad range of chemical scaffolds. Licochalcone A (LCA), a natural chalcone isolated from the root of, is known to possess a broad spectrum of biological and pharmacological activities, including pro-apoptotic and antiproliferative effects in various cancer cell lines. In this study, the chemosensitization effect of LCA was examined in ABCG2-overexpressing multidrug-resistant cancer cells. Experimental data demonstrated that LCA inhibits the drug transport function of ABCG2 and reverses ABCG2-mediated multidrug resistance in human multidrug-resistant cancer cell lines in a concentration-dependent manner. Results of LCA-stimulated ABCG2 ATPase activity and the in silico docking analysis of LCA to the inward-open conformation of human ABCG2 suggest that LCA binds ABCG2 in the transmembrane substrate-binding pocket. This study provides evidence that LCA should be further evaluated as a modulator of ABCG2 in drug combination therapy trials against ABCG2-expressing drug-resistant tumors.

read more

PMID: 

Pharmazie. 2019 12 1 ;74(12):751-754. PMID: 31907117

Abstract Title: 

Vasorelaxation effect of 18β-glycyrrhetinic acid on the thoracic aorta of rats: proposed mechanism.

Abstract: 

18β-Glycyrrhetinic acid (18β-GA) is an effective component extracted from the traditional Chinese medicine(Leguminosae) and has various biological activities. This study was performed to investigate the vasodilatory effects of 18β-GA on isolated rat thoracic aortic rings and explore the underlying mechanisms. The rings were obtained from normal Sprague-Dawley rats and then precontracted with norepinephrine (NE) (1 μM) or KCl (60 mM). 18β-GA (1.883-11.297mg/L) was added successively by cumulative dosing to observe and record the changes in the tension of the vascular ring. The effects of NG-nitro-l-arginine methylester (L-NAME), indomethacin (INDO), barium chloride (BaCl₂), 4-aminopyridine(4-AP), tetraethylammonium (TEA), and glibenclamide on the vascular diastolic function of 18β-GA were determined. 18β-GA substantially exhibited a dose-dependent vasorelaxant effect on the NE-induced and KCl-induced contractions of the rings. The integrity of the vascular endothelium had no influence on the 18β-GA-induced vasorelaxation effect in the rings. L-NAME and IDON showed no significant differences in their effects on this vasorelaxation process in the rings precontracted with NE. This result suggests that the vasorelaxation mechanism of 18β-GA may be independent of the vascular endotheliumBaCl₂ and 4-AP antagonized the vasorelaxation effect of 18β-GA, but TEA and glibenclamide showed no remarkable effect on the vasodilation of 18β-GA. Findings suggest that 18β-GA induces vasorelaxation in thoracic aortic rings via the receptor-operated Cachannels and voltage-operated Cachannels and the opening of inward rectifier potassium channels and voltage-operated potassium.

read more

PMID: 

Biomed Pharmacother. 2020 May ;125:109702. Epub 2020 Feb 25. PMID: 32106383

Abstract Title: 

18α-Glycyrrhetinic acid (GA) ameliorates fructose-induced nephropathy in mice by suppressing oxidative stress, dyslipidemia and inflammation.

Abstract: 

Excessive fructose (FRU) intake can result in insulin resistance and metabolic disorder, which are related to renal injury.18α-Glycyrrhetinic acid (GA) is a bioactive component mainly extracted from Glycyrrhiza radix, and has anti-oxidant and anti-inflammatory activities. However, its effects on FRU-induced renal injury still remain unclear. In this study, we found that 18α-GA treatments could significantly ameliorate the cell viability in FRU-treated tubule epithelial cells, accompanied with improved mitochondrial membrane potential. Furthermore, reactive oxygen species (ROS) accumulation in FRU-stimulated cells was markedly reduced by 18α-GA, which were associated with the activation of nuclear factor (erythroid-derived-2)-like 2 (Nrf-2) and the blockage of MAPKs signaling. Additionally, dyslipidemia detected in FRU-treated cells was greatly inhibited by 18α-GA. We also found that 18α-GA significantly ameliorated FRU-induced inflammation in cells through reducing the expression of pro-inflammatory cytokines and chemokine. The anti-inflammatory effects regulated by 18α-GA were mainly related to the repression of nuclear factor-κB(NF-κB) signaling. Furthermore, the protective effects of 18α-GA against ROS production, lipid accumulation and inflammation were verified in renal tissues from FRU-challenged mice, consequently improving metabolic disorder and kidney injury. Taken together, these findings demonstrated that 18α-GA exerted renal protective effects through reducing oxidative stress, lipid deposition and inflammatory response, and thus could be considered as a promising therapeuticstrategy for metabolic stress-induced kidney injury.

read more

PMID: 

Pharmacol Res. 2020 Apr 28 ;157:104840. Epub 2020 Apr 28. PMID: 32353589

Abstract Title: 

18β-Glycyrrhetinic acid acts through hepatocyte nuclear factor 4 alpha to modulate lipid and carbohydrate metabolism.

Abstract: 

Hepatocyte nuclear factor 4 alpha (HNF4α) regulates the expression of essential genes involved in very-low-density lipoprotein (VLDL) homeostasis and gluconeogenesis.　18β-glycyrrhetinic acid (GA) is an active ingredient of Glycyrrhiza uralensis an herbal medicine used for treating liver aliments. In this study, we established that GAfunctions as a partial antagonist of HNF4α through HNF4α-driven reporter luciferase assay and co-immunoprecipitation experiments with co-activator PGC1α. By virtual docking and site-directed mutagenesis analysis, we confirmed that serine 190 and arginine 235 of HNF4α are both essential for GA to exert its antagonistic action on HNF4α. Importantly, GA suppressed the expression of HNF4α target genes such as apolipoprotein B (ApoB), microsomal triglyceride transfer protein (MTP) and phospholipase AG12B (PLA2G12B) modulating hepatic VLDL secretion in mice fed on a high fat diet. In addition, GA also suppressed gluconeogenesis and ameliorated glucose intolerance via down-regulating the expression of HNF4α target genes glucose-6-phosphatase (G6pc) and phosphoenolpyruvate carboxykinase (Pepck). Furthermore, GA significantly lowered blood glucose and improved insulin resistance in db/db mice. In all, we established that GA acts as a partial HNF4α antagonist modulating lipid and carbohydrate metabolism.

read more

It seems evident that face masks help slow the spread of COVID-19, but does it really make sense? Is it supported by science? Are there any adverse consequences of wearing a mask?