permeability

Digitonin is a natural product of the glycoside family and is a detergent. Digitonin has antitumor activity, binds to cholesterol molecules to increase the permeability of cell membranes, and is active in the cleavage of cell membranes in a wide range of cells.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Vancomycin is a glycopeptide antibiotic that exerts its antimicrobial activity by altering the permeability of cell membranes and selectively inhibiting ribonucleic acid synthesis. Vancomycin can be used for the treatment of serious infections for which all antibiotics have failed.

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

Dimethyl fumarate (DMF) is an Nrf2 activator with oral activity and blood-brain barrier permeability. Dimethyl fumarate has antimicrobial, anti-inflammatory, and immunomodulatory activities and has been used in the study of multiple sclerosis.

Diclofop-methyl is a common post-growth herbicide commonly used in agriculture. It enhances proton permeability of isolated oat root vesicle membranes.

Aloe-emodin-glucoside is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.

Macrocarpal C, isolated from the fresh leaves of Eucalyptus globulus Labill. (Lan An) and identified as its major antifungal component by bioassay-guided purification, the antifungal action of macrocarpal C was associated with increases of membrane permea

3-Hydroxybakuchiol exerts cytotoxic and anti-proliferative effects on the TA3 Ha mouse mammary adenocarcinoma cell line and induces a decrease in the mitochondrial transmembrane potential, the activation of caspase-3, the opening of the mitochondrial perm

Dodecanoylcarnitine ((-)-Lauroylcarnitine) has been associated with disturbances in fatty acid oxidation, and the use of Dodecanoylcarnitine resulted in an increase in the permeability of salmon calcitonin.

Agaricic acid is an adenine nucleotide translocase antagonist.It is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid (Agaricinic Acid) induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism.

Cognac oil, predominantly derived from wine lees, exhibits distinctive fatty acid compositions, characterized by high proportions of Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), and Oleic acid (8.3%) among other fatty acids. Notably, the application of Cognac oil enhances the permeability of Rhodamine 6G (R6G) across various membranes, resulting in a generalized increase in permeation.

2-Aminoimidazole is a potent antimicrobial agent that effectively targets drug-resistant Mycobacterium tuberculosis by disrupting the proton motive force and blocking the electron transport chain, potentiates the action of beta-lactam antibiotics against Mycobacterium tuberculosis by decreasing the secretion of beta-lactamases and increasing the permeability of cell membranes, activates drug-resistant bacteria and improves therapeutic efficacy.

Coronarin D methyl ether has inhibitory effects on the increase in vascular permeability, nitric oxide production, and inducible nitric oxide synthase induction.

POPE(1-Palmitoyl-2-oleoyl-sn-glycero-3-PE) is a compound found in Escherichia coli, part of the cell membrane, and can be used to study changes in cell membrane permeability.

Echinatin exerts a protective effect against ischemia reperfusion (I R)-induced myocardial injury on hearts, this effect may be attributed to the antioxidant and anti-inflammatory activities of this compound. Echinatin can inhibit DNP-ATPase activity whil

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.

Roemerine ((-)-Roemerine) is a porphyrin alkaloid from Senegalese lychee with antifungal and anticancer activity that prevents berberine efflux through inhibition of Bmr. Roemerine increases cell membrane permeability in a concentration-dependent manner and has been used in studies of fungal infections and prostate cancer.

Bactenecin TFA (Bactenecin, bovine TFA), a potent 12-aa looped antimicrobial peptide derived from bovine neutrophils, effectively inhibits bacterial and yeast growth, eradicates Trichophyton rubrum fungus, enhances membrane permeability, and suppresses B. pseudomallei growth and biofilm formation [1] [2] [3].

Cnidilin (Knidilin) is found in association with Angelica dahurica roots, has high BBB permeability and has pharmacokinetic potential in the treatment of CNS disorders.

Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.

1. Yunaconitine (Guayewuanine B) has anti-inflammatory and analgesic actions. 2. Yunaconitine was shown to have anti-thermic effect in pyrexial rats when administered orally at a dose of 5 μg kg. 3. Yunaconitine shows positive effect in the granuloma inhibition test when it was subcutaneously injected, 1 μg kg for 6 d, or added directly to the cotton-pellet. 4. Yunaconitine inhibited the increased vascular permeability caused byacetic acid and histamine, the leucocyte migratory response induced by injection of 1 % carrageenin .1 ml in rat's thoracic cavity.

Eledoisin trifluoroacetate (69-25-0 free base) is a peptide extracted from the posterior salivary glands of certain small octopi (Eledone spp., Mollusca), or obtained by synthesis. Its actions resemble those of SUBSTANCE P; it is a potent vasodilator and increases capillary permeability.

Nystatin A1, a polyene macrolide (antibiotic), is isolated from the Streptomyces noursei bacterium. It functions by binding with ergosterol on fungal cell membranes, enhancing membrane permeability, and consequently causing leakage of cellular contents, which inhibits fungal growth and reproduction.