α-Cyclodextrin (α-CD) is a saccharide comprised of six glucose subunits linked by α-1,4 bonds, which results in a cone-shaped molecule.1It contains a hydrophobic interior and hydrophilic exterior, which allow it to form inclusion complexes with wide variety of molecules, conferring enhanced solubility and stabilization to the molecules. α-CD has commonly been used in the separation and purification of chemicals on an industrial scale.1,2Formulations containing α-CD have been used in the pharmaceutical industry to improve the physical and chemical properties of compounds, the food industry as flavor carriers and stabilizers in processed and ultra-processed foods and certain beverages, as well as in other industrial applications. 1.Li, S., and Purdy, W.C.Cyclodextrins and their applications in analytical chemistryChem. Rev.92(6)1457-1470(1992) 2.Astray, G., Gonazalez-Barreiro, C., Mejuto, J.C., et al.A review on the use of cyclodextrins in foodsFood Hydrocolloids23(7)1631-1640(2009)
Hydroxypropyl-beta-cyclodextrin, also known as Hydroxypropyl-beta-cyclodextrin; THPB; HP-beta-CD; HPbCD; HP-beta-CyD; VTS-270; HPbetaCD; HPbetaCyD, is a drug candidate potentially for the treatment of Niemann-Pick type C diseases. In April 2009, hydroxypr
Limaprost alfadex is an oral medicine for the circulatory system (for confinement-related thromboangiitis ulcer, anaphrodisia, sharp pain and ischemia characteristics symptom, the improvement of subjective symptom and walking ability with postnatal lumbar
Mitoquinone-cyclodextrin is a 1:1 molar ratio complex of Mitoquinone mesylate with cyclodextrin. Mitoquinone mesylate is a mitochondria-targeted antioxidant designed to accumulate within mitochondria in vivo in order to protect against oxidative damage. M
Cho-Arg is a steroid-based cationic lipid that contains a cholesterol skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratios greater than or equal to 4. Cho-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence or absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It is cytotoxic to H1299 cells (IC50 = 88.5 μg/ml).
Dios-Arg is a steroid-based cationic lipid that contains a diosgenin skeleton coupled to an L-arginine head group. It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratio greater than or equal to 4. Dios-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence and absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It has been used, coupled to 1,2-dioleoyl-sn-glycero-3-PE , to bind siRNA and plasmid DNA to form cationic lipid nanoparticles for intracellular transport. Dios-Arg is cytotoxic to H1299 and HeLa cells (IC50s = 83.5 and 74.1 μg/ml, respectively).
2H-Cho-Arg is a steroid-based cationic lipid that contains a 2H-cholesterol skeleton coupled to an L-arginine head group and can be used to facilitate gene transfection. It forms a complex with plasmid DNA (pDNA) and decreases pDNA migration in an electrophoretic mobility shift assay at +/- charge ratios of 4 or higher. 2H-Cho-Arg facilitates transfection of a luciferase gene into H1299 cells, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein , but not by inhibitors of clathrin- or micropinocytosis-mediated endocytosis. It induces cytotoxicity in H1299 cells (IC50 = 92.7 μg/ml).
6-O-Sulfo-β-cyclodextrin is a sulfated cyclodextrin.1It has been used for the chiral separation of nadolol racemates by capillary electrophoresis. 1.Wang, F., Dowling, T., Bicker, G., et al.Electrophoretic chiral separation of pharmaceutical compounds with multiple stereogenic centers in charged cyclodextrin mediaJ. Sep. Sci.24(5)378-384(2001)
Sugammadex is an agent for reversal of neuromuscular blockade by the agent rocuronium in general anaesthesia. It is the first selective relaxant binding agent (SRBA). Sugammadex is a modified γ-cyclodextrin, with a lipophilic core and a hydrophilic periph
PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the lead compound of a new class of potential agents that inhibit Akt survival signaling.
Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50 IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 + - 0.08 micromol l after 24 h) than As(2)O(3) (IC50 = 1.60 + - 0.23 micromol l after 24 h) or melarsoprol (IC50 = 1.44 + - 0.08 micromol l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.