The effect of solvent, substrate-to-solvent ratio and concentration of pectinase on the extraction of betacyanins from the pulp of red pitahaya (Hylocereus polyrhizus) was evaluated with respect to yield, betacyanin content (BC) and total sugar content. The application of betacyanins from red pitahaya in ice cream was then evaluated by comparison to a commercial colourant, E-162. Without the use of pectinase, the highest yields (9.11 ± 0.35%) of betacyanins were obtained using 95% ethanol at a substrate-to-solvent ratio of 1:1. With the use of pectinase at a concentration of 1.5%, the highest yield (17.11-17.45%) of betacyanins were obtained using water as a solvent at a substrate-to-solvent ratio of 1:1 and 1:2. Pectinase treatment (1.5-2.5%) using water as a solvent yielded betacyanins with the highest BC (126.47-130.83 g kg^-1) and lowest total sugar content (57.85-59.74 g kg^-1). The BC and total colour changes were similar in ice cream containing betacyanins from red pitahaya and E-162 throughout the 21-days of frozen storage at -18 °C. Betacyanins from red pitahaya or E-162 enhanced the antioxidant properties of ice cream. The sensory evaluation of ice cream containing betacyanins from red pitahaya showed a better colour acceptability than E-162.

01 Jul 2018·British Journal of PharmacologyQ2 · MEDICINE

Antinociceptive effects of novel histamine H₃ and H₄ receptor antagonists and their influence on morphine analgesia of neuropathic pain in the mouse

Q2 · MEDICINE

Article

Author: Latacz, Gniewomir ; Popiolek‐Barczyk, Katarzyna ; Stark, Holger ; Mika, Joanna ; Łażewska, Dorota ; Olejarz, Agnieszka ; Makuch, Wioletta ; Kieć‐Kononowicz, Katarzyna

Background and PurposeThe histaminergic system is a promising target for the development of new analgesics, as histamine H3 and H4 receptors are expressed in regions concerned with nociceptive transmission. Here we have determined the analgesic effects of new H3 and H4 receptor antagonists in naive and neuropathic mice.Experimental ApproachWe used chronic constriction injury (CCI) to the sciatic nerve in mice to model neuropathy. Effects of a new H3 receptor antagonist, E‐162(1‐(5‐(naphthalen‐1‐yloxy)pentyl)piperidine) and H4 receptor antagonist, TR‐7(4‐(4‐chlorophenyl)‐6‐(4‐methylpiperazin‐1‐yl)‐1,3,5‐triazin‐2‐amine) were assessed on mechanical (von Frey) and thermal (cold plate, tail flick) stimuli in mice with and without CCI (7 days after injury). Effects of these antagonists on morphine analgesia were also evaluated, along with the possible participation of H1 receptors in their effects. We analysed the compounds in binding and functional cAMP assays at the H3 and H4 receptors and determined metabolic stability.Key ResultsE‐162 and TR‐7 attenuated nociceptive responses and profound morphine analgesia in males with CCI. These antagonists showed analgesia in naive mice (tail flick test) and produced prolonged analgesia in neuropathic females. E‐162‐induced analgesia was reversed by pyrilamine, an H1 receptor antagonist. E‐162 bound potently to H3 receptors (Ki = 55 nM) and inhibited cAMP accumulation (IC50 = 165 nM). TR‐7 showed lower affinity for H4 receptors (Ki = 203 nM) and IC50 of 512 nM.Conclusions and ImplicationsWe describe a therapeutic use for new H3 (E‐162) and H4 receptor (TR‐7) antagonists in neuropathy. Targeting H3 and H4 receptors enhanced morphine analgesia, consistent with multimodal pain therapy.

01 Jul 2018·Food Research InternationalQ1 · AGRICULTURAL & FORESTRY SCIENCE

Microencapsulation of betanin in monodisperse W/O/W emulsions

Q1 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: Kobayashi, Isao ; Khalid, Nauman ; Pagano, Ana Paula Eskildsen ; Nakajima, Mitsutoshi ; Neves, Marcos Antonio ; Bastos, Erick Leite

Betanin is the main pigment of the food color beetroot red (E162). Due to the fair heat and light stability of E162, this pigment is mainly used in minimally processed packaged food products. Encapsulation increases the stability of betanin, but detailing on the effect of different sources of betanin on the properties and stability of multiple emulsions are scarce. Here we describe the encapsulation of E162, spray-dried beetroot juice and betanin in a monodisperse food-grade water-in-oil-in-water (W/O/W) emulsions by using microchannel emulsification. We compare the tinctorial strength of the encapsulated pigments and investigate the effect of temperature, storage period and pigment concentration on emulsion stability and color. Betanin increases the overall stability of the W/O/W emulsion, reduce the oil droplet size and improve size distribution when compared to the negative control without pigment and to emulsions containing betanin from other sources.

100 Deals associated with E-162(Clovis Oncology, Inc.)

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Preclinical	-	Clovis Oncology, Inc.	-
Neoplasms	Preclinical	-	Karus Therapeutics Ltd.	-

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