Five polypeptides with a potential umami taste were isolated and purified from Yanjin black bone chicken. However, the flavor characteristics and umami mechanism have not been clarified. The umami properties of these five peptides were investigated in this work using a range of analytical techniques, computer simulation, and sensory evaluation. HE-10 and TP-7 exhibited the strongest umami flavors. Furthermore, dose-response experiments showed that the umami peptides enhanced umami by generating peptide mineral chelates. Environmental scanning electron microscopy (ESEM) microstructural analyses supported this finding. The molecular docking results indicated that the five polypeptides bind to four critical amino acid residues, namely Glu217, Glu148, Asp216, and His145, of the T1R1/T1R3 receptor. The binding occurred through van der Waals, electrostatic interactions, hydrogen bonding, and hydrophobic interactions. The main surface forces implicated include aromatic interactions, hydrogen bonding, hydrophilicity, and solvent accessibility.

01 Aug 2017·Toxicology and Applied PharmacologyQ3 · MEDICINE

Anti-liver cancer activity in vitro and in vivo induced by 2-pyridyl 2,3-thiazole derivatives

Q3 · MEDICINE

Article

Author: Dos Santos Silva, Thiago David ; Bezerra, Daniel Pereira ; Leite, Ana Cristina Lima ; Soares, Milena Botelho Pereira ; Bomfim, Larissa Mendes ; Sales, Caroline Brandi Schlaepfer ; da Cruz Rodrigues, Ana Carolina Borges ; de Oliveira Cardoso, Marcos Veríssimo ; Militão, Gardenia Carmen Gadelha ; Rocha, Clarissa Araújo Gurgel ; Dias, Rosane Borges

A total of 24 hybrid compounds containing pyridyl and 1,3-thiazole moieties were screened against HL-60 (leukemia), MCF-7 (breast adenocarcinoma), HepG2 (hepatocellular carcinoma), NCI-H292 (lung carcinoma) human tumor cell lines and non-tumor cells (PBMC, human peripheral blood mononuclear cells). Most of them were highly potent in at least one cell line tested (IC₅₀≤3μM), being HL-60 the most sensitive and HepG2 the most resistant cell line. Among them, TAP-07 and TP-07 presented cytotoxic activity in all tumor cell lines, including HepG2 (IC₅₀ 2.2 and 5.6μM, respectively) without antiproliferative effects to normal cells (PBMC) (IC₅₀>30μM), making TAP-07 and TP-07, the compounds with the most favorable selectivity index. TAP-07 and TP-07 induced apoptosis in HepG2 cells and presented in vivo antitumor activity in hepatocellular xenograft cancer model in C.B-17 severe combined immunodeficient mice. Systemic toxicological verified by biochemical and histopathological techniques reveled no major signs of toxicity after treatment with TAP-07 and TP-07. Together the results indicated the anti-liver cancer activity of 2-pyridyl 2,3-thiazole derivatives.

Pharmacological reports : PR

Influence of long-term treatment with tuftsin analogue TP-7 on the anxiety-phobic states and body weight.

Article

Author: Cygan, Beata ; Wolański, Lukasz ; Kozlovsky, Igor ; Czabak-Garbacz, Róza

TP-7 is a synthetic analogue of tuftsin. It has a structure of tuftsin, to which three natural L-amino-acids Pro-Gly-Pro are attached. This heptapeptide improves learning and memorization and causes antidepressant and anxiolytic effect. It is possible to use TP-7 in the future to optimize cognitive functions and as a potential new anxioselective, fast-acting and easy-dosed drug. Therefore, it was purposeful to study such properties of the heptapeptide as its influence on anxiety-fear and body weight under a long-term treatment regimen. The experiment was performed on 24 preselected Wistar rats with the use of Rodina's method. There were three experimental groups of animals with high initial emotional reactivity: passive control group (P), active control group (A, receiving distilled water) and group treated with TP-7 at the dose of 0.3 mg/kg (T). The rats of A and T groups received intraperitoneal injections every day. The experiments were conducted 15 min after the administration of the drug, one and two days after initial testing day, then 1, 2, 3 and 4 weeks after that. The heptapeptide reduced the anxiety-phobic states significantly starting from the second day of drug application. The observed effects persisted throughout four weeks of the experiment, which confirmed effective long-term anxiolytic properties of the heptapeptide. TP-7 did not cause any changes in the body mass by itself.

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Indication	Highest Phase	Country/Location	Organization	Date
Proctocolitis	Discovery	CH	Tillotts Pharma AG	-

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