Comparative Analysis of Apigenin-3 Acetate versus Apigenin and Methyl-Prednisolone in Inhibiting Proliferation and Gene Expression of Th1 Cells in Multiple Sclerosis.

Article

Author: Rahmati, Mahshid ; Ghannadian, Seyed Mostafa ; Kasiri, Neda ; Ashtari, Fereshteh ; Ahmadi, Leila ; Hosseini, Reza ; Pourazar, Abbasali ; Eskandari, Nahid

OBJECTIVEIn spite of the advances in therapeutic modalities, morbidity, due to multiple sclerosis (MS), still remains high. Therefore, a large body of research is endeavouring to discover or develop novel therapies with improved efficacy for treating MS patients. In the present study, we examined the immunomodulatory effects of apigenin (Api) on peripheral blood mononuclear cells (PBMCs) isolated from MS patients. We also developed an acetylated form of Api (apigenin- 3-acetate) to improve In its blood-brain barrier (BBB) permeability. Additionally, we compared its anti-inflammatory properties to original Api and methyl-prednisolone-acetate (a standard therapy), as a potential option in treating MS patients.MATERIALS AND METHODSThe current study was an experimental-interventional research. The half maximal inhibitory concentration (IC₅₀) values for apigenin-3-acetate, apigenin, and methyl-prednisolone-acetate were determined in healthy volunteers' PBMCs (n=3). Gene expressions of T-box transcription factor (TBX21 or T-bet) and IFN-γ, as well as proliferation of T cells isolated from MS patients' PBMCs (n=5), were examined in co-cultures of apigenin-3-acetate, Api and methyl-prednisolone-acetate after 48 hours of treatment, using quantitative reverse transcription polymerase chain reaction (qRT-PCR).RESULTSOur findings showed that apigenin-3-acetate, apigenin, and methyl-prednisolone-acetate at concentrations of 80, 80, and 2.5 M could inhibit Th1 cell proliferation after 48 hours (P=0.001, P=0.036, and P=0.047, respectively); they also inhibited T-bet (P=0.015, P=0.019, and P=0.022) and interferon-γ (IFN-γ) gene expressions (P=0.0001).CONCLUSIONOur findings suggested that Api may have anti-inflammatory properties, possibly by inhibiting proliferation of IFN-producing Th1 cells. Moreover, comparative immunomodulatory effects were found for the acetylated version of apigenin-3-acetate versus Api and methyl-prednisolone-acetate.

01 Oct 2017·Archives of Toxicology

Phenyl valerate esterase activity of human butyrylcholinesterase

Article

Author: Vilanova, Eugenio ; Mangas, Iris ; Estévez, Jorge

Phenyl valerate is used for detecting and measuring neuropathy target esterase (NTE) and has been used for discriminating esterases as potential target in hen model of organophosphorus delayed neuropathy. In previous studies we observed that phenyl valerate esterase (PVase) activity of an enzymatic fraction in chicken brain might be due to a butyrylcholinesterase protein (BuChE), and it was suggested that this enzymatic fraction could be related to the potentiation/promotion phenomenon of the organophosphate-induced delayed neuropathy (OPIDN). In this work, PVase activity of purified human butyrylcholinesterase (hBuChE) is demonstrated and confirms the novel observation that a relationship of BuChE with PVase activities is also relevant for humans, as is, therefore the potential role in toxicity for humans. The K_M and catalytic constant (k_cat) were estimated as 0.52/0.72 µM and 45,900/49,200 min^-1 respectively. Furthermore, this work studies the inhibition by preincubation of PVase and cholinesterase activities of hBuChE with irreversible inhibitors (mipafox, iso-OMPA or PMSF), showing that these inhibitors interact similarly in both activities with similar second-order inhibition constants. Acethylthiocholine and phenyl valerate partly inhibit PVase and cholinesterase activities, respectively. All these observations suggest that both activities occur in the same active center. The interaction with a reversible inhibitor (ethopropazine) showed that the cholinesterase activity was more sensitive than the PVase activity, showing that the sensitivity for this reversible inhibitor is affected by the nature of the substrate. The present work definitively establishes the capacity of BuChE to hydrolyze the carboxylester phenyl valerate using a purified enzyme (hBuChE). Therefore, BuChE should be considered in the research of organophosphorus targets of toxicity related with PVase proteins.

01 Feb 2013·Australasian Journal of DermatologyQ4 · MEDICINE

Granuloma annulare‐like reaction to the bacillus Calmette‐Guerin vaccination

Q4 · MEDICINE

Article

Author: Hideya Takenaka ; Saburo Kishimoto ; Tomoko Nomiyama ; Norito Katoh

ABSTRACTWe report the case of a 6‐month‐old girl with a granuloma annulare (GA)‐like reaction to the bacillus Calmette‐Guerin (BCG) vaccination. The eruption developed at the vaccination site 1 month after vaccination and the lesion gradually disseminated over the body within 2 months. A biopsy specimen of the skin lesion showed degenerated collagen bundles surrounded by imperfect palisading histiocytes, lymphocytes and epithelioid cells in the dermis, which led to a diagnosis of GA‐like reaction as a secondary reaction to BCG inoculation. The eruption at the vaccination site and the scattered GA reaction resolved after 1 month of treatment with prednisolone valerate acetate ointment, leaving only pigmentation.

100 Deals associated with Prednisolone valerate acetate

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Indication	Country/Location	Organization	Date
Keratoderma, Palmoplantar	JP	Iwaki Seiyaku Co., Ltd.	17 Jan 1992
Neurodermatitis	JP	Iwaki Seiyaku Co., Ltd.	17 Jan 1992
Psoriasis	JP	Iwaki Seiyaku Co., Ltd.	17 Jan 1992
Eczema	JP	Kowa Co., Ltd.	15 Jun 1982
Insect Bites and Stings	JP	Kowa Co., Ltd.	15 Jun 1982
Prurigo	JP	Kowa Co., Ltd.	15 Jun 1982
Pustulosis of Palms and Soles	JP	Kowa Co., Ltd.	15 Jun 1982
Urticaria	JP	Kowa Co., Ltd.	15 Jun 1982

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