4-Hydroxy-3-methoxyphenyl O-beta-D-6-O-syringate-glucopyranoside

Role of ((E)-(E)-4-(4-hydroxy-3-methoxyphenyl)-2-oxobut-3-en-1-yl 3-(4-hydroxy-3-methoxyphenyl) acrylate in preservation of spatial cognitive functions of rats with chronic epilepsy.[Pubmed:26379828]

Int J Clin Exp Med. 2015 Jul 15;8(7):10380-7. eCollection 2015.

The present study demonstrates the effect of ((E)-(E)-4-(4-hydroxy-3-methoxyphenyl)-2-oxobut-3-en-1-yl 3-(4-hydroxy-3-methoxyphenyl) acrylate (CA) on spatial cognitive functions of rats with lobal cerebrovascular hypoperfusion. The bilateral common carotid arteries occlusion (2VO) surgery was performed to prepare the cerebrovascular hypoperfusion rat model. The effect of CA on spatial cognitive function was analysed using Morris water maze (MWM) test prior to and after 2VO operation. Sixty rats were randomly assigned into two groups of 30 each; long-term memory (LTM) and short-term memory (STM) groups. Both the groups were further divided into 3 subgroups: control, untreated and CA treated groups. The animals received 50 mug/kg of CA for 10 weeks of 2VO operation following which all the subgroups were tested with MWM. Both the escape latency time and total distance travelled were significantly lower for control and CA treated groups compared to untreated group revealed by working memory test. The maze test performance for control and CA treated groups was found to be improved markedly. Similarly, the results from probe memory test performance revealed significant improvement for CA treated groups compared to untreated group. Therefore, CA exhibits significant effect on the spatial cognitive preservation in rats with chronic epilepsy.

7-(4-Hydroxy-3-methoxyphenyl)-1-phenyl-4E-hepten-3-one alleviates Abeta1-42 induced cytotoxicity through PI3K-mTOR pathways.[Pubmed:28131834]

Biochem Biophys Res Commun. 2017 Mar 4;484(2):365-371.

Alzheimer's disease (AD) is the most common neurodegenerative disease in the elderly. Increasing evidence has shown that beta-amyloid protein (Abeta) production is the key pathological cause of AD. 7-(4-Hydroxy-3-methoxyphenyl)-1-phenyl-4E-hepten-3-one (AO-2), a natural diarylheptanoid, is previously found to have activities in neuronal differentiation and neurite outgrowth, and its analogue shows protective effects against Abeta. In this study, we further investigated the function of AO-2 toward Abeta-induced injuries in PC12 cells and hippocampal neurons. Pretreatment of PC12 cells with AO-2 restored cell viability in a concentration-dependent manner against Abeta-induced neurotoxicity. Moreover, the Abeta stimulated apoptosis and caspase-3 activation were markedly inhibited by AO-2. We found that AO-2 prevented the downregulation of PI3K-Akt-mTOR signaling after Abeta damage, and blockade of either PI3K or mTOR activity led to the failure of AO-2 on caspase-3 inhibition. We further showed that AO-2 was protective against two devastating effects of Abeta, increased reactive oxygen species (ROS) production and dendrite injury, and this protection was also dependent on PI3K and mTOR activities. Taken together, this study showed that AO-2 acts against Abeta-induced damages in PC12 cells and hippocampal neurons through PI3K-mTOR pathways, thus providing a new neuroprotective compound which may shed light on drug development of AD.

A Review on Pharmacological Properties of Zingerone (4-(4-Hydroxy-3-methoxyphenyl)-2-butanone).[Pubmed:26106644]

ScientificWorldJournal. 2015;2015:816364.

Humans have been using natural products for medicinal use for ages. Natural products of therapeutic importance are compounds derived from plants, animals, or any microorganism. Ginger is also one of the most commonly used condiments and a natural drug in vogue. It is a traditional medicine, having some active ingredients used for the treatment of numerous diseases. During recent research on ginger, various ingredients like zingerone, shogaol, and paradol have been obtained from it. Zingerone (4-(4-hydroxy-3-methoxyphenyl)-2-butanone) is a nontoxic and inexpensive compound with varied pharmacological activities. It is the least pungent component of Zingiber officinale. Zingerone is absent in fresh ginger but cooking or heating transforms gingerol to zingerone. Zingerone closely related to vanillin from vanilla and eugenol from clove. Zingerone has potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic, and so forth properties. Besides, it displays the property of enhancing growth and immune stimulation. It behaves as appetite stimulant, anxiolytic, antithrombotic, radiation protective, and antimicrobial. Also, it inhibits the reactive nitrogen species which are important in causing Alzheimer's disease and many other disorders. This review is written to shed light on the various pharmacological properties of zingerone and its role in alleviating numerous human and animal diseases.

Antispasmodic and antidiarrhoeal activities of 6-(4-hydroxy-3-methoxyphenyl)-hexanonic acid from Pycnocycla spinosa Decne. exBoiss.[Pubmed:25657799]

Res Pharm Sci. 2014 Jul-Aug;9(4):279-86.

Pharmacological activities of 6-(4-hydroxy-3-methoxyphenyl)-hexanonic acid (HMPHA), a phenolic compound, isolated from the extract of Pycnocycla spinosa was investigated on ileum motility in vivo and in vitro. Ileum motility was examined by measuring charcoal movement through the gut in mice. In addition, antidiarrhoeal activity of HMPHA was assessed and compared with standard drug; loperamide (2 mg/kg) and the hydroalcoholic extract of P. spinosa (2 mg/kg). Furthermore, concentration response curve to contraction induced by acetylcholine (ACh), 5-hydroxy triptamine (5-HT) and electrical field stimulation (EFS) were obtained after incubation of ileum segment with various concentrations of HMPHA or hydroalcoholic extract of P. spinosa. HMPHA (2 mg/kg and 5 mg/kg, orally) significantly inhibited gut movements in vivo and reduced diarrhoea induced by castor oil or sulphate magnesium. In addition, HMPHA reduced ileum contraction induced by ACh (IC50=33 +/- 6 mug/ml), 5-HT (IC50=87 +/- 12 mug/ml) and EFS (IC50=36 +/- 3 mug/ml) in vitro in a concentration-dependent manner. The inhibitory effect was reversible following washing off the drug. These studies indicate that HMPHA as an active component of P. spinosa extract has significant antispasmodic and antidiarrhoeal activities and therefore, has the potential as a lead compound for further development of a new spasmolytic remedy.