Essential oils and their volatile constituents are used widely to prevent and treat human disease. The possible role and mode of action of these natural products is discussed with regard to the prevention and treatment of cancer, cardiovascular diseases including atherosclerosis and thrombosis, as well as their bioactivity as antibacterial, antiviral, antioxidants and antidiabetic agents. Their application as natural skin penetration enhancers for transdermal drug delivery and the therapeutic properties of essential oils in aroma and massage therapy will also be outlined.

Pharmaceutical and therapeutic potentials of essential oils and their individual volatile constituents: a review.

Anaphylaxis

Pharmacognostic and pharmacological profile of Humulus Lupulus L.

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The Botany Of Mangroves

We tested whether the dominant intestinal sugar transporter GLUT2 was inhibited by intestinal luminal compounds that are inefficiently absorbed and naturally present in foods. Because of their abundance in fruits and vegetables, flavonoids were selected as model compounds. Robust inhibition of glucose and fructose transport by GLUT2 expressed in Xenopus laevis oocytes was produced by the flavonols myricetin, fisetin, the widely consumed flavonoid quercetin, and its glucoside precursor isoquercitrin. IC50s for quercetin, myricetin, and isoquercitrin were ∼200- to 1000-fold less than glucose or fructose concentrations, and noncompetitive inhibition was observed. The two other major intestinal sugar transporters, GLUT5 and SGLT1, were unaffected by flavonoids. Sugar transport by GLUT2 overexpressed in pituitary cells and naturally present in Caco-2E intestinal cells was similarly inhibited by quercetin. GLUT2 was detected on the apical side of Caco-2E cells, indicating that GLUT2 was in the correct orientati...

Inhibition of the intestinal glucose transporter GLUT2 by flavonoids

To study the effects of polyphenols on the Na(+)/glucose cotransporter (SGLT1) response, SGLT1 was expressed in Xenopus oocytes by injecting cRNA synthesized from the cloned cDNA of the small intestine cotransporter of rats, and the electrical response elicited by glucose or galactose was measured by a voltage clamping method. Most phenol derivatives had no effect on the response. However, the polyphenols (+)-catechin, (-)-epicatechin gallate (ECg), and (-)-epigallocatechin gallate (EGCg), which are components of green tea, caused an inhibition of the response, which was almost independent of glucose concentration. The inhibition constants were estimated to be 2.3 mM for (+)-catechin and 0.45 mM for both ECg and EGCg, assuming the noncompetitive inhibition mechanism. Saponin prepared from tea seeds also inhibited the response significantly. Tannic acid and aqueous extracts of teas induced nonspecific electrical responses in both cRNA-injected and noninjected oocytes at lower concentrations than those that caused an inhibition of the SGLT1 response when their dose-dependent effects were examined. These results are possibly helpful in the development of a dietary supplement for diabetic patients.

Polyphenol-Induced Inhibition of the Response of Na+/Glucose Cotransporter Expressed in Xenopus Oocytes

To study the effects of tea components on ionotropic gamma-aminobutyric acid (GABA) receptor response, ionotropic GABA receptors (GABA(A) receptors) were expressed in Xenopus oocytes by injecting cRNAs synthesized from cloned cDNAs of the alpha(1) and beta(1) subunits of the bovine receptors, and their electrical responses were measured by a voltage clamping method. Extracts of green tea, black tea, and oolong tea in an aqueous solution induced the GABA-elicited response, which showed that these teas contain GABA, whereas coffee does not. Caffeine weakly inhibited the response in a competitive manner (K(i) = 15 mM), and (+)-catechin inhibited it in a noncompetitive one (K(i) = 1.7 mM). Especially, two catechin derivatives, (-)-epicatechin gallate and (-)-epigallocatechin gallate, inhibited the response strongly. Alcohols such as leaf alcohol or linalool potentiated the response, possibly because their binding to the potentiation site enhances the GABA-binding affinity to GABA(A) receptors when they bind. Extracts of green tea made with ethyl ether, which must contain lipophilic components of green tea, inhibited the response elicited by GABA, possibly because the amounts of caffeine and catechin derivatives were much larger than fragrant alcohols in such extracts of tea.

Effects of Coffee Components on the Response of GABAA Receptors Expressed in Xenopus Oocytes

We electrophysiologically investigated the effect of some fragrant compounds in oolong tea on the response of ionotropic gamma-aminobutyric acid (GABA) receptors (GABAA receptors) which were expressed in Xenopus oocytes. Of the tested fragrances in oolong tea, cis-jasmone, jasmine lactone, linalool oxide and methyl jasmonate significantly potentiated the response. Among these, cis-jasmone and methyl jasmonate potently potentiated the response, having a respective dissociation constant of the compound (Kp) and maximum potentiation (Vm) of 0.49 mM and 322% for cis-jasmone, and 0.84 mM and 450% for methyl jasmonate. Inhalation of 0.1% cis-jasmone or methyl jasmonate significantly increased the sleeping time of mice induced by pentobarbital, suggesting that these fragrant compounds were absorbed by the brain and thereby potentiated the GABAA receptor response. Both of these compounds may therefore have a tranquillizing effect on the brain.

https://www.tandfonline.com/doi/pdf/10.1271/bbb.68.1842

Fragrances in Oolong Tea That Enhance the Response of GABAA Receptors

To seek out a cheap source of dietary polyphenols and antioxidants along with anti-amylase and anti-glucosidase activities, ethanol extracts of eleven cheap Bangladeshi fruits were investigated. The extracts were also examined for anti-allergic activity using rat peritoneal exudate cells exposed to the calcium ionophore A23187. Phyllanthus emblica (emblic myrobalan) had the highest total polyphenol content (339 mg gallic acid equivalent (GAE)/g), followed by Syzygium cumini (Indian blackberry; 192.3 mg GAE/g), and Aegle marmelos (wood apple; 53.7 mg GAE/g). P. emblica, and S. cumini also exhibited the most potent DPPH radical scavenging activity, with an IC50 of 2.1 and 8.6 μg/mL respectively. These extracts also showed promising reducing powers with P. emblica having the greatest such activity (optical density (O.D.) 1.66), followed by S. cumini (O.D. 1.34), at a concentration of 0.2 mg/mL. The extracts of Artocarpus heterophyllus (jackfruit) and S. cumini showed promising chelating activities. At a concentration of 1 mg/mL, Dillenia indica (chalta) showed the highest inhibition of α-amylase activity (60%), and A. marmelos, D. indica, P. emblica, Spondias dulcis (hog-plum) & S. cumini completely inhibited α-glucosidase activity (100%). Apart from A. heterophyllus, D. indica and Phyllanthus acidus (star-gooseberry), all other extracts inhibited the release of histamine from the peritoneal exudate cells, with S. cumini having the strongest effect. These fruits therefore have activities beneficial to physiological health.

Total Phenolic Content, Antioxidative, Anti-amylase, Anti-glucosidase, and Antihistamine Release Activities of Bangladeshi Fruits

Beer induced the response of the ionotropic γ-aminobutyric acid receptors (GABAA receptors) expressed in Xenopus oocytes, indicating the presence of γ-aminobutyric acid (GABA)-like activity. Furthermore, the pentane extract of the beer, hop (Humulus lupulus L.) oil, and myrcenol potentiated the GABAA receptor response elicited by GABA. The GABAA receptor responses were also potentiated by the addition of aliphatic esters, most of which are reported to be present in beer flavor. Aliphatic esters showed the tendency to decrease in the potentiation of the GABAA receptor response with an increase in their carbon chain length. When myrcenol was injected to mice prior to intraperitoneal administration of pentobarbital, the pentobarbital-induced sleeping time of mice increased additionally. Therefore, the beer contained not only GABA-like activity but also the modulator(s) of the GABAA receptor response. Keywords: Beer; GABA; GABAA receptor; hop; myrcenol

Sheikh Julfikar Hossain

Papers

Polyphenol-Induced Inhibition of the Response of Na+/Glucose Cotransporter Expressed in Xenopus Oocytes

Effects of Coffee Components on the Response of GABAA Receptors Expressed in Xenopus Oocytes

Fragrances in Oolong Tea That Enhance the Response of GABAA Receptors

Total Phenolic Content, Antioxidative, Anti-amylase, Anti-glucosidase, and Antihistamine Release Activities of Bangladeshi Fruits

Effects of Beer and Hop on Ionotropic γ-Aminobutyric Acid Receptors