bitter

Sucrose octaacetate is an acetylated derivative of sucrose used as a food additive, binder, and plasticizer. It is also incorporated in many pesticides, insecticides, and other toxic products as a deterrent to accidental poisoning.

Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a derivative of quinine with antimicrobial activity against Streptococcus pneumoniae and antimalarial activity with an IC50 of 25.75 nM against Plasmodium falciparum. It is also an agonist of Gallus gallus2 receptors (ggTas2r1, ggTas2r2, and ggTas2r7).

(R)-(+)-Citronellal ((+)-Citronellal) is a monoterpene compound isolated from citrus, lavender, and eucalyptus oils. It has antifungal activity and reduces the bitterness of caffeine by inhibiting bitter receptors TAS2R43 and TAS2R46. It is commonly used in skincare products.

Lascivol is a bitter substance derived from Tricholoma lascivum.

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA ethyl ester is a neutral, more lipid soluble form of the free acid.

Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA methyl ester is a neutral, more lipid soluble form of the free acid.

Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1, capable of autoinducing the production of antibacterial substances active against S. aureus at low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro at concentrations of 16 and 32 μM, increases phosphorylation of the PI3K substrate Akt, and this induction can be blocked by the PI3K inhibitor LY294002. Additionally, it enhances axon sprouting of calcitonin gene-related protein positive (CGRP+) primary afferents in the spinal cord post-crush injury and of serotonin neurons in the uninjured spinal cord. Cyclo(L-Phe-L-Val) is also a bitter taste component of cocoa and roasted coffee.

Kushenol O is a natural compound that belongs to the flavonoid group. It can be isolated from bitter ginseng.

Colupulone, a bitter β-acid, can be isolated from hops [1].

GIV3727, a bitter taste receptor hTAS2R antagonist, inhibits the activation of hTAS2R31 by saccharin and acesulfame potassium, effectively diminishing the bitter taste in foods, beverages, and pharmaceuticals [1].

Glycyrrhetinic acid-d3 is a deuterated compound of Glycyrrhetinic acid. Glycyrrhetinic acid has a CAS number of 1449-05-4. Enoxolone (INN, BAN; also known as glycyrrhetinic acid) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb licorice. It is used in flavoring and it masks the bitter taste of drugs like aloe and quinine. It is effective in the treatment of peptic ulcer and also has expectorant (antitussive) properties.

Mogroside IIe is a bitter triterpenoid saponin which is the main component of unripe Luo Han Guo fruit and a precursor of the commercially available sweetener mogroside V.

Glaucarubin is a bitter lactone naturally found in the fruits of Simaruba glauca. It is employed as an anti-amebic agent in research focused on amebiasis. The compound exhibits good tolerability, with a median lethal dose (LD50) of 1,600 mg/kg in mice and 6,400 mg/kg in rats.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

Momordicoside A is a triterpenoid saponin compound isolated from bitter melon (Momordica charantia L.), which possesses a variety of biological activities, including inhibition of protein tyrosine phosphatase (PTP1B), and can be used in the treatment of type 2 diabetes. In addition, Momordicoside A has anti-inflammatory, antioxidant, antitumor, and anti-HIV AIDS potentials.

Momordicosides K and L, the main bitter taste triterpene glycosides in Bitter melon; and bitter melon has been reported to have hypoglycemic, anti atherogenic and anti HIV activities.

Yadanziolide B, a bitter wood bittersweet analog from the stem of Brucea mollis, is cytotoxic with an IC50 value of 3.00-5.81 μM.

Bruceoside A is a bitter wood glycoside that can be isolated from opuntia and has anticancer and tumor activity and can be used with the study of leukemia.

Dehydrobruceantinol shows bitter taste and has antileukemic activity.

Glaucin B is a new bitter limonoid.

Jasminin is a bitter natural compound that belongs to the flavonoid family found in a variety of plants, including jasmine, and has been shown to have anti-inflammatory, antioxidant, and antitumor activity.

Lyoniresinol, a lignan isolated from Tarenna attenuata, exhibits free radical scavenging activity (IC50 of 82.4 μM) and DPPH antioxidant activity, demonstrating anti-melanogenic properties. It possesses a strong bitter taste, whereas its enantiomer (-)-Lyoniresinol is odorless.

Trifloroside is a bitter iridoid glycoside.

Campneoside I, a bitter phenyl propanoid glycoside, can be isolated from the roots of Incarvillea compacta [1] [2].