JX-401 is potent, reversible inhibitor of p38α that displays no activity on the p38γ isoform. JX-401 is effective in mammalian cells, as it blocks the differentiation of myoblasts into myotubes.

The sesquiterpene trilactone bilobalide is one of the active constituents of the 50:1 Ginkgo biloba leaf extract widely used to enhance memory and learning. Bilobalide was found to antagonise the direct action of gamma-aminobutyric acid (GABA) on recombinant alpha(1)beta(2)gamma(2L) GABA(A) receptors. Bilobalide showed anticonvulsant properties through the activation of glutamic acid decarboxylase (GAD) enzyme, which is a key enzyme in biosynthesis of GABA. Bilobalide has been proposed to exert protective and trophic effects on neurons. Bilobalide may be useful in developing therapy for diseases involving age-associated neurodegeneration. Bilobalide is an active component of EGb, a standardised extract of Ginkgo biloba leaves. Bilobalide accounts for about 3% of the total extract.

S-ETHYLCYSTEINE is hydrophilic cysteine-containing compound naturally synthesized in many Allium plant foods such as garlic and onion. Dietary intake of S-Ethyl-L-cysteine displayed anti-oxidative and anti-inflammatory protection against ethanol-induced liver injury in mice. S-Ethyl-L-cysteine ameliorated H2O2-induced apoptotic, oxidative and inflammatory injury in human BEAS-2B cells (bronchial cells) through preserving Bcl-2 expression, decreasing ROS formation and limiting protein expression of NAPDH oxidase, NF-kB, and MAPK. S-Ethyl-L-cysteine is used as the chiral reagent.

Datiscetin is a yellow plant dye from the flavonol group. It exhibited inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA). Datiscetin demonstrated antioxidant activity – it inhibits CCl4-induced microsomal lipid peroxidation and behaved as potent scavenger of the superoxide anion radicals. Datiscetin activated the human constitutive androstane receptor. It inhibited amyloid beta-42 protein aggregation. Datiscetin interacts with amyloid beta-42 protein directly, with monomers and small aggregates.

Cholesteryl hemisuccinate (CHEMS) is an acidic cholesterol ester. It self-assembles into bilayers in alkaline and neutral aqueous media. CHEMS exhibits pH sensitive polymorphism. It consists of succinic acid esterified to the beta-hydroxyl group of cholesterol. It was shown; that CHEMS was potent inhibitors of acetylcholinesterase and it alone or in combination with tetrahydroaminoacridine could be used in the treatment of organophosphate poisoning and Alzheimer's disease. It was also revealed, that CHEMS upon incorporation into the cell membrane, which presumably promotes the expression of latent tumor-associated antigens, induced a marked increase in specific immunogenicity of tumor cells.

4-Hydroxyindole is a simple indole derivative. It effectively inhibits Abeta peptide-induced amyloid fibril formation and prevent cell death induced by the peptide in culture. 4-Hydroxyindole was glucuronidated mainly by UGT1A6, with minor activity by UGT1A9. 4-hydroxyindole is used for the synthesis of anti-inflammatory angular pyrrolocoumarins.

Isoacteoside (2-(3′,4′-dihydroxyphenyl)ethyl 6-O-caffeoyl-3-O-(α-l-rhamnopyranosyl)-β-d-glucopyranoside), a phenylethanoid glycoside isomeric to acteoside, exists in various plants, such as Cistanches spp., Castilleja spp. and Plantago spp. It exerts wide range of pharmacological activity including anti-inflammatory and cytoprotective actions.

Salsolidine is a simple 1-substituted tetrahydroisoquinoline isolated from many natural sources as the racemate and in its enantiomeric modifications. Stereoselective competitive inhibition of MAO A was found with the R enantiomer of salsolidine (Ki = 6 uM). Salsolidine also inhibits acetylcholinesterase (AChE), and buytlcholinesterase (BChE). Salsolidine may inhibit catechol-O-methyltransferase (COMT). Derivatives of salsolidine are neurotoxic and cytotoxic. R enantiomer of salsolidine is more potent than the S form.

Allocryptopine is isoquinoline alkaloid found primarily in the plant families Fumariaceae, Papaveraceae, Berberidaceae, Ranunculaceae, Rutaceae, and Sapindaceae. It have been reported to possess strong antibacterial, anti-inflammatoty, antiparasitic, antineoplastic and anti-addictive activities. Allocryptopine inhibits human acetylcholinesterase and butyrylcholinesterase. It blocks hERG current in HEK293 cells. Allocryptopine strongly enhanced the I(peak) of the T353I channel by enhancing the plasma membrane (PM) expression of Nav1.5 and rescued defective trafficking after co-incubation with HEK293 cells that carry mutation channel 24 h. A possible preparation for the treatment of HIV-1 and HIV-2 viruses containing pharmaceutically effective amounts of allocryptopine has been patented.

Geniposide, a key component extracted from the fruit of Gardenia jasminoides Ellis, is a major iridoid glycoside considered to be responsible for various biological effects of the herbs, and its aglycon is genipin. Gardenia is a widely used Chinese herb for the treatment of hepatic disease, inflammation disorders, contusions and brain disorders. Increasing studies have focused on the neuroprotective effect of geniposide in brain diseases, especially neurodegenerative disorders. Its protective effect from memory impairment and the normalization of objection recognition has been shown in animal behavioral experiments. Using a high-throughput screen for GLP-1R agonists, geniposide was identified as an agonist for GLP-1R. It has been shown that the activation of GLP-1R by geniposide induces neurotrophic and neuroprotective effects in cells. Geniposide exerted anti-inflammatory effects by interfering with the expression of P2Y14 receptor, which subsequently inhibits the downstream ERK1/2 signaling pathways and the release of the pro-inflammatory cytokines IL-8, MCP-1, IL-1β.