Zingiber officinale is one of the most frequently used medicinal herbs in Asia. Using rodent seizure models, it was previously shown that Zingiber officinale hydroethanolic extract exerts antiseizure activity, but the active constituents responsible for this effect have not been determined. In this paper, we demonstrated that Zingiber officinale methanolic extract exerts anticonvulsant activity in the pentylenetetrazole (PTZ)-induced hyperlocomotion assay in larval zebrafish. Next, we isolated 6-gingerol (6-GIN)—a major constituent of Zingiber officinale rhizoma. We observed that 6-GIN exerted potent dose-dependent anticonvulsant activity in the PTZ-induced hyperlocomotion seizure assay in zebrafish, which was confirmed electroencephalographically. To obtain further insight into the molecular mechanisms of 6-GIN antiseizure activity, we assessed the concentration of two neurotransmitters in zebrafish, i.e., inhibitory γ-aminobutyric acid (GABA) and excitatory glutamic acid (GLU), and their ratio after exposure to acute PTZ dose. Here, 6-GIN decreased GLU level and reduced the GLU/GABA ratio in PTZ-treated fish compared with only PTZ-bathed fish. This activity was associated with the decrease in grin2b, but not gabra1a, grin1a, gria1a, gria2a, and gria3b expression in PTZ-treated fish. Molecular docking to the human NR2B-containing N-methyl-D-aspartate (NMDA) receptor suggests that 6-GIN might act as an inhibitor and interact with the amino terminal domain, the glutamate-binding site, as well as within the ion channel of the NR2B-containing NMDA receptor. In summary, our study reveals, for the first time, the anticonvulsant activity of 6-GIN. We suggest that this effect might at least be partially mediated by restoring the balance between GABA and GLU in the epileptic brain; however, more studies are needed to prove our hypothesis.
Background: In the search for novel antidepressive drug candidates, bioguided fractionation of nonpolar constituents present in the oleoresin from ginger rhizomes (Zingiber officinale Roscoe, Zingiberaceae) was performed. This particular direction of the research was chosen due to the existing reports on the antidepressive properties of ginger total extract. The search for individual metabolites acting as MAO-A inhibitors, which correspond to the apparent effect of the total extract, is the subject of this work. Methods: Hexane extracts from ginger rhizomes were fractionated by using column chromatography (including silica gel impregnated with silver nitrate) and semi-preparative high-performance chromatography. For the activity assessment, an in vitro monoamine oxidase A (MAO-A) inhibition luminescence assay was performed on 10 purified terpenes: 1,8-cineole, α-citronellal, geraniol, β-sesquiphellandrene, γ-terpinen, geranyl acetate, isobornyl acetate, terpinen-4-ol, (E,E)-α-farnesene, and α-zingiberene. Results: Geraniol and (−)-terpinen-4-ol were found to be the strongest enzyme inhibitors with inhibition of 44.1% and 42.5%, respectively, at a concentration of 125 µg/mL. No differences in the inhibition potential were observed for the different groups of terpenes: sesquiterpenes, monoterpenes, or sesquiterpene alcohols; however, the two most active compounds contained a hydroxyl moiety. Conclusions: Terpene constituents from ginger’s extract were found to exhibit moderate inhibitory properties against the MAO-A enzyme in in vitro tests.
Ginger (Zingiber officinale Rosc.) is both a commonly used spice, and an ingredient of various dietary supplements and medications. Its diverse applications result from the range of health benefits that this plant brings thanks to the presence of active compounds (secondary metabolites) in the matrix. Even if several studies underline a stronger pharmacological activity of fresh ginger rhizomes, the unprocessed plant is relatively rarely used. Ginger rhizomes are subjected to thermal processing, such as boiling, blanching, steam drying and others, at different temperature and time settings. Additionally, freeze-drying of the rhizomes is used as the first step in the preparation of raw material. It was proved that the composition of secondary metabolites of the Zingiber officinale rhizome changes upon the influence of temperature. Therefore, the aim of the review was to put together scientific results on the impact of traditional and unconventional methods of heat treatment on ginger rhizomes and to show the compositional differences that they induce in the plant matrix. Variations in the content and the transformation of some compounds into other metabolites will be also discussed, with particular attention paid to two major groups of secondary metabolites present in the plant, namely, phenolics and terpenes.
Ginger (Zingiber officinale Rosc.) is a spice, medicinal and cosmetic plant that has been known for centuries. It can be used in dried, fresh, marinated or candied form, and is also an essential ingredient in well-known curry blends. Ginger rhizomes are often freeze-dried as the first step in the preparation of the raw material. Many studies have proved that the composition and biological activity of ginger changes due to thermal processing. Therefore, the aim of the review was to summarize the scientific results on the impact of traditional and unconventional methods of the heat treatment of ginger rhizomes and their influence on the antioxidant and other selected biological activities of the plant. The review of the available scientific data is inconclusive, and it is hard to state unequivocally whether the thermal treatment of the raw material increases or decreases biological activity. Based on the presented literature review, it can be concluded that traditional cooking and microwave processing in general decrease the antioxidant activity of the ginger rhizome, whereas frying, autoclaving, blanching or traditional drying in the sun mostly lead to a significant increase in ginger activity. Interesting data were presented in the works describing the freeze-drying process during which the antioxidant potential of ginger increased.
Curcuma longa from Zingiberaceae belongs to the major spices consumed around the world, known from its cholagogue, anti-inflammatory, and antimicrobial properties. Lack of data on the activity of single components of turmeric extract encouraged the authors to apply TLC (thin-layer chromatography) based bioautography studies to reveal its antimicrobial constituents and construct a universal platform for the bioactivity assessment of crude extracts, with help of a freeware ImageJ software. This optimized chromatographic bioassay performed on diethyl ether and methanol extracts of Curcuma longa was successfully applied on the total extract and revealed the antimicrobial potential of single components against a variety of Gram-positive strains, with no need for their isolation from the mixture. The obtained results were further confronted with a classic microdilution antimicrobial assay on the isolates, purified from the crude extracts by centrifugal partition chromatography in the following solvent system: heptane-chloroform-methanol-water (5:6:3:2) (v/v/v/v).