Allicin
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Garlic (Allium sativum L.) is a well-known spice widely utilised for its medicinal properties. There is an extensive record of the many beneficial health effects of garlic which can be traced back to as early as the ancient Egyptian era. One of the most studied properties of garlic is its ability to cure certain ailments caused by infections. In the 1940s, the antimicrobial activities exhibited by garlic were first reported to be due to allicin, a volatile compound extracted from raw garlic. Since then, allicin has been widely investigated for its putative inhibitory activities against a wide range of microorganisms. Allicin has demonstrated a preference for targeting the thiol-containing proteins and/or enzymes in microorganisms. It has also demonstrated the ability to regulate several genes essential for the virulence of microorganisms. Recently, it was reported that allicin may function better in combination with other antimicrobials compared to when used alone. When used in combination with antibiotics or antifungals, allicin enhanced the antimicrobial activities of these substances and improved the antimicrobial efficacy. Hence, it is likely that combination therapy of allicin with additional antimicrobial drug(s) could serve as a viable alternative for combating rising antimicrobial resistance. This review focuses on the antimicrobial activities exhibited by allicin alone as well as in combination with other substances. The mechanisms of action of allicin elucidated by some of the studies are also highlighted in the present review in order to provide a comprehensive overview of this versatile bioactive compound and the mechanistic evidence supporting its potential use in antimicrobial therapy.
- MeSH
- antiinfekční látky farmakologie terapeutické užití MeSH
- česnek chemie MeSH
- kombinovaná farmakoterapie MeSH
- kyseliny sulfinové farmakologie terapeutické užití MeSH
- lidé MeSH
- rostlinné extrakty farmakologie terapeutické užití MeSH
- synergismus léků MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
Garlic is a well-known example of natural self-defence system consisting of an inactive substrate (alliin) and enzyme (alliinase) which, when combined, produce highly antimicrobial allicin. Increase of alliinase stability and its activity are of paramount importance in various applications relying on its use for in-situ synthesis of allicin or its analogues, e.g., pulmonary drug delivery, treatment of superficial injuries, or urease inhibitors in fertilizers. Here, we discuss the effect of temperature, pH, buffers, salts, and additives, i.e. antioxidants, chelating agents, reducing agents and cosolvents, on the stability and the activity of alliinase extracted from garlic. The effects of the storage temperature and relative humidity on the stability of lyophilized alliinase was demonstrated. A combination of the short half-life, high reactivity and non-specificity to particular proteins are reasons most bacteria cannot deal with allicin's mode of action and develop effective defence mechanism, which could be the key to sustainable drug design addressing serious problems with escalating emergence of multidrug-resistant (MDR) bacterial strains.
- MeSH
- antibakteriální látky farmakologie MeSH
- Bacteria účinky léků ultrastruktura MeSH
- biokatalýza účinky léků MeSH
- časové faktory MeSH
- česnek enzymologie MeSH
- chemické jevy * MeSH
- disulfidy chemie metabolismus MeSH
- kinetika MeSH
- koncentrace vodíkových iontů MeSH
- kyseliny sulfinové chemie metabolismus MeSH
- lyasy štěpící vazby C-S metabolismus MeSH
- lyofilizace MeSH
- mikrobiální testy citlivosti MeSH
- mikrobiální viabilita účinky léků MeSH
- pufry MeSH
- stabilita enzymů účinky léků MeSH
- stereoizomerie MeSH
- teplota MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- MeSH
- antioxidancia terapeutické užití MeSH
- beta-karoten MeSH
- česneky MeSH
- dospělí MeSH
- infekce vyvolané Helicobacter pylori diagnóza farmakoterapie metabolismus MeSH
- kyselina askorbová MeSH
- lidé středního věku MeSH
- lidé MeSH
- rostlinné extrakty terapeutické užití MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- Publikační typ
- srovnávací studie MeSH
Práce shrnuje nové experimentální poznatky týkající se jednotlivých skupin organických sirnýchlátek česneku: sulfoxidů, thiosulfinátů, ajoenů, vinyldithiinů, alkyl a alkensulfidů a glutamylpep-tidů sirných aminokyselin, jejich transformačních reakcí (daných teplotou, pH, extrakčním prostře-dím a časem) a výsledných produktů transformací (obr. 1 a 2). Zabývá se aktivitou enzymu alliinázynezbytné pro přeměnu sulfoxidů přítomných v celistvém česneku, její izolací a stabilitou, jakoži stabilitou dominantního thiosulfinátu allicinu v různých prostředích a simulovaných tělních teku-tinách. Poukazuje na studie metabolizmu a přeměn nejdůležitějších sirných komponent in vitro nahepatocytech a na izolovaných játrech potkanů a in vivo na potkanech včetně skladby vydechova -ného vzduchu. Z publikovaných prací vyplývá, že všechny rozdílné degradační produkty thiosulfi-nátů, hlavně převažujícího allicinu, jsou nositeli rozmanitých biologických aktivit. Práce rovněžuvádí typy komerčních preparátů připravovaných z česneku, jejich rozdílnosti a značnou variabilituv obsahu účinných látek.
The paper sums up new experimental knowledge concerning the individual groups of organicsulfurous substances of the garlic: sulfoxides, thiosulfinates, ajoens, vinyldithiines, alkyl and alkenesulfides and glutamylpeptides of sulfurous amino acids, their transformation reactions (based onthe temperature, pH, extraction medium, and time) and the final products of transformations(Scheme 1, 2). It deals with the activity of the enzyme alliinase necessary for the transformation ofsulfoxides present in the whole garlic, its isolation and stability as well as the stability of thedominant thiosulfinate allicin in various media and simulated body fluids. It refers to the studiesof the metabolism and transformations of the most important sulfurous components performed invitro on the hepatocytes and on the isolated rat liver, and those carried out in vivo on the rats andincluding the examination of the composition of the exhaled air. It follows from published papersthat all different degradation products of thiosulfinates, mainly the prevailing allicin, are carriersof various biological activities. The paper also lists the types of commercial preparations preparedfrom the garlic, their differences, and considerable variability of their contents of active principles.
V posledních desetiletích se zvýšil počet systémových houbových onemocnění a zlepšila se identifikacejejich původců. Intenzivně se hledají nové léky, které by byly účinnější a méně toxické než dosudužívané. Z tohoto aspektu je věnována pozornost také česneku – jeho extraktům a jednotlivýmsložkám, tzn. allicinu, ajoenu, polysulfidům, silici. Nové experimentální poznatky potvrzují významnouantifungální aktivitu sirných sloučenin česneku. Ve sdělení je zmíněna také možnost využíváníčesnekových extraktů nebo silice v potravinářském průmyslu jako alternativní cesty ochranypotravin před kontaminací houbami.
The recent decades saw an increase in the number of systemic fungal diseases and improvementsin the identification of their causative agents. There has been an intensive search for new drugswhich would be more effective and less toxic than those already in use. From this aspect, attentionhas been paid also to garlic – its extracts and individual components, i.e., allicin, ajoen, polysulfides,essential oil. New experimental knowledge confirms a significant antifungal activity of sulfurouscompounds of garlic. The paper also mentions a possible use of employing garlic extracts or essentialoils in food industry as an alternative way of protection of foodstuffs from contamination with fungi.
BACKGROUND: Alliinase is an important enzyme occurring in Allium species that converts precursors of sulfuric compounds, cysteine sulfoxides into a biologically active substance termed allicin. Allicin facilitates garlic defense against pests and produces health-promoting compounds. Alliinase is encoded by members of a multigene family that has not yet been sufficiently characterized, namely with regard to the copy numbers occurring within the genome and the polymorphisms among the family members. RESULTS: We cloned 45 full-length alliinase amplicons of cultivar (cv.) Jovan. Sequence analyses revealed nine different sequence variants (SVs), confirming the multilocus nature of this gene family. Several mutations in exons, mainly occurring in the first exon coding for vacuolar signal peptide, were found. These results enabled us to identify sequences with putatively modified vacuole-targeting abilities. We found additional sequence variants using partial amplicons. We estimated that the minimum number of gene copies in the diploid genome of the investigated cultivar was fourteen. We obtained similar results for another three cultivars, which differed in bolting type and place of origin. The further identification of high degree of polymorphisms in the intron regions allowed us to develop a specific polymerase chain reaction assay capable to capture intron length polymorphism (ILP). This assay was used to screen 131 additional accessions. Polymorphic data were used for cluster analysis, which separated the bolting and non-bolting garlic types and those with high cysteine-sulfoxide contents in a similar way as AFLP analysis in previous study. These newly developed markers can be further applied for the selection of desirable garlic genotypes. CONCLUSIONS: Detailed analysis of sequences confirmed multigenic nature of garlic alliinase. Intron and exon polymorphism analysis generated similar results as whole genome variability assessed previously by AFLP. Detected polymorphism is thus also associated with cysteine-sulphoxide content in individual genotypes. ILP markers capable to detect intron polymorphisms were newly developed. Developed markers could be applied in garlic breeding. Higher genetic variability found in bolting genotypes may indicates longer period of their sexual propagation in comparison with nonbolting genotypes.
Allium sativum L. (Garlic) is a fragrant herb and tuber-derived spice that is one of the most sought-after botanicals, used as a culinary and ethnomedicine for a variety of diseases around the world. An array of pharmacological attributes such as antioxidant, hypoglycemic, anti-inflammatory, antihyperlipidemic, anticancer, antimicrobial, and hepatoprotective activities of this species have been established by previous studies. A. sativum houses many sulfur-containing phytochemical compounds such as allicin, diallyl disulfide (DADS), vinyldithiins, ajoenes (E-ajoene, Z-ajoene), diallyl trisulfide (DATS), micronutrient selenium (Se) etc. Organosulfur compounds are correlated with modulations in its antioxidant properties. The garlic compounds have also been recorded as promising immune-boosters or act as potent immunostimulants. A. sativum helps to treat cardiovascular ailments, neoplastic growth, rheumatism, diabetes, intestinal worms, flatulence, colic, dysentery, liver diseases, facial paralysis, tuberculosis, bronchitis, high blood pressure, and several other diseases. The present review aims to comprehensively enumerate the ethnobotanical and pharmacological aspects of A. sativum with notes on its phytochemistry, ethnopharmacology, toxicological aspects, and clinical studies from the retrieved literature from the last decade with notes on recent breakthroughs and bottlenecks. Future directions related to garlic research is also discussed.
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
... Allicin (302) —128. Weitere Phytoncide aus Knoblauch (304) — 129. Raphanin (304) — 130. ...
332 s. : il. ; 24 cm
- Konspekt
- Farmacie. Farmakologie
- NLK Obory
- farmacie a farmakologie
- farmakoterapie
- farmacie a farmakologie
- NLK Publikační typ
- studie
The ankyrin transient receptor potential channel TRPA1 is a non-selective cationic channel that is expressed by sensory neurons, where it can be activated by pungent chemicals, such as AITC (allyl isothiocyanate), cinnamon or allicin, by deep cooling (<18 °C) or highly depolarizing voltages (>+100 mV). From the cytoplasmic side, this channel can be regulated by negatively charged ligands such as phosphoinositides or inorganic polyphosphates, most likely through an interaction with as yet unidentified positively charged domain(s). In the present study, we mutated 27 basic residues along the C-terminal tail of TRPA1, trying to explore their role in AITC- and voltage-dependent gating. In the proximal part of the C-terminus, the function-affecting mutations were at Lys969, Arg975, Lys988 and Lys989. A second significant region was found in the predicted helix, centred around Lys1048 and Lys1052, in which single alanine mutations completely abolished AITC- and voltage-dependent activation. In the distal portion of the C-terminus, the charge neutralizations K1092A and R1099A reduced the AITC sensitivity, and, in the latter mutant, increased the voltage-induced steady-state responses. Taken together, our findings identify basic residues in the C-terminus that are strongly involved in TRPA1 voltage and chemical sensitivity, and some of them may represent possible interaction sites for negatively charged molecules that are generally considered to modulate TRPA1.
- MeSH
- aminokyseliny bazické genetika fyziologie MeSH
- ankyrinová repetice MeSH
- ankyriny MeSH
- ionty farmakologie MeSH
- kationtové kanály TRP chemie metabolismus MeSH
- lidé MeSH
- membránové potenciály fyziologie MeSH
- nervové receptory chemie MeSH
- proteiny nervové tkáně chemie metabolismus MeSH
- statická elektřina MeSH
- substituce aminokyselin MeSH
- vápníkové kanály chemie metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
... varíabilis -- Biologické zvláštnosti česneku -- Obsahové látky česneku -- Sirné látky -- Alliin -- Allicin ...
167 s. : il., tab. ; 25 cm
Publikace vychází z dlouholetých zkušeností autora, jehož snahou bylo shrnutí rozptýlených poznatků o česneku do jednoho přehledu. Čtenář se tak seznámí s česnekem jako s kulturní rostlinou a jejími zvláštnostmi, jeho původem, historií, biologií, pěstováním a zpracováním, obsahovými látkami podmiňujícími léčebné schopnosti a se zkušenostmi v oblasti medicíny.
- MeSH
- česnek MeSH
- hypolipidemika farmakologie metabolismus terapeutické užití MeSH
- léčivé rostliny MeSH
- Publikační typ
- monografie MeSH
- Konspekt
- Botanika
- NLK Obory
- zájmy a záliby
- botanika
- biologie
- farmacie a farmakologie
