Izolace, identifikace a biologická aktivita obsahových látek druhů rodu Coleus

PharmDr. Sabína Jurkaninová

Doctoral thesis

Isolation, identification and biological activity of compounds from genus Coleus.

Abstract:

From the three plant species, Coleus blumei Benth, C. aromaticus Benth., and C. caninus (Roth.) Vatke, predominantly from Asia, twelve pure compounds were isolated in this study. Already known caffeic acid, rosmarinic acid, luteolin, nepetoidin B (C. blumei), vicenin-2, cirsimaritin (C. aromaticus), 12-O-deacetyl-coleon R (C. caninus) and new compounds spirocoleon-7-O-β-D-glucoside, apigenin-7-O-(3´´-O-acetyl)-β-D-glucuronide, apigenin-5-O-(3´´-O-acetyl)-β-D-glucuronide, sincoetsin C (C. blumei) and 3,12-bis-(O-deacetyl)-coleon R (C. caninus), which have not been described in the literature before. The substances were tested for in vitro biological activity against the enzymes collagenase, elastase, hyaluronidase, xanthine oxidase, cyclooxygenase-1 and cyclooxygenase-2 and tested for their antioxidant activity in vitro. The most promising compound is nepetoidin B, which was isolated from C. blumei for the first time. It significantly inhibited collagenase, elastase, hyaluronidase and xanthine oxidase and also showed antioxidant activity. Luteolin significantly inhibited elastase, hyaluronidase and xanthine oxidase and also showed antioxidant activity. Rosmarinic acid has confirmed its strong antioxidant properties. Sincoetsin C and apigenin-5-O-(3´´-O-acetyl)-β-D-glucuronide were the most important collagenases among the tested compounds. Sincoetsin C together with spirocoleon-7-O-β-D-glucoside was tested for antibacterial activity against methicillin-resistant strain of Staphylococcus aureus subsp. aureus CCM 4750 (MRSA) in vitro. Sincoetsin C proved also in this test to be a promising compound with antibacterial activity. The compounds of C. blumei Benth., C. aromaticus Benth., and C. caninus (Roth.) Vatke appear to be effective agents in the prevention and treatment of inflammatory skin diseases associated with oxidative stress and photoaging that may adversely affect human health.

Abstract:

Z troch rastlinných druhov, Coleus blumei Benth., C. aromaticus Benth. a C. caninus (Roth.) Vatke, pochádzajúcich prevažne z Ázie, sa podarilo v rámci tejto štúdie izolovať dvanásť čistých látok. Známu kyselinu kávovú, kyselinu rozmarínovú, luteolín, nepetoidín B (C. blumei), vicenín-2, cirsimaritín (C. aromaticus), 12-O-deacetyl-coleon R (C. caninus) a nové látky spirocoleon-7-O-β-D-glukozid, apigenín-7-O-(3´´-O-acetyl)-β-D-glukuronid, apigenín-5-O-(3´´-O-acetyl)-β-D-glukuronid, sincoetsin C (C. blumei) a 3,12-bis-(O-deacetyl)-coleon R (C. caninus), ktoré doposiaľ neboli popísané v literatúre. Látky boli podrobené testovaniu biologickej aktivity in vitro voči enzýmom kolagenáza, elastáza, hyaluronidáza, xantínoxidáza, cyklooxygenáza-1 a cyklooxygenáza-2 a bola testovaná ich antioxidačná aktivita in vitro. Najperspektívnejšou látkou je nepetoidín B, ktorý sa podarilo z druhu C. blumei izolovať po prvýkrát. Signifikantne inhiboval kolagenázu, elastázu, hyaluronidázu a xantínoxidázu a vykazoval aj antioxidačnú aktivitu. Luteolín signifikantne inhiboval elastázu, hyaluronidázu a xantínoxidázu a vykazoval takisto antioxidačnú aktivitu. Kyselina rozmarínová potvrdila svoje silné antioxidačné vlastnosti. Sincoetsin C a apigenín-5-O-(3´´-O-acetyl)-β-D-glukuronid boli najvýznamnejšími inhibítormi kolagenázy spomedzi testovaných látok. U sincoetsinu C spoločne so spirocoleon-7-O-β-D-glukozidom bola testovaná antibakteriálna aktivita proti meticilín rezistentnému kmeňu Staphylococcus aureus subsp. aureus CCM 4750 (MRSA) in vitro. Sincoetsin C sa aj v tomto teste preukázal ako perspektívna látka s antibakteriálnou aktivitou. Obsahové látky C. blumei Benth., C. aromaticus Benth. a C. caninus (Roth.) Vatke sa javia ako účinné prostriedky v prevencii a liečbe zápalových ochorení kože súvisiacich s oxidačným stresom a fotostarnutím, ktoré môžu negatívne ovplyvňovať zdravie ľudí.

Keywords

anti-MRSA aktivita, antioxidačná aktivita, Coleus, cyklooxygenáza, elastáza, fotostarnutie, hyaluronidáza, kolagenáza, oxidačný stres, xantínoxidáza anti-MRSA activity, antioxidant activity, cyclooxygenase, elastase, photoaging, hyaluronidase, collagenase, oxidative stress, xanthin oxidase

Language used: Slovak

Date on which the thesis was submitted / produced: 13. 9. 2021

Thesis defence

• Date of defence: 14. 12. 2021
• Supervisor: doc. PharmDr. Renata Kubínová, Ph.D.
• Reader: doc. PharmDr. Silvie Bittner Fialová, Ph.D., doc. Ing. Jaroslav Havlík, Ph.D.

Masaryk University

Faculty of Pharmacy

Doctoral programme:
Pharmacognosy