Bioactive compounds of Crocus sativus L. and their semi-synthetic derivatives as promising anti-Helicobacter pylori, anti-malarial and anti-leishmanial agents

被引：55

作者：

De Monte, Celeste ^{[1
]}

Bizzarri, Bruna ^{[1
]}

Gidaro, Maria Concetta ^{[2
]}

Carradori, Simone ^{[3
]}

Mollica, Adriano ^{[3
]}

Luisi, Grazia ^{[3
]}

Granese, Arianna ^{[1
]}

Alcaro, Stefano ^{[2
]}

Costa, Giosue ^{[2
]}

Basilico, Nicoletta ^{[4
]}

Parapini, Silvia ^{[5
]}

Scaltrito, Maria Maddalena ^{[4
]}

Masia, Carla ^{[4
]}

Sisto, Francesca ^{[4
]}

机构：

[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, Ple A Moro 5, I-00185 Rome, Italy

[2] Magna Graecia Univ Catanzaro, Dipartimento Sci Salute, Catanzaro, Italy

[3] G DAnnunzio Univ Chieti Pescara, Dept Pharm, Chieti, Italy

[4] Univ Milan, Dipartimento Sci Biomed Chirurg & Odontoiatr, Milan, Italy

[5] Univ Milan, Dipartimento Scienze Farmacol & Biomol, Milan, Italy

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2015年 / 30卷 / 06期

关键词：

Anti-leishmanial agents; anti-malarial agents; Crocus sativus L; Helicobacter pylori; safranal; CARRIER PROTEIN DEHYDRATASE; IN-VITRO; MOLECULAR DOCKING; UREASE; INHIBITION; ASSAY; CYTOTOXICITY; FLAVONOIDS; DISCOVERY; KINETICS;

D O I：

10.3109/14756366.2014.1001755

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Crocus sativus L. is known in herbal medicine for the various pharmacological effects of its components, but no data are found in literature about its biological properties toward Helicobacter pylori, Plasmodium spp. and Leishmania spp. In this work, the potential antibacterial and anti-parasitic effects of crocin and safranal, two important bioactive components in C. sativus, were explored, and also some semi-synthetic derivatives of safranal were tested in order to establish which modifications in the chemical structure could improve the biological activity. According to our promising results, we virtually screened our compounds by means of molecular modeling studies against the main H. pylori enzymes in order to unravel their putative mechanism of action.

引用

页码：1027 / 1033

页数：7

共 44 条

[1] [Anonymous], 2013, SCHROD SUIT 2013 PRO
[2] [Anonymous], GLID VERS 6 2
[3] [Anonymous], 2014, PYMOL MOL GRAPH SYST
[4] [Anonymous], LIGPREP VERS 2 9
[5] [Anonymous], PYMOL MOL GRAPH SYST
[6] [Anonymous], 2014, MAESTR VERS 9 7
[7] A novel nanobody against urease activity of Helicobacter pylori
Ardekani, Leila Safaee
Gargari, Seyed Latif Mousavi
Rasooli, Iraj
Bazl, Masoumeh Rajabi
Mohammadi, Mohammad
Ebrahimizadeh, Walead
Bakherad, Hamid
Zare, Hamed
[J]. INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES, 2013, 17 (09) : E723 - E728
[8] Synthesis, biological assay in vitro and molecular docking studies of new Schiff base derivatives as potential urease inhibitors
Aslam, Muhammad Adil S.
Mahmood, Shams-ul
Shahid, Mohammad
Saeed, Aamer
Iqbal, Jamshed
[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (11) : 5473 - 5479
[9] Design of inhibitors of Helicobacter pylori glutamate racemase as selective antibacterial agents: Incorporation of imidazoles onto a core pyrazolopyrimidinedione scaffold to improve bioavailabilty
Basarab, Gregory S.
Hill, Pamela
Eyermann, Charles J.
Gowravaram, Madhu
Kack, Helena
Osimoni, Ekundayo
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 22 (17) : 5600 - 5607
[10] New Applications and Mechanisms of Action of Saffron and its Important Ingredients
Bathaie, S. Zahra
Mousavi, S. Zeinab
[J]. CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION, 2010, 50 (08) : 761 - 786

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