Cytotoxic Thiophenes from the Root of Echinops grijisii Hance

Zhang, Peng; Liang, Dong; Jin, Wenrong; Qu, Haibin; Cheng, Yiyu; Li, Xian; Ma, Zhongjun

doi:10.1515/znc-2009-3-407

Cited by 14 publications

(10 citation statements)

References 10 publications

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“…The chemical composition of Echinops is also somewhat specific, and some species in this genus have insecticidal, nematicidal, antifungal, bactericidal and also antiviral properities (i.e. Fokialakis et al 2006 ; Zhanget al 2009 ; Abdelnabby and Abdelrahman 2012 ; Tekwu et al 2012 ; Gemechu et al 2013 ; Liu et al 2013 ). Therefore, the inhabitants of Echinops flower heads might also be protected from some parasites and predators because of the chemical compounds in the plant.…”

Section: Resultsmentioning

confidence: 99%

Description of the immature stages of Larinus vulpes and notes on its biology (Coleoptera, Curculionidae, Lixinae)

Skuhrovec¹,

Volovnik

Gosik³

2017

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Mature larva and pupa of Larinus vulpes (Olivier, 1807) (Curculionidae: Lixinae: Lixini) are morphologically described for the first time and compared with known larvae and pupae of other Larinus species. Very high counts of larval body setae (pronotum with more than 25 setae and postdorsum on meso- and metathorax and also on abdominal segments I–VII with more than 12 setae) are characteristic features of the nominotypical subgenus Larinus. The biology of the species was studied in Ukraine. Echinops ruthenicus and E. sphaerocephalus were identified as host plants of both larvae and adults of this weevil based on the present research in Ukraine, which shows probably oligophagous. Overwintering beetles emerged at the end of May or earlier, then feeding and mating on the host plants. The highest level of adult activity was observed at the end of June. Larvae were endophagous within the flower heads. In July and August, the larvae pupated within inflorescences in a pupation cell. Adults exited the cells at the end of August and did not hibernate on the host plants. Sometimes, larvae and imagines of a new generation were found outside the flower heads in chambers constructed on the stems.

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Section: Resultsmentioning

confidence: 99%

Description of the immature stages of Larinus vulpes and notes on its biology (Coleoptera, Curculionidae, Lixinae)

Skuhrovec¹,

Volovnik

Gosik³

2017

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“…These drugs exhibited higher activity than previous inhibitors [64]. Likewise, thiophene-containing natural products, such as the bi-thiophenes arctinal and arctinol-b, have been shown to have antifungal and antimicrobial activity [65], as well as other cytotoxic effects on tumoral cell lines [66]. Thiophene-modified coumarins also exhibit enhanced cytotoxicity towards cancer cell lines, whereas normal fibroblast cells are less affected [67].…”

Section: Discussionmentioning

confidence: 99%

Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery

Ripoll¹,

Herrero-Foncubierta²,

Puente-Muñoz³

et al. 2020

Preprint

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Recently, it was proposed that the thiophene ring is capable of promoting mitochondrial accumulation when linked to fluorescent markers. As a noncharged group, thiophene presents several advantages from a synthetic point of view, making it easier to incorporate such a side moiety into different molecules. Herein, we confirm the general applicability of thiophene group as mitochondrial carrier for drugs and fluorescent markers, based on a new concept of nonprotonable, noncharged transporters. We implemented this concept in a medicinal chemistry application by developing an anti-tumoral, metabolic chimeric drug, based on PDHK inhibitor dichloroacetate (DCA). The promising features of the thiophene moiety as a noncharged carrier for targeting mitochondria may represent a starting point for the design of new metabolism-aimed drugs.

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“…Similarly, Zhang et al (2009) evaluated the cytotoxic effect of thiophenes isolated from E. grijisii on human cancer cell lines, HL60 and K562. Significantly potent effect was achieved with 5 (IC 50 = 0.23 and 0.47 µg/mL) and 14 (IC 50 = 0.27 and 0.43 µg/mL) against HL60 and K562, respectively.…”

Section: Biological Activitiesmentioning

confidence: 99%

The Genus Echinops: Phytochemistry and Biological Activities: A Review

Bitew

Hymete

2019

Front. Pharmacol.

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The genus Echinops belongs to the family of Asteraceae and comprises about 130 species. Many species belonging to the genus Echinops are traditionally used as medicinals mainly in Africa and Asia. The genus is reported to contain diverse secondary metabolites. The aim of this review is to critically evaluate the available research reports on the genus and systematically organize the findings. Information for this study was obtained using various search engines including PubMed and Google Scholar. This review revealed that the genus is used traditionally to treat pain, inflammation, respiratory diseases, diseases caused by different microorganisms, as an aphrodisiac, to fasten expulsion of placenta, and for removal of renal stones. More than 151 secondary metabolites have been reported from the genus in which thiophenic compounds held the biggest share. Various extracts, essential oils, and isolated compounds from members of this genus are shown to exhibit different biological effects mainly anti-microbial, anti-proliferative, and anti-inflammatory. However, there are a number of species in this genus that are claimed to have traditional medicinal uses but their biological effect not yet been evaluated.

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Cytotoxic Thiophenes from the Root of Echinops grijisii Hance

Cited by 14 publications

References 10 publications

Description of the immature stages of Larinus vulpes and notes on its biology (Coleoptera, Curculionidae, Lixinae)

Description of the immature stages of Larinus vulpes and notes on its biology (Coleoptera, Curculionidae, Lixinae)

Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery

The Genus Echinops: Phytochemistry and Biological Activities: A Review

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