Cytotoxic and Anti-Inflammatory Activity of Labdane and cis-Clerodane Type Diterpenes

Demetzos, Costas; Dimas, Kostas; Hatziantoniou, Sophia; Anastasaki, Thalia; Angelopoulou, Dimitra

doi:10.1055/s-2001-17362

Cited by 65 publications

(51 citation statements)

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“…Labd-13(E)-ene-8α,15-diol (62) was cytotoxic to human T and pre-B cell lines . This compound had growth inhibitory and cytotoxic effects against numerous human and one mouse cancer cell lines, though this activity was weak in many cases (Chinou et al, 1994;Demetzos et al, 1994Demetzos et al, , 2001Dimas et al, 1998). It was found to reduce DNA synthesis (Dimas et al, 1998).…”

Section: 26mentioning

confidence: 99%

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

et al. 2007

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Plants in the genus Tripterygium, such as Tripterygium wilfordii Hook. f., have a long history of use in traditional Chinese medicine. In recent years there has been considerable interest in the use of Tripterygium extracts and of the main bioactive constituent, the diterpene triepoxide triptolide (1), to treat a variety of autoimmune and inflammation-related conditions. The main mode of action of the Tripterygium extracts and triptolide (1) is the inhibition of expression of proinflammatory genes such as those for interleukin-2 (IL-2), inducible nitric oxide synthase (iNOS), tumor necrosis factor-α (TNF-α), cyclooxygenase-2 (COX-2) and interferon-gamma (IFN-γ). The efficacy and safety of certain types of Tripterygium extracts were confirmed in human clinical trials in the US and abroad. Over 300 compounds have been identified in the genus Tripterygium, and many of these have been evaluated for biological activity. The overall activity of the extract is based on the interaction between its components. Therefore, the safety and efficacy of the extract cannot be fully mimicked by any individual constituent. This review discusses the biochemical composition and biological and pharmacological activities of Tripterygium extracts, and their main bioactive components.

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Section: 26mentioning

confidence: 99%

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

et al. 2007

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“…The herb is also used in the treatment of carbuncles, lung abscesses, breast lumps, and goiter. Additionally, DB was reported to display a range of pharmacological properties, including antitumor (Grynberg et al 1999), antifeedant (Cifuente et al 2002), anti-inflammatory (Demetzos et al 2001), and antisalmonellal activities (Teponno et al 2006). DB and related remedies are used for the treatment of thyroid gland diseases and a variety of tumors (Tang 1995;Rasikari et al 2005).…”

Section: Introductionmentioning

confidence: 98%

Metabolic activation of furan moiety makes Diosbulbin B hepatotoxic

Lin

Gao

et al. 2015

Arch Toxicol

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Diosbulbin B (DIOB), a furanoid, is a major constituent of herbal medicine Dioscorea bulbifera L. Exposure to DIOB caused liver injury in humans and experimental animals. The mechanisms of DIOB-induced hepatotoxicities remain unknown. The present study demonstrated that DIOB induced hepatotoxicities in a time- and dose-dependent manner in mice. H&E stained histopathologic image showed the occurrence of necrosis in the liver obtained from the mice treated with DIOB at dose of 200 mg/kg. Pretreatment with KTC protected the animals from hepatotoxicities and hepatic GSH depletion induced by DIOB, increased area under the concentration-time curve of blood DIOB, decreased urinary excretion of GSH conjugates derived from DIOB, and increased urinary excretion of parent drug. Pretreatment with BSO exacerbated DIOB-induced hepatotoxicities. In order to define the role of furan moiety in DIOB-induced liver toxicities, we replaced the furan of DIOB with a tetrahydrofuran group by chemical hydrogenation of the furan ring of DIOB. No liver injury was observed in the animals given the same doses of tetrahydro-DIOB. The furan moiety was essential for DIOB-induced hepatotoxicities. The results implicate the cis-enedial reactive metabolite of DIOB was responsible for the observed toxicities. The observed modest depletion of hepatic GSH in DIOB-treated animals suggests the actions of one or more reactive metabolites, and the hepatic injury observed could be due at least in part to reactions of these metabolites with crucial biomolecules. Cytochrome P450 3A enzymes are implicated in DIOB-induced hepatotoxicities by catalyzing the formation of the reactive metabolite of DIOB.

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“…The Cistaceae family (consisting of eight genera and 175 species) includes the genus Cistus, which comprises about 20 shrub species found broadly throughout the entire Mediterranean region (COMANDINI et al, 2006, TOMAS-MENOR et al, 2013 In Mediterranean folk medicine, Cistus species have been used as general remedies (BARRAJÓN-CATALÁN et al, 2010) and for their antiinflammatory (DEMETZOS et al, 2001), antiulcerogenic, wound healing, anti-microbial (DEMETZOS et al,1999, antifungal (BAYOUB et al, 2010), antiviral, anti-tumor (DIMAS et al, 2000, cytotoxic (BEN JEMIA et al, 2013) and antinociceptive (BARRAJÓN-CATALÁN et al, 2010) properties. For example, tea prepared from C. salvifolius L. herb (AL-KHALIL, 1995) has traditionally been used for the treatment of gout (AL-KHALIL, 1995) and ulcers (YESILADA et al, 1999).…”

Section: Introductionmentioning

confidence: 99%

Comparison of antioxidant and antimicrobial activities of two cultivated Cistus species from Tunisia

Mahmoudi¹,

Aouadhi²,

Kaddour³

et al. 2016

Biosci. J.

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ABSTRACT:The secondary metabolite composition, antioxidant activities, and microbial inhibition properties of leaves of two Cistus species; C. monspeliensis and C. salvifolius were investigated using three solvent extracts (ethanol, hexane and distilled water). Ethanol extracts were most efficient at extracting phenolics, flavonoids and condensed tannins compared to hexane and distilled water for both Cistus species. A total antioxidant test (TAA) and two radical scavenging tests (DPPH and ABTS) indicated that the 70% ethanolic extract from C. salvifolius leaves had stronger antioxidant activity compared to the C. monspeliensis 70% ethanol extract, while the aqueous extract of C. monspeliensis was much stronger than the aqueous extract or the 70% ethanol extract of C. salvifolius. Overall, the polar extracts were more active in both species than the non-polar extracts. Thus aqueous ethanol extracts of the leaves of each Cistus species were tested for their ability to inhibit seven pathogenic microbial strains, including Escherichia coli ATCC 8739, Salmonella typhimurium NCTC 6017, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 29213, Enterococcus faecalis, Aspergillus niger, and Candida albicans. Leaf ethanol extracts from both species were active against each microbial species, but the C. monspeliensis leaf ethanolic extract was much more active against several microbial species than that of C. salvifolius. For example, the C. salvifolius 70% ethanol extract showed its highest antimicrobial activity against P. aeruginosa and A. niger (MIC 3.1 mg/ml and MBC 6.3 mg/ml for both), while the C. monspeliensis extract showed much higher overall activity against E. coli, P. aeruginosa and C. albicana. (MIC 6.25 mg/ml and MBC 12.5 mg/ml for all three). In conclusion, maceration with 70% ethanol was the most efficient method for extracting total polyphenols, flavonoids, and condensed tannins from the two Cistus species, and the aqueous-ethanol extracts displayed the highest antioxidant and antimicrobial activities. Hence, the aqueousethanolic extracts of both species may be considered as potential sources of natural antioxidants and antimicrobial agents.

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Cytotoxic and Anti-Inflammatory Activity of Labdane and cis-Clerodane Type Diterpenes

Cited by 65 publications

References 0 publications

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

Metabolic activation of furan moiety makes Diosbulbin B hepatotoxic

Comparison of antioxidant and antimicrobial activities of two cultivated Cistus species from Tunisia

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