General Behavior, Toxicity, and Cytotoxic Activity of Elenoside, a Lignan from Justicia hyssopifolia

Abstract

Cytotoxicity, acute toxicity, and general pharmacological effects in mice of an arylnaphthalene lignan isolated from Jisticia hyssopifolia were studied. Elenoside was cytotoxic to human cancer cell lines in a range of concentrations from 10(-5) to 10(-4)M. It has an LD(50), ip in mice, of 305 mg/kg and central depressive properties at doses of 25, 50, and 100 mg/kg. Thus, elenoside appears to be a sedative with broad spectrum cytotoxicity.

Chemical constituents and biological activities of species of Justicia: a review

“…This compound shows sedative, muscle relaxant, cytotoxic, antiviral, insecticidal, cardiotonic, analgesic, lipid peroxidation inhibitory, anti-inflammatory, and stimulant activities and exhibits significant central nervous system depressant properties in rats. Its anxiolytic action, inducing sedation and muscle relaxation (Navarro et al, 2001a), is similar to other tranquilizer drugs (Irwin, 1968) such as the action of sedative-hypnotic barbiturates (Navarro et al, 2004). The cytotoxic activity of 42 was verified in human cancer cell lines in a range of concentrations from 10 -5 to 10 -4 M, with an LD50 of 305 mg/kg in mice and central depressive properties at doses of 25, 50, and 100 mg/kg.…”

“…No lethality was observed for five days following administration of this compound (Alonso et al, 1997). As a consequence, this compound behaves as a sedative with broad-spectrum cytotoxicity (Navarro et al, 2001b), also showing cytotoxic effects toward leukemia cell lines (Navarro et al, 2001a).…”

Ailanthoidol Derivatives and their Anti-inflammatory Effects

“…14 In order to investigate the anti-inflammatory properties of the prepared seven benzofurans (2)(3)(4)(5)(6)(7)(8) to compare with which of ailanthoidol 1, we measured the amount of nitric oxide (NO), which is one of essential mediators on inflammation, in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages (Fig. 2 and Table 2).…”

“…1 While there have been no reports on this compound's biological activities, extracts of the bark and leaves of this tree have been used in folk medicine. The 2-arylbenzo[b]furan structures in natural and unnatural sources showed a wide variety of biological activities including anticancer, 2 antiproliferative, 3 antiinflammatory, 4 antiviral, 5 antifungal, 6 immunosuppressive, 7 antiplatelet, 8 antioxidative, 9 antifeedent, 10 and insecticidal activities. 11 The investigation of structure-activity relationships for 2-arylbenzo[b]furan substituents is still attractive due to a variety of biological activities.…”

Facile Preparation of 2-Arylbenzo[b]furan Molecules and Their Anti-inflammatory Effects

“…1 Many 2-arylbenzo[b]furan derivatives are well-known to exhibit broad range of biological activities including anticancer, 2 antiproliferative, 3 anti-inflammatory, 4 antiviral, 5 antifungal, 6 immunosuppressive, 7 antiplatelet, 8 antioxidative, 9 antifeedent, 10 and insecticidal activities. 11 The investigation of structure-activity relationships for 2-arylbenzo[b]furan substituents is still attractive due to variety of biological activities.…”