The naphthoquinone 7-methyljuglone (5-hydroxy-7-methyl-1,4-naphthoquinone) has previously been isolated and identified as an active component of root extracts of Euclea natalensis which displays antitubercular activity. Herein, a series of synthetic and plantderived naphthoquinone derivates of the 7-methyljuglone scaffold have been prepared and evaluated for antibacterial activity against Mycobacterium tuberculosis. Several of these compounds have been shown to operate as subversive substrates with mycothiol disulfide reductase. The absence of a direct correlation between antitubercular activity and subversive substrate efficiency with mycothiol disulfide reductase, might be a consequence of their non-specific reactivity with multiple biological targets (e.g. other disulfide reductases).
openUP (December 2007)
Graphical abstractArticle Outline
In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis, a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected human cancer lines. These compounds were screened in vitro for anticancer activity on MCF-7, HeLa, SNO and DU145 human cancer cell lines by MTT assay. Most of them exhibited significant toxicity on cancer cell lines with lower IC 50 values. The most potent derivative (19) exhibited the toxicity on HeLa and DU145 cell lines with IC 50 value of 5.3 and 6.8 µM followed by compound (5) with IC 50 value of 10.1 and 9.3 µM, respectively. Structureactivity relationship reveals that the fluoro substituents at position C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity.
This study was carried out to determine the cytotoxic effect of seven plant extracts and the isolated compounds - syringin and 4-methoxycinnamyl alcohol - on cancerous and non-cancerous cells. The ethanol extract of Foeniculum vulgare was found to exhibit the most significant toxicity with an IC50 value of 19.97 μg/mL on HeLa cells. Bioassay-guided fractionation led to the isolation of two compounds, syringin (1) and 4-methoxycinnamyl alcohol (2). Both compounds showed toxicity against MCF-7, HeLa and DU145 cancer cell line. The results showed that compound 2 showed high toxicity against all the cancer cell lines with IC50 values of 14.24, 7.82 and 22.10 μg/mL, respectively. 4-Methoxycinnamyl alcohol also showed no apoptotic effect in cell cycle analysis after 48 h at a concentration of 10 μg/mL. However, DNA fragmentation study revealed that necrosis took place at a concentration of 10 μg/mL after 48 h exposure.
This paper describes appropriate project selection criteria and gate review-point criteria for government agencies that fund technology innovation projects in South Africa. Data was gathered via a Delphi survey i n w h i c h seven expert respondents participated. The most significant project selection criteria and relevant gate reviewing criteria were established. The proposed basic framework consists of fourteen selection criteria, their associated weights, and forty relevant gate reviewing criteria. Commercial risk and feasibility was considered the most important criterion, followed by the team's skills and competence in second place. The use of these criteria when considering investment in technology innovation projects could improve the likelihood of commercial success.
OPSOMMINGHierdie artikel beskryf, vir staatsinstansies wat projekte vir tegnologiese innovasie in Suid Afrika befonds, toepaslike kriteria vir die seleksie van projekte en vir oorsig by hersieningspunte aan die einde van projek fases. Data is ingewin deur middel van ʼn Delphiopname waaraan sewe deskundige respondente deelgeneem het. Die mees beduidende kriteria vir seleksie en oorsig is bepaal. Die voorgestelde raamwerk bestaan uit veertien seleksie-kriteria, relatiewe gewigte vir elk, en veertig kriteria vir hersiening by oorsigpunte. Kommersiële risiko en doenbaarheid word beskou as die belangrikste kriterium, wat gevolg word deur die span se vaardigheid in die tweede plek. Die gebruik van hierdie kriteria wanneer investering in projekte vir tegnologiese innovasie oorweeg word, kan die waarskynlikheid van kommersiële sukses verhoog.
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