Inhibition of the enzymatic activity of prostate‐specific antigen by boric acid and 3‐nitrophenyl boronic acid

Gallardo-Williams, Maria T.; Maronpot, Robert R.; Wine, Robert N.; Brunssen, Susan; Chapin, Robert E.

doi:10.1002/pros.10166

Cited by 62 publications

(43 citation statements)

References 35 publications

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“…Specific interest in selenium as a chemopreventive agent for prostate cancer has arisen recently [41]. Lastly, PSA activity is inhibited in vitro by boron and boronated compounds [26].…”

Section: Discussionmentioning

confidence: 99%

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Thiophilic-interaction chromatography of enzymatically active tissue prostate-specific antigen (T-PSA) and its modulation by zinc ions

Babu

Vijayalakshmi

Smith

et al. 2008

Journal of Chromatography B

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Prostate-specific antigen (PSA) is a serine protease secreted both by normal prostate glandular epithelia cells and prostate cancer cells. We explored "thiophilic-interaction chromatography" (TIC) to isolate tissue prostate-specific antigen (T-PSA) from fresh human prostate cancer tissue harvested by radical prostatectomy for the purpose to characterize T-PSA for its enzymatic activity and sensitivity to zinc ions. We have shown, for the first time, that T-PSA has strong affinity for the thiophilic gel (T-gel). The average recovery of T-PSA from T-gel is over 87%. The presence of PSA in the column eluate was confirmed by ELISA and SDS/PAGE. Western blot developed with monoclonal antibody to PSA revealed that T-PSA was predominantly in the "free" form having a molecular weight of 33kDA. Furthermore, T-PSA was found to be enzymatically active. T-PSA was found to be less enzymatically active as compared to seminal plasma PSA. The inhibition of enzymatic activity of both f-PSA and T PSA over a wide range of concentrations of Zn 2+ ions (10 nM to 50 μM) was comparable. In contrast, the enzymatic activity of chymotrypsin, another serineprotease, was affected differently. At higher concentrations of Zn 2+ (10 μM and higher) the enzymatic activity of chymotrypsin was inhibited, whereas, at lower concentrations of Zn 2+ (5 μM and lower), the enzymatic activity was enhanced.

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“…Specific interest in selenium as a chemopreventive agent for prostate cancer has arisen recently [41]. Lastly, PSA activity is inhibited in vitro by boron and boronated compounds [26].…”

Section: Discussionmentioning

confidence: 99%

“…The blank was prepared containing the substrate in assay buffer. The details of the procedure are described elsewhere [18,26].…”

Section: Enzymatic Activity Of Psamentioning

confidence: 99%

Thiophilic-interaction chromatography of enzymatically active tissue prostate-specific antigen (T-PSA) and its modulation by zinc ions

Babu

Vijayalakshmi

Smith

et al. 2008

Journal of Chromatography B

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“…Serine proteases are reversibly inhibited by simple and substituted boric acid compounds (Hunt and Idso, 1999). Barranco and Eckhert (2004) and Gallardo-Williams et al (2003) reported that boric acid inhibits human prostate cancer cell proliferation.…”

Section: Introductionmentioning

confidence: 99%

Effects of dietary boron on cervical cytopathology and on micronucleus frequency in exfoliated buccal cells

Korkmaz

Uzgören

Bakırdere

et al. 2007

Environmental Toxicology

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Recent evidence indicates that boron and borates may have anticarcinogenic properties. In this study, we have investigated the incidence of adverse cytological findings in cervical smears and the micronucleus (MN) frequency in women living in boron-rich and boron-poor regions. Cervical smears were prepared from 1059 women with low socioeconomic status; 472 of the women lived in relatively boronrich rural areas, while 587 lived in relatively boron-poor regions. The average and standard deviation values for the age of the women screened with the cervical Pap smear test were 41.55 6 8.38. The mean dietary intake of boron was 8.41 mg/day for women from the boron-rich regions, and 1.26 mg/day for women living in the boron-poor regions (P < 0.0001). Women from the boron-rich regions had no cytopathological indications of cervical cancer, while there were cytopathological findings for 15 women from the boronpoor areas ( 2 ¼ 10.473, P < 0.05). Sixty women, 30 from each region, were chosen for evaluating MN frequencies in exfoliated buccal cells. MN frequencies for women from the boron-rich and boron-poor regions were not significantly different (t ¼ À0.294, P > 0.05). Also, there were no significant correlations between age and MN frequency for women from both the boron-rich (r ¼ 0.133, P ¼ 0.48, P > 0.05) and boron-poor (r ¼ À0.033, P ¼ 0.861, P > 0.05) regions. The results suggest that ingestion of boron in the drinking water decreases the incidence of cervical cancer-related histopathological findings. There was no correlation between the pathological findings from the cervical smears and buccal cell MN frequency suggesting that the two study populations were exposed equally to gentotoxic agents. Nonetheless, cervical cancer-related histopathological findings should be validated by other researchers. # 2007 Wiley Periodicals, Inc. Environ Toxicol 22: 17-25, 2007.

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“…Treatment of nude mice, injected with androgen-sensitive LNCaP prostate cancer cells, with BA caused a reduction in tumour growth of 25 -38%, along with a reduction in plasma PSA levels of 88% (Gallardo-Williams et al, 2004). BA inhibits the activity of serine proteases, including prostate-specific antigen (PSA), presumably by binding to its active site (Bone et al, 1987;Gallardo-Williams et al, 2003). In culture, BA has been shown to inhibit the proliferation of LNCaP and the androgen-independent prostate cancer cell lines DU-145 and PC-3, in a dose-dependent manner (Barranco and Eckhert, 2004).…”

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confidence: 99%

Cellular changes in boric acid-treated DU-145 prostate cancer cells

Barranco

Eckhert

2006

Br J Cancer

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Epidemiological, animal, and cell culture studies have identified boron as a chemopreventative agent in prostate cancer. The present objective was to identify boron-induced changes in the DU-145 human prostate cancer cell line. We show that prolonged exposure to pharmacologically-relevant levels of boric acid, the naturally occurring form of boron circulating in human plasma, induces the following morphological changes in cells: increases in granularity and intracellular vesicle content, enhanced cell spreading and decreased cell volume. Documented increases in b-galactosidase activity suggest that boric acid induces conversion to a senescentlike cellular phenotype. Boric acid also causes a dose-dependent reduction in cyclins A -E, as well as MAPK proteins, suggesting their contribution to proliferative inhibition. Furthermore, treated cells display reduced adhesion, migration and invasion potential, along with F-actin changes indicative of reduced metastatic potential. Finally, the observation of media acidosis in treated cells correlated with an accumulation of lysosome-associated membrane protein type 2 (LAMP-2)-negative acidic compartments. The challenge of future studies will be to identify the underlying mechanism responsible for the observed cellular responses to this natural blood constituent.

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Inhibition of the enzymatic activity of prostate‐specific antigen by boric acid and 3‐nitrophenyl boronic acid

Cited by 62 publications

References 35 publications

Thiophilic-interaction chromatography of enzymatically active tissue prostate-specific antigen (T-PSA) and its modulation by zinc ions

Thiophilic-interaction chromatography of enzymatically active tissue prostate-specific antigen (T-PSA) and its modulation by zinc ions

Effects of dietary boron on cervical cytopathology and on micronucleus frequency in exfoliated buccal cells

Cellular changes in boric acid-treated DU-145 prostate cancer cells

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