Interaction effect between the receptor for advanced glycation end products (RAGE) and high-mobility group box-1 (HMGB-1) for the migration of a squamous cell carcinoma cell line.

AIMS AND BACKGROUND: The receptor for advanced glycation end products (RAGE) is a multiligand cell surface receptor of the immunoglobulin superfamily and a newly recognized invasion-related gene. High mobility group box-1 (HMGB-1) is a 30-kD protein binding to RAGE and acting as a transcription-factor-like protein that regulates the expression of several genes. In this study, the interaction effect between RAGE and HMGB-1 on the migration of SCC7 cells was investigated along with the inhibitory effect of the drug nifedipine on this interaction effect. METHODS AND STUDY DESIGN: Ten surgical specimens from patients with squamous cell carcinoma (SCC) of the head and neck and a SCC7 cell line were stained using immunohistochemical and immunocytochemical methods. Reverse transcriptase-polymerase chain reaction (RT-PCR) was used to detect RAGE expression in SCC7 cells; Western blot analysis was used to detect HMGB-1 expression in SCC7 cells. An in vitro migration assay (Boyden chamber migration assay) was used for evaluating the interaction effect between RAGE and HMGB-1 on the migration of SCC7 cells. HMGB-1 and various concentrations of nifedipine were tested for their effect on SCC7 cell migration with in vitro migration assays. RESULTS AND CONCLUSIONS: RAGE and HMGB-1 were expressed in almost all human head and neck SCC tissues and in SCC7 cells as detected by immunostaining. The migration assay showed that the interaction between RAGE and HMGB-1 increased SCC7 migration activity depending on the level of HMGB-1, and nifedipine inhibited the interaction effect between RAGE and HMGB-1 on SCC7 cells in a dose-dependent manner. The interaction between RAGE and HMGB-1 could be closely associated with metastasis of SCC of the head and neck. Nifedipine may have an inhibitory effect on tumor metastasis.

Efficacy of spray formulations containing binary mixtures of clove and eucalyptus oils against susceptible and pyrethroid/ malathion-resistant head lice (Anoplura: Pediculidae).

The control efficacy of clove, Eugenia caryophyllata, and eucalyptus, Eucalyptus globulus, essential oils and 15 formulations containing these essential oils alone (8, 12, and 15% sprays) and their binary mixtures (7:3, 5:5, and 3:7 by weight) against adult females of insecticide-susceptible KR-HL and dual malathion- and permethrin-resistant BR-HL strains of head louse, Pediculus humanus capitis (De Geer), was examined by using contact plus fumigant and human hair wig (placed over the head of mannequin) mortality bioassays. In contact plus fumigant mortality bioassay, essential oils from eucalyptus (0.225 mg/cm2) and clove (1.149 mg/cm2) were less effective than either d-phenothrin (0.0029 mg/cm2) or pyrethrum (0.0025 mg/cm2) based on 6-h median lethal concentration values. However, the efficacies of eucalyptus and clove oils were almost identical against females fromn both strains, despite high levels of resistance of the BR-HL females to d-phenothrin (resistance ratio, 667) and pyrethrum (resistance ratio, 754). In human hair wig mortality bioassay, eucalyptus oil spray treatment gave better control efficacy than either spray treatment with clove oil alone or their binary mixtures. Thus, eucalyptus applied as 8% sprays (15 or 20 ml) appears to provide effective protection against pediculosis even to insecticide-resistant head louse populations. Once the safety issues resolved, covering the treated hair and scalp with bath shower cap or hat would ensure the fumigant action of the essential oil.

Markedly enhanced recyclability of osmium catalyst in asymmetric dihydroxylation reactions by using macroporous resins bearing both residual vinyl groups and quaternary ammonium moieties.

Markedly enhanced recyclability of osmium catalyst in asymmetric dihydroxylation has been achieved by using osmylated macroporous resins bearing both residual vinyl groups and quaternary ammonium moiety.

Electrophilic aromatic addition reaction: electrophilic attack at an aromatic H substituent position.

[reaction: see text] We report and propose a mechanism for an unusual electrophilic aromatic addition reaction (Ad(E)()Ar). During our preparation of 5,7-dibromo-8-methoxyquinaldine as a key intermediate in the synthesis of 7-bromoquinaldine-5,8-dione, direct bromination in either acidic or neutral conditions led only to the formation of 5-bromo-8-methoxyquinaldine. Under basic methanolic conditions, however, we unexpectedly obtained the 5,7-dibromo-8,8-dimethoxy-7,8-dihydroquinaldine adduct 2a. This result not only allows for the functionalization of aromatic compounds via the addition adducts, but also introduces the possibility of an alternate mechanism for electrophilic substitution reactions.

Ovicidal and adulticidal activity of Eucalyptus globulus leaf oil terpenoids against Pediculus humanus capitis (Anoplura: Pediculidae).

The toxic effects of Eucalyptus globulus leaf oil-derived monoterpenoids [1,8-cineole, l-phellandrene, (-)-alpha-pinene, 2-beta-pinene, trans-pinocarveol, gamma-terpinene, and 1-alpha-terpineol] and the known Eucalyptusleaf oil terpenoids (beta-eudesmol and geranyl acetate) on eggs and females of the human head louse, Pediculus humanus capitis, were examined using direct contact and fumigation bioassays and compared with the lethal activity of delta-phenothrin and pyrethrum, two commonly used pediculicides. In a filter paper contact bioassay with female P. h. capitis, the pediculicidal activity was more pronounced with Eucalyptus leaf oil than with either delta-phenothrin or pyrethrum on the basis of LT(50) values (0.125 vs 0.25 mg/cm(2)). 1,8-Cineole was 2.2- and 2.3-fold more toxic than either delta-phenothrin or pyrethrum, respectively. The pediculicidal activities of (-)-alpha-pinene, 2-beta-pinene, and (E)-pinocarveol were comparable to those of delta-phenothrin and pyrethrum. l-Phellandrene, gamma-terpinene, and 1-alpha-terpineol were relatively less active than delta-phenothrin and pyrethrum. beta-Eudesmol and geranyl acetate were ineffective. 1-alpha-Terpineol and (E)-pinocaveol were highly effective at 0.5 and 1.0 mg/cm(2), respectively, against P. h. capitis eggs. At 1.0 mg/cm(2), (-)-alpha-pinene, 2-beta-pinene, and gamma-terpinene exhibited moderate ovicidal activity, whereas little or no ovicidal activity was observed with the other terpenoids and with delta-phenothrin and pyrethrum. In fumigation tests with female P. h. capitis at 0.25 mg/cm(2), 1,8-cineole, (-)-alpha-pinene, (E)-pinocarveol, and 1-alpha-terpineol were more effective in closed cups than in open ones, indicating that the effect of the monoterpenoids was largely due to action in the vapor phase. Neither delta-phenothrin nor pyrethrum exhibited fumigant toxicity. Eucalyptus leaf oil, particularly 1,8-cineole, 1-alpha-terpineol, and (E)-pinocaveol, merits further study as potential pediculicides or lead compounds for the control of P. h. capitis.

Nonselective bromination-selective debromination strategy: selective bromination of unsymmetrical ketones on singly activated carbon against doubly activated carbon.

[reaction: see text] We have found a new synthetic method for the preparation of the alpha-bromoketones that are brominated in the less activated terminal position of unsymmetrical ketones. Brominations in short reaction times (kinetically controlled) provided internally brominated compounds as a major product. However, brominations in longer reaction times (thermodynamically controlled) gave more of the terminally brominated compound through the reversible reaction by Br(2) and produced hydrogen bromide. Several brominated compounds at the terminal position were successfully prepared through the new synthetic route.

Preparation of 7-alkylamino-2-methylquinoline-5,8-diones.

Several novel 7-alkylamino-2-methylquinoline-5,8-diones (2) were synthesized from 2,5-dimethoxyaniline in five steps via the Skraup reaction followed by demethylations, oxidative bromination, amination, and debromination. We have achieved an unusual hydrobromic acid catalyzed debromination reactions of several 6-bromo-7-alkylamino-2-methylquinoline-5,8-diones, giving 7-alkylamino-2-methylquinoline-5,8-diones in good yields.

Is the higher prevalence of benign prostatic hyperplasia related to lower urinary tract symptoms in Korean men due to a high transition zone index?

OBJECTIVE: Asian men generally have smaller prostate gland sizes than their Western counterparts. Nonetheless, the prevalence of lower urinary tract symptoms (LUTS) is similar between native Asian men and men in the Western hemisphere. The purpose of this study was to determine if the enlargement of the transition zone volume (TZV) relative to the overall prostate volume (PV) might account for the prevalence of LUTS among Korean men despite having "smaller" prostates. METHODS: Three hundred and seventy consecutive age-matched men (94 Caucasian, 94 Hispanic, 93 African-American, and 89 Korean) with LUTS were evaluated utilizing the International Prostate Symptom Score (IPSS), peak flow rate (Q(max)), serum PSA and transrectal ultrasound (TRUS). The ratio of TZV to total PV was used to determine the transition zone index (TZI). RESULTS: Mean baseline IPSS and Q(max) were significantly different (p<0.001 and p<0.03) for Korean men (19.9+/-7.6 and 11.3+/-4.2) in comparison to African-American (14.6+/-3.7, 12.6+/-4.1), Caucasian (13.4+/-4.3, 12.5+/-3.8), and Hispanic (13.9+/-3.1, 11.9+/-4.5) men. Regardless of race, TZI correlated with IPSS (r=0.31, p<0.01) and Q(max) (r=0.26, p<0.04). Mean TZI was significantly (p<0.001) higher in Korean and African-American men (0.45+/-0.08 and 0.44+/-0.05, respectively) than Caucasian and Hispanic men (0.39+/-0.03 and 0.38+/-0.02, respectively). CONCLUSIONS: Among age-matched, ethnically diverse men with moderate to severe LUTS, Korean men demonstrated more clinical symptoms and a higher ratio of transition zone enlargement relative to total prostate in comparison to Caucasian, Hispanic, and African-American men. The clinical significance of these findings remains to be determined.