Synthesis, physicochemical properties and antimicrobial evaluation of new (E)-chalcones.

In a wide search program towards new and efficient antimicrobial agents, a series of 40 substituted chalcones have been synthesized and tested for their in vitro antibacterial and antifungal activities. The structures of these compounds have been investigated by nuclear magnetic resonance spectroscopy and mass spectrometry. Among the (E)-4-aminoalkylthiochalcones and (E)-4-aminoalkoxychalcones tested, compounds 7, 10, 11, 30 and 31 have exhibited good antibacterial property against Staphylococcus aureus, Enterococcus faecalis and Bacillus subtilis.

Short and long-term physiological responses of male and female rats to two dietary levels of pre-gelatinized maca (lepidium peruvianum chacon).

OBJECTIVE: The aim of this study is to identify physiological responses of male and female rats to either a short- or long-term administration of two doses of Maca (Lepidium peruvianum) and observe relationships which may exist between groups of hormones and effects mediated by them. DESIGN: The effect of pre-gelatinized (extruded) organic Maca powder (Maca-GO) was studied on Sprague-Dowley male and female rats (1:1 ratio) receiving two dietary levels of Maca-GO (0.75 g/kg and 7.5 g/kg body weight) and assessed against control during 28 and 90 day laboratory trials on 30 and 60 rats respectively. Blood morphology, biochemistry (hormones, lipids and minerals) and histology of internal organs were determined. Homogenates of skeletal muscles and bones of rats were also analyzed. RESULTS: Maca-GO has low toxicity (LD=7.5 g/kg) and appears to be safe for short-term and extended use as dietary supplement or as a component of functional dietary and therapeutic preparations. There were different responses of male and female rats to different levels of Maca-GO administered during a short- and a longer-term periodl. When administered at higher dose for extended period of time (90 days), Maca-GO acted as a toner of hormonal processes in adult female rats at increased progesterone and a steady estradiol level, without affecting levels of blood FSH, LH and TSH. CONCLUSIONS: Obtained results justify further clinical research on use of Maca-GO in sportsmen, physically-active people of both sexes and peri-menopausal women to clarify mechanisms underlaying physiological mode of action of Maca-GO validaet in clinical study on humans. Substantial decrease in blood cortisol levels in a short- and longer-term trial and simultaneous tendency to lower blood ACTH, may indicate antidepressive effect of Maca-GO, which together with reduction in body weight, lowering triglycerides in blood plasma and increasing calcium and phosphorus deposition in bone and muscle tissues is worthy consideration in potential application to women at both, pre- and postmenopausal stage.

Therapeutic Effects of Pre-Gelatinized Maca (Lepidium Peruvianum Chacon) used as a Non-Hormonal Alternative to HRT in Perimenopausal Women - Clinical Pilot Study.

BACKGROUND: Roots of cruciferous plant Lepidium peruvianum Chacon cultivated in high plateaus of Andes and known under its common name Maca, have been traditionally-used as an energizing vegetable with therapeutic properties for both men and women. Maca has been recognized by natives of Peru as herbal remedy helping to treat conditions affecting menopausal women. OBJECTIVE: The effects of Pre-Gelatinized Organic Maca (Maca-GO) on quantitative physiological responses and alleviation of symptoms contributing to menopausal discomfort in perimenopausal women was examined. METHODS: IN THIS, FOUR MONTHS, DOUBLE BLIND, CROSSOVER, RANDOMIZED PILOT TRIAL, MONTHLY MEASUREMENTS OF THE FOLLOWING BLOOD SERUM CONSTITUENTS WERE TAKEN: Estrogen (E2), Follicle Stimulating Hormone (FSH), Luteinizing Hormone (LH) and Progesterone (PGS), Cortisol (CT), Adrenocorticotropic Hormone (ACTH), Thyroid Hormones (TSH, T3, T4), minerals (Ca, K, Fe) and lipid profile (Triglicerides, Total Cholesterol, LDL, HDL). In monthly interviews conducted by gynecologist, body weight and blood pressure were registered and Menopausal Index according to Kupperman's was determined. Toxicity of Maca -GO determined on rats showed its safe use at the level of 7.5mg/kg body weight. A group of 20 women (aged 41-50 years), who fulfilled criteria of being in perimenopausal stage (E2 above 40pg/ml and FSH below 30IU/ml), were randomly allocated to two even groups, one receiving for two months Maca-GO and the other Placebo capsules followed by a crossover with treatment change for another two months period. All participants signed informed consent to participate. Two 500mg hard capsules with Maca-GO or Placebo were self-administered by participants twice daily with meals (total 2g/day). RESULTS: Two months administration of Maca-GO significantly alleviated symptoms of discomfort observed in majority of women involved in the study (74%-87%) as assessed by Kupperman's Menopausal index. This was associated with significant increase in E2 and FSH, Progesterone and ACTH levels, and reduction in blood pressure, body weight, Triglycerides and Cholesterol levels. There was a distinctive placebo effect observed at the beginning of the study. CONCLUSIONS: The results showed that in addition to reduction in body weight, blood pressure and increasing serum HDL and Iron, pre-gelatinized Maca-GO may be a valuable non-hormonal plant preparation for balancing levels of hormones (FSH, E2, PG and ACTH) and alleviating negative physiological and psychological symptoms (frequency of hot flushes, incidence in night sweating, interrupted sleep pattern, nervousness, depression and heart palpitations) experienced by women in perimenopausal stage. It appears that Maca-GO may act as a toner of hormonal processes, leading to alleviation of discomfort felt by perimenopausal women, hence, its potential use as non-hormonal alternative to HRT program.

Hormone-Balancing Effect of Pre-Gelatinized Organic Maca (Lepidium peruvianum Chacon): (I) Biochemical and Pharmacodynamic Study on Maca using Clinical Laboratory Model on Ovariectomized Rats.

Ovariectomized rats were used in a model laboratory study to examine biochemical and pharmacodynamic effects of pre-gelatinized organic preparation of Lepidium peruvianum Chacon (Maca-GO). Biochemical and Pharmacodynamic effects of Maca-GO (250 mg Maca-GO per kg body weight (bw) administered by intubation twice daily) were assessed in a 28 day model laboratory study on ovariectomized (by laparoscopy) Wistar rats with pharmacodynamic tests performed at the conclusion of the trial followed by blood collection for morphology and biochemical tests. Toxicity of Maca-GO used in the study was determined in bioassay on mice and rats. Anti-depressive function (Porsolt's test) and anxiolytic sedative and cognitive effects (using elevated-plus maze, locomotor activity and passive avoidance tests) were assessed against control (laparotomized female rats with intact ovaries). In addition to blood morphology, the following blood serum constituents were analyzed: Estrogen (E2), Progesterone (PGS), Cortisol (CT), Adrenocorticotropic Hormone (ACTH), Thyroid Hormones (TSH, T3, and T4), Iron (Fe) and lipid profile (Triglycerides, Total Cholesterol, LDL, HDL). Analytically-determined non-toxic status of Maca-GO was confirmed in bioassays when applied to mice and rats at levels of 0.5 and up to 15mg/kg bw which shows it safe use in humans with the LD50>15 mg/kg bw. Maca-GO showed a distinctive, (P<0.05) antidepressant-like and sedative effect in ovariectomized rats only, while there was no anxiolytic activity nor disturbance of cognitive function observed in both, test and control animals. Observed in this study balancing effect of Maca-GO on sex hormone levels show its potential as a safe preparation for use in correcting physiological symptoms characteristic in postmenopausal stage with an indication of potentially even more value for its use in pre-menopausal women.

Hormone-Balancing Effect of Pre-Gelatinized Organic Maca (Lepidium peruvianum Chacon): (II) Physiological and Symptomatic Responses of Early-Postmenopausal Women to Standardized doses of Maca in Double Blind, Randomized, Placebo-Controlled, Multi-Centre Clinical Study.

This was a double-blind, randomized, placebo-corrected, outpatient, multi-centre (five sites) clinical study, in which a total of 168 Caucasian early-postmenopausal women volunteers (age>49 years) participated after fulfilling the criteria: follicle stimulating hormone (FSH) >30 IU/ml and estrogen (E2) <40 pg/ml levels at admission. They were randomly allocated to Placebo and Pre-Gelatinized Organic Maca (Maca-GO) treatment, according to different monthly treatment sequences scheduled for each site. Two 500 mg vegetable hard gel capsules with Maca-GO or Placebo powder were self-administered twice daily with meals (total 2 g/day) during three (Trial I; n=102) or four (Trial II; n=66) months study periods. At the baseline and follow- up monthly intervals, blood levels of FSH, E2, progesterone (PRG) and lutinizing hormone (LH), as well as serum cholesterol (CHOL), triglycerides (TRG), high- and low density lipoproteins (HDL and LDL) were measured. Menopausal symptoms were assessed according to Greene's Score (GMS) and Kupperman's Index (KMI). Data were analyzed using multivariate technique on blocs of monthly results in one model and Maca versus Placebo contrast in another model. A total of 124 women concluded the study. Maca-GO significantly stimulated production of E2 (P<0.001) with a simultaneous suppression (P<0.05) of blood FSH, increase (P<0.05) in HDL. Maca-GO significantly reduced both frequency and severity of individual menopausal symptoms (hot flushes and night sweating in particular) resulting in significant (P<0.001) alleviation of KMI (from 22 to 10), thus, offering an attractive non-hormonal addition to the choices available to early-postmenopausal women in the form of a natural plant alternative to Hormone Replacement Therapy (HRT) - hence, reducing dependence on hormone therapy programs.

Hormone-Balancing Effect of Pre-Gelatinized Organic Maca (Lepidium peruvianum Chacon): (III) Clinical responses of early-postmenopausal women to Maca in double blind, randomized, Placebo-controlled, crossover configuration, outpatient study.

This is the second, conclusive part of the clinical study on clinical responses of early-postmenopausal women to standardized doses of pre-Gelatinized Organic Maca (Maca-GO). Total of 34 Caucasian women volunteers participated in a double-blind, randomized, four months outpatient crossover configuration Trial. After fulfilling the criteria of being early-postmenopausal: blood Estrogen (E2<40 pg/ml) and Follicle Stimulating Hormone (FSH>30 IU/ml) at admission, they were randomly allocated to Placebo (P) and Maca-GO (M) treatments (2 groups of 11 participants each). Two 500 mg vegetable hard gel capsules with Maca-GO or Placebo powder were self-administered twice daily with meals (total 2 g/day). At admission and follow-up monthly intervals, body mass index (BMI), blood pressure, levels of gonadal, pituitary, thyroid and adrenal hormones, lipids and key minerals were measured. Bone markers were determined after four months M and P use in 12 participants. Menopausal symptoms were assessed according to Greene's Score (GMS) and Kupperman's Index (KMI). Data were analyzed using multivariate technique on blocs of monthly. Results and canonical variate technique was applied to GMS and KMI matrices. Two months application of Maca-GO stimulated (P<0.05) production of E2, suppressed (P<0.05) blood FSH, Thyroid (T3) and Adrenocorticotropic hormones, Cortisol, and BMI, increased (P<0.05) low density lipoproteins, blood Iron and alleviated (P<0.001) menopausal symptoms. Maca-GO noticeably increased bone density markers. In conclusion, Maca-GO applied to early-postmenopausal women (i) acted as a toner of hormonal processes along the Hypothalamus-Pituitary-Ovarian axis, (ii) balanced hormone levels and (iii) relieved symptoms of menopausal discomfort, (hot flushes and night sweating in particular), thus, (iv) exhibited a distinctive function peculiar to adaptogens, providing an alternative non-hormonal plant option to reduce dependence on hormone therapy programs (HRT).

Synthesis and antimicrobial properties of N-substituted derivatives of (E)-4-azachalcones.

Syntheses of 11 new N-bromoalkyl substituted bromides of (E)-4-azachalcone and N-o-(m- and p-) halobenzyl substituted halides of (E)-3'-hydroxy-4-azachalcone of antimicrobial activity are reported. Compounds 3d, 3e, 6b, 6c, and 6e reveal good antimicrobial activity against Staphylococcus aureus and Enterococcus faecalis as well as moderate activity against Escherichia coli and Klebsiella pneumoniae.

Development of occupational safety and health training programs in Poland.

The author describes a Polish-Swedish cooperative venture to develop curricula and training materials in the area of occupational safety and health. The resulting courses, which are consonant with the mandates of the revised Polish Labor Code, have been used to train yearly 1,300 people, including employers, employees, and 300 new trainers. A project to extend such training to workplaces is under way.

Synthesis and antimicrobial activity of (E)-acetoxystilbenes and alpha,alpha'-dibromoacetoxybibenzyls.

The synthesis of 13 new (E)-acetoxystilbenes and alpha,alpha'-dibromoacetoxybibenzyls and their antimicrobial activity are reported. The results of microbiological screening of 17 (E)-stilbenols and (E)-acetoxystilbenes, unknown in the literature, have also been discussed. In particular, coumpounds 1c, 1g, 2a, 3a, 3b, 4a, 6a, 6b showed good antibacterial activity against Staphylococcus aureus and 1c also against Bacillus subtilis.

Antimicrobial activity of some N-alkyl and N-nitrobenzyl substituted halides of (E)-4'-hydroxy-3'-methoxystilbazoles-4.

The synthesis of 11 new N-substituted derivatives of (E)-4'-hydroxy-3'-methoxystilbazoles-4 and their antimicrobial activity are reported. The relationships between structure and antibacterial activity are studied. In particular, compounds 5, 7 and 8 showed good antibacterial activity against Staphylococcus aureus, Streptococcus faecalis and Bacillus subtilis, while compound 6 did so against S. aureus and S. faecalis.

Accommodative facility test results and academic success in Polish second graders.

BACKGROUND: Accommodative infacility, as commonly measured by accommodative flippers, has been implicated as a factor in academic underperformance. This study compares four areas of academics (reading, writing, math and gym) to accommodative flexibility scores. METHODS: Seventy-six elementary school children with a mean age was 8 years, 8 months were tested monocularly and binocularly with traditional accommodative flexibility flipper testing and with a new accommodative flexibility apparatus that allows control of visual acuteness, minification/magnification, and reaction time. These scores were then compared with academic scores using a number of failure criteria. The academic ratings were based on teacher responses for each student. RESULTS: Our data did not show any clear correlation or relationship between evaluations by reading, writing, math, or gym teachers and accommodative flexibility by either the traditional or new testing methods. CONCLUSION: Accommodative function, free of contaminating variables, does not appear to predict academic function any better than the traditional.

Factors affecting the clinical testing of accommodative facility.

A number of variables in the accommodation flipper test are thought to contaminate the results: the time for naming symbols; the manual facility to actually operate the flippers; the minification or magnification of symbol target size by the lenses; saccadic eye movements; and the relationship between the accommodation stimulus and its response. With the exception of the last variable, all undesirable factors have been eliminated in a newly developed modified method of accommodation facility measurement. In this method, double measurement through plano and +/- 2.00 D lenses, is executed. The average time in seconds per one cycle, taking only the accommodation into account for a group of 43 children (age from 7 years 11 months to 9 years 11 months), is 3.7 monocularly and 8.5 binocularly and the average number of cycles per minute in this group is 32.1 and 33.8 monocularly (for the dominant and nondominant eye, respectively) and 22.6 binocularly. These results in sec/cycle do not differ considerably from results received by other authors, if one considers the time necessary for naming the digits, mechanically changing the lenses, saccadic eye movements etc., and even those results given in cycles/minute do not differ either taking the wide ranges of standard deviations into account. However, the method reported here reflects accommodation facility more precisely. Measurements were performed also with the hand held flipper. Comparison of results summarised above and those obtained with a hand held flipper demonstrates that the hand held flipper is not a good device to measure accommodative facility.

Control of the myopic shift in modified Badal optometer.

Refractive error measurements made with the Badal optometer typically register more myopia than is actually present. In this paper we measured the influence of the image size on the endpoint of a Badal optometer's refractive error measurement. The optometer was modified with a camera's zoom lens in such a way that the retinal image size could be controlled. It was found that retinal image size is a major factor in controlling the subjective endpoint. When retinal image size is diminished rather than increased as the target approaches the subject, as is the case under normal circumstances, the perceived endpoint more closely agrees with the actual refractive error.

Synthesis and antimicrobial properties of N-substituted halides of (E)-azastilbenols.

The synthesis of 15 new N-benzyl substituted derivatives of (E)-gamma-azastilbenols-2'(3' and 4') and their antimicrobial activity are reported. In particular, compounds 1a-c, 1h and 2a-b showed good antibacterial activity against Staphlococcus aureus.

Resolving power to narrow and extended light sources and its influence on legibility of the optotypes.

The resolving power of the human visual system has been found to depend on the sizes of the light sources. The sources used in this experiment were two rectangular white fields separated by a vertical black bar. The minimal angle of resolution measured on five subjects decreased by about 10-20 times while the light sources were extended up to the effective range of spatial summation. For larger sources no significant changes of spatial resolution were observed. The experimental data revealed biphasic dependence of the minimal angle of resolution on the sizes of the light sources and permitted estimation of the effective range of spatial summation for 3-9 min arc. This range encompasses the angular diameters of typical optotypes recognized by normal observers (visual acuity greater than 1, optotypes smaller than 5 min arc), therefore we show how the spatial arrangement of the lines and strokes of optotypes determines their legibility.

Resolving power of the human visual system to monochromatic stimuli.

The resolving power in monocular, foveal vision was found to depend on the size of a white light source made of two white rectangles separated by vertical black bar. The question arises whether the wavelength of light influences this dependence. An experiment was done on three subjects using six monochromatic lights the range 450-625 nm, and white light for control measurements. The diagram of the dependence of the minimal angle of resolution on the source size takes the shape of a biphasic curve, i.e. decreasing and constant function. The wavelength was found to have no impact on the curve shape or values. The data points obtained for white light coincide with those for monochromatic lights. The results confirm a thesis that all three colour mechanisms in the human visual system are stimulated and are active in spatial summation processes, but to a degree conditioned by a spectral sensitivity of the particular colour apparatus. It was confirmed that all colour mechanisms have potentially the same acuity but the axial chromatic aberration causes observed reduction of acuity.

Synthesis and antimicrobial properties of N-substituted derivatives of (E)-alpha-(or gamma)-azastilbenols.

The synthesis of 19 new N-substituted derivatives of (E)-alpha and gamma-azastillbenols-2'(3' and 4') and their antimicrobial activity are reported. In particular, compounds 4a-4f and 6a showed good antibacterial activity against Staphylococcus aureus, Streptococcus faecalis, Bacillus subtilis and Escherichia coli.

Synthesis and antimicrobial properties of S-substituted derivatives of 2-thiouracil.

The synthesis of 24 new 2-alkylthio and 2-(E)-N-thioalkyl-4-azachalkonyl substituted derivatives of uracil and their antimicrobial activity are reported. In particularly compounds 6o and 6p showed a good antibacterial activity against Staphylococcus aureus and Streptococcus faecalis.

[Use of the Foucault's test for determining the contrast sensitivity of the visual system]. / Próba zastosowania testu foucaulta do wyznaczania wrazliwosci ukladu wzrokowego na kontrast.

The authors present the thesis that in apperception of the Foucault's test in condition of a threshold contrast only the first harmonic component is decisive; in connection with this one can replace the sinusoidal tests applied for the demarcation of the sensitivity curve of the visual system to contrast by Foucault's test. They point to the eventual possibility--if the influence of the following components would prove to be essential--of using the Foucault's test together with the sinusoidal test in order to make the diagnosis of pathological conditions more selective. The CSF function was designated by means of the sinusoidal and Foucault's tests seen on a monitor screen using the methods of contrast increase. In 8 subjects observing simultaneously one discovered that for the frequencies larger or equal to 1.5 stop-1 one can apply the Foucault's test instead of the sinusoidal test. Below the space frequency of 1.5 stop-1 one observed differences between the values of sensitivity to contrast demarcated by means of both tests; these differences result probably from the influence of the higher harmonics of the Foucault's test on the apperception of the test.