Sulfemodin 8-O-beta-D-glucoside,a new sulfated anthraquinone glycoside,and antioxidant phenolic compounds from Rheum emodi

A sulfated emodin glucoside, emodin 8-O-beta-D-glucopyranosyl-6-O-sulfate (1), was isolated from the roots of Rheum emodi in an investigation of the active constituents of this Nepalese medicinal plant, and its structure was determined by spectroscopic and chemical methods. Additionally, two rare auronols, carpusin (2) and maesopsin (3), besides other anthraquinones and phenolics, were isolated and identified. Compounds 2 and 3 showed significant antioxidant activity in the DPPH assay, while chrysophanol, physcion, and emodin and their 8-O-glucosides were found to be inactive.     

Gestational diabetes screening in a private, midwestern American population

This prospective investigation was undertaken to compare the value of routine versus selective diabetes screening in a group of predominantly middle-class, healthy, Caucasian pregnant women. Two thousand consecutively chosen persons were divided into two groups: those to undergo routine screening between 24 and 28 weeks' gestation and those to be tested selectively in the presence of standard risk factors. The two groups of patients were otherwise similar. The method of screening involved a 50 gm oral glucose challenge, followed by a 3-hour glucose test if necessary. The incidence of gestational onset diabetes in the selectively screened group (19/453, 4.2%) was twice that in the routinely screened group (21/1000, 2.1%). Evidence of glucose intolerance without a risk factor was found in only one case (1/1000, 0.1%) in the routinely screened group. This assessment of our clinical practice has allowed us to safely eliminate the need for diabetes screening in more than half of our private patients, which will reduce office time, patient inconvenience, and expense.     

TRPC6

TRPC6 is a Ca(2+)-permeable non-selective cation channel expressed in brain, smooth muscle containing tissues and kidney, as well as in immune and blood cells. Channel homomers heterologously expressed have a characteristic doubly rectifying current-voltage relationship and are six times more permeable for Ca2+ than for Na+. In smooth muscle tissues, however, Na+ influx and activation of voltage-gated calcium channels by membrane depolarization rather than Ca2+ elevation by TRPC6 channels is the driving force for contraction. TRPC6 channels are directly activated by the second messenger diacylglycerol (DAG) and regulated by specific tyrosine or serine phosphorylation. Extracellular Ca2+ has inhibitory effects, while Ca2+/calmodulin acting from the intracellular side has potentiator effects on channel activity. Given its specific expression, TRPC6 is likely to play a number of physiological roles. Studies with TRPC6(-/-) mice suggest a role for the channel in the regulation of vascular and pulmonary smooth muscle contraction. TRPC6 was identified as an essential component of the slit diaphragm architecture of kidney podocytes. Other functions in immune and blood cells, as well as in brain and in smooth muscle-containing tissues such as stomach, colon and myometrium, remain elusive.     

Beitrag zur carcinogenen Wirkung von Dibenzopyrenen

Zusammenfassung Nach Synthese und/order sorgfältiger Reinigung wurden neun hexacyclische Verbindungen im Pinselungstest im Vergleich zu Benzo(a)-pyren an der Maus auf ihre krebserzeugende und Tumor-Initiatowirkung geprüft. Es ergaben sich folgende Reihen der Aktivitäten: Als Vollcarcinogen sind Benzo(a) pyren (X) stark aktiv; dibenzo(a, h)pyren (IV), Dibenzo(a, l)pyren(I), und Dibenzo(a, i)pyren (V) aktiv; Dibenzo(a, e)pyren (II) und Indeno(1,2,3-cd)pyren (IX) schwach aktiv und Dibenzo(a, l)pyren (III), Dibenzo (cd-jk)pyren (VI), Benzo(ghi)perylen (VII) und Naphtho(2,3-e)pyren (VIII) inaktiv. Im Tumor-Initiatortest, in dem 2,5% Grotonöl als Promotor verwendet wurde, waren stark aktiv die Kohlenwasserstoffe X und IV; aktiv I und V; schwach aktiv II, VIII und IX; inaktiv die Verbindungen III, VI und VII. Die Ergebnisse der biologischen Versuche werden mit Berechnungen und Testen der Aktivitäten dieser polycyclischen Kohlenwasserstoffe verglichen. Da viele dieser Verbindungen in der Umwelt des Menschen vorkommen, sind die Beobachtungen von akademischer wie auch praktischer Bedeutung.

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Summary Nine synthesized and/or highly purified hexacyclic aromatic hydrocarbons were tested for carcinogenicity and tumor-initiating potency on mouse skin. Their activities were compared with those of benzo(a)pyrene. The following order of activities was found: As complete carcinogen benzo(a)pyrene (X) rates strongly active; dibenzo(e, h)pyren (IV), dibenzo(a, l)pyrene (I) and dibenzo(a, i)pyrene (V) were active; dibenzo(a, e)pyrene (II) and indeno(1,2,3-cd)pyrene (IX) were weakly active and dibenzo(e, l)pyrene (III), dibenzo(cd-jk)pyrene (VI); benzo(ghi)perylene (VII) and naphtho(2,3-e)pyrene (VIII) were inactive. The initiator test for the polycyclic hydrocarbons made use of 2,5% Croton oil as promoter. The initiating activity was found to be strongly active for the polycyclic hydrocarbons X and IX; active for I and V, weakly active for II, VIII and IX and inactive for III, VI and VII. The results of the mouse skin tests are compared with data resulting from theoretical considerations and with predictions of carcinogenicity on the basis of physico-chemical reactions for these polynuclear aromatic hydrocarbons. Since many of these compounds occur in man's environment, these investigations are not only of academic but also of practical importance.

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Herrn Professor Dr. K. H. Bauer zum 75. Geburtstag gewidmet.     

Allgemeines

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Statistik

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Morphologie

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Metastasen

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Gehirn,Nerven

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