Constituents of the Vietnamese medicinal plant Orthosiphon stamineus

From the MeOH extract of the aerial part of Vietnamese Orthosiphon stamineus, five new isopimarane-type diterpenes [orthosiphols F-J (1-5)] and two new diterpenes [staminols A (6) and B (7)] with a novel carbon-framework, to which we proposed the name "staminane", and three new highly-oxygenated staminane-type diterpenes [staminolactones A (8) and B (9) and norstaminol A (10)1 were isolated. Moreover, staminolactone A (8) is 8,14-secostaminane-type and staminolactone B (9) is 13,14-secostaminane-type, while norstaminol A (10) is 14-norstaminen-type. Together with these new diterpenes, sixteen known compounds were also isolated and identified to be: 7,3',4'-tri-O-methylluteolin (11), eupatorin (12), sinensetin (13), 5-hydroxy-6,7,3',4'-tetramethoxyflavone (14), salvigenin (15), ladanein (16), tetramethylscutellarein (17), 6-hydroxy-5,7,4'-trimethoxyflavone (18), vomifoliol (19), aurantiamide acetate (20), rosmarinic acid (21), caffeic acid (22), oleanolic acid (23), ursolic acid (24), betulinic acid (25), and beta-sitosterol (26). All the isolated compounds were tested for their cytotoxicity towards highly liver metastatic murine colon 26-L5 carcinoma cells, and the new diterpenes, except for 4, and flavonoids (11, 12, 16, 18) showed cytotoxicity with an ED50 value between 10 and 90 microg/ml.     

A new approach to the synthesis of cyclic ethers via the intermolecular allylation of α-acetoxy ethers and ring-closing metathesis

A concise synthesis of the isolaurepinnacin skeleton 6 was achieved via the intermolecular allylation of the α-acetoxy ether 3 followed by ring-closing metathesis. This methodology was successfully applied to the convergent synthesis of the oxocene 15, an advanced synthetic intermediate for the total synthesis of laurencin.     

Infraglottic aspect of canine vocal fold vibration: Effect of increase of mean airflow rate and lengthening of vocal fold

The mucosal upheaval (MU), where the mucosal wave starts and propagates upward, appears only when the vocal fold vibrates. The location of the MU histologically and the effect of changes in mean air flow rate (MFR) and vocal fold length on occurrence of the MU were studied in twelve excised canine larynges. The lower surface of the vocal fold was marked to serve as a landmark for subsequent study. Cricothyroid approximation was performed to lengthen the vocal fold. After taking high-speed pictures or recording stroboscopic images from the tracheal side, a small cut wound was made at the mark. This wound served to compare the position of the MU with the histologically identified location of the mark. The larynx was then sectioned in the frontal plane. Before lengthening the vocal fold, the MU occurred on the area where the lamina propria became thinner and where the muscular layer neared the epithelial layer. After lengthening the vocal fold, the MU actually shifted medially compared with its original position. The subglottic area surrounded by the bilateral MUs became longer and thinner. Whether or not complete glottal closure during a vibratory cycle was achieved did not alter these findings. In contrast, with a fixed vocal fold length the MU appeared more laterally as MFR increased, but, based on the relation with the mark, its location on the vocal fold did not change from its original position before increase of MFR.     

Cytotoxicity of constituents from Mexican propolis against a panel of six different cancer cell lines

The cytotoxicity of 39 compounds, including eighteen flavonoids (flavanones, 1-10; flavones, 11-17; flavanol, 18), sixteen phenolic acid derivatives (aromatic acids, 19-24; aldehyde, 25; esters, 26-34) and five glycerides (35-39), isolated from Mexican propolis, were evaluated against a panel of six different cancer cell lines; murine colon 26-L5 carcinoma, murine B16-BL6 melanoma, murine Lewis lung carcinoma, human lung A549 adenocarcinoma, human cervix HeLa adenocarcinoma and human HT-1080 fibrosarcoma. A phenylpropanoid-substituted flavanol, (2R,3S)-8-[4-phenylprop-2-en-1-one]-4',7-dihydroxy-3',5-dimethoxyflavan-3-ol (18), showed the most potent cytotoxicity against A549 cells (IC50, 6.2 microM) and HT-1080 cells (IC50, 3.9 microM), stronger than those of the clinically used anticancer drug, 5-fluorouracil (IC50, 7.5 microM and 5.4 microM, respectively). Based on the observed results, the structure-activity relationships are discussed.     

Convergent synthesis of the HIJKLM ring system of ciguatoxin CTX3C

The HIJKLM ring system of ciguatoxin CTX3C was synthesized in a convergent manner. The key steps were a conjugate addition/alkylation sequence, spiroacetalization, intramolecular allylation, ring-closing metathesis, and hydrogenation to form the 36-α-methyl substituent.     

Flavour issues for string-motivated heavy scalar spectra with a low gluino mass: the G 2-MSSM case

In recent years it has been learned that scalar superpartner masses and trilinear couplings should both generically be larger than about 20?TeV at the short-distance string scale if our world is described by a compactified string or M-theory with supersymmetry breaking and stabilized moduli (Acharya et?al. in arXiv:1006.3272 [hep-ph], 2010). Here we study implications of this, somewhat generally and also in detail for a particular realization (compactification of M-theory on a G ₂ manifold) where there is significant knowledge of the superpotential and gauge kinetic function, and a light gluino. In a certain sense this yields an ultraviolet completion of minimal flavour violation. Flavour violation stems from off-diagonal and non-universal diagonal elements of scalar mass matrices and trilinear couplings, and from renormalization group running. We also examine stability bounds on the scalar potential. While heavy scalars alone do not guarantee the absence of flavour problems, our studies show that models with heavy scalars and light gluinos can be free from such problems.     

Formal total synthesis of enigmazole A

A stereoselective formal total synthesis of enigmazole A, a marine macrolide isolated from Cinachyrella enigmatica, is described. Lewis acid mediated intramolecular allylation of an α-acetoxy ether, prepared from alcohol and carboxylic acid fragments was carried out to construct the methylene THP ring with high stereoselectivity. The late-stage macrolactonization of the corresponding seco-acid provided a known synthetic intermediate of enigmazole A.     

Measurements of high pT light fragments at CM 90° in 800 A MEV C + C collisions

The spectra of high-p_T fragments have been measured at CM 90° in 800 A MeV C + C collisions for p_T up to 1.8 GeV/c (proton), 2.5 GeV/c (deuteron) and 2.8 GeV/c (triton) at the Bevalac. Invariant cross sections were measured down to eight orders of magnitude lower than those for production of low momentum protons. The proton spectrum shows a significant deviation from the Boltzmann shape in the high-energy region. The spectra of deuterons and tritons are explained well by, respectively, squaring and cubing the observed proton spectra.     

(6Li,d) reactions on 24Mg and 26Mg at 73 MeV

The ^{24, 26}Mg(⁶Li, d)^{28, 30}Si reactions have been studied at 73 MeV bombarding energy. The angular distributions were analyzed with exact finite-range distorted wave Born approximation calculations assuming a direct α-cluster transfer. Extracted spectroscopic strengths leading to low-lying levels of ²⁸Si and relative spectroscopic strengths between transitions to ²⁸Si and ³⁰Si ground states are consistent with those previously obtained by several α-transfer reactions. Many strongly populated levels have been observed at E_x ? 10 MeV for ²⁸Si. A marked similarity was found between the deuteron spectrum and the ²⁴Mg(α, α)²⁴Mg excitation function in this excitation energy region. A brief comparison of the present α-transfer results with previous two-nucleon transfer data leading to ^28,30Si is also presented.