Synthesis of a new water-soluble hexacarboxylated tribenzotriquinacene derivative and its competitive host-guest interaction for drug delivery.

A new water-soluble hexacarboxylated tribenzotriquinacene derivative (TBTQ-CB6) was synthesized and used as a supramolecular drug carrier to load the model anticancer drugs dimethyl viologen (MV) and doxorubicin (DOX) via host-guest interactions. The drugs could be effectively released by spermine (SM), a molecule overexpressed in cancer cells, through host-guest competitive substitution since TBTQ-CB6 has a stronger binding affinity toward SM than MV and DOX. The host-guest interactions of the complexes of TBTQ-CB6 with MV, DOX and SM were investigated by NMR spectroscopy and fluorescence spectroscopy. The association stoichiometry of the complexes of TBTQ-CB6 with MV, DOX, and SM was found to be 1:1 with association constants of K a = (7.67 ± 0.34) × 104 M-1, K a = (6.81 ± 0.33) × 104 M-1, and K a = (5.09 ± 0.98) × 105 M-1, respectively. The competitive substitution process was visualized by NMR titration. This novel TBTQ-based host-guest drug delivery system may have potential use in supramolecular chemotherapy.

Water-soluble host-guest complexes between fullerenes and a sugar-functionalized tribenzotriquinacene assembling to microspheres.

A sugar-functionalized water-soluble tribenzotriquinacene derivative bearing six glucose residues, TBTQ-(OG) 6 , was synthesized and its interaction with C60 and C70-fullerene in co-organic solvents and aqueous solution was investigated by fluorescence spectroscopy and ultraviolet-visible spectroscopy. The association stoichiometry of the complexes TBTQ-(OG) 6 with C60 and TBTQ-(OG) 6 with C70 was found to be 1:1 with binding constants of K a = (1.50 ± 0.10) × 105 M-1 and K a = (2.20 ± 0.16) × 105 M-1, respectively. The binding affinity between TBTQ-(OG) 6 and C60 was further verified by Raman spectroscopy. The geometry of the complex of TBTQ-(OG) 6 with C60 deduced from DFT calculations indicates that the driving force of the complexation is mainly due to the hydrophobic effect and to host-guest π-π interactions. Hydrophobic surface simulations showed that TBTQ-(OG) 6 and C60 forms an amphiphilic supramolecular host-guest complex, which further assembles to microspheres with diameters of 0.3-3.5 µm, as determined by scanning electron microscopy.

New eudesmane sesquiterpenes from Alpinia oxyphylla and determination of their inhibitory effects on microglia.

The fruits of Alpinia oxyphylla are used as healthcare products for the protection on neurons and prevention of dementia. Two new noreudesmane sesquiterpenoids, (5R,7S,10S)-5-hydroxy-13-noreudesma-3-en-2,11-dione (1) and (10R)-13-noreudesma-4,6-dien-3,11-dione (2), and a new eudesmane sesquiterpenoid, (5S,8R,10R)-2-oxoeudesma-3,7(11)-dien-12,8-olide (3), as well as 12 known sesquiterpenoids, were isolated from the fruits of A. oxyphylla. The structures of the new compounds (1-3) were elucidated on the basis of spectroscopic data and circular dichroism experiments. All isolates were evaluated their neuroprotective potential by inhibitory assay on nitric oxide (NO) and tumor necrosis factor-α (TNF-α) production in lipopolysaccharide (LPS)-induced mouse microglia BV-2 cells.

Measurement Properties of the Simplified Chinese Version of the Lumbar Spine Instability Questionnaire for Patients With Low Back Pain in Mainland China.

STUDY DESIGN: A prospective study. OBJECTIVE: To develop a simplified Chinese version of Lumbar Spine Instability Questionnaire (SC-LSIQ) and test its measurement properties. SUMMARY OF BACKGROUND DATA: The LSIQ has been translated into several languages. Different versions of LSIQ have proved good reliability and validity in evaluating patients with low back pain. However, there is no simplified Chinese version of LSIQ (SC-LSIQ). MATERIALS AND METHODS: The SC-LSIQ has been translated into a simplified Chinese version according to a standard procedure. A total of 155 patients with low back pain completed the SC-LSIQ along with Oswestry Disability Index, Roland-Morris disability questionnaire, Tampa Scale for Kinesiophobia, and visual analogue scale (VAS). The internal consistency, test-retest reliability, and validity of SC-LSIQ were then calculated to evaluate the measurement properties of SC-LSIQ. RESULTS: The results of SC-LSIQ demonstrated that there was no ceiling or floor effect detected. The Cronbach α coefficient of 0.911 determined a well internal consistency. The intraclass correlation coefficient (0.98) presented an excellent reliability of SC-LSIQ. The Pearson correlation coefficient (r) showed that the SC-LSIQ was excellent correlated to Oswestry Disability Index (r=0.809), Roland-Morris disability questionnaire (r=0.870), and Tampa Scale for Kinesiophobia (r=0.945,). Furthermore, it moderately correlated to visual analogue scale (r=0.586). CONCLUSION: The SC-LSIQ features good internal consistency, reliability, and validity for evaluating Chinese patients with LBP. Results suggest that the SC-LSIQ can be appropriately applied to patients with LBP in routine clinical practice.