Synthesis, antitumor and antibacterial activities of cordycepin derivatives.

Twelve novel cordycepin derivatives were designed and synthesized with modification at positions of 2', 5'-hydroxyl and N6 amino groups of cordycepin. The results showed that the inhibitory activities of 3, 4b, 6c and 6d on A549 were comparable to the positive control gefitinib, and the inhibitory activity of 6a on A549 was better than that of gefitinib. Also, the inhibitory activities of twelve cordycepin derivatives against E. coli 1924, S. aureus 4220 and S. mutans 3289 were studied. Among them, 4b showed certain inhibitory on S. mutans 3289, while 6b showed certain inhibition on S. aureus 4220.

Erythrocyte-Like Mesoporous PDA@CeO2 Nanozyme with Dual Drugs for Periodontitis Treatment.

Periodontitis is a chronic oral inflammatory disease with the characteristic of excess oxidative stress in the inflammatory site, dramatically decreasing the quality of life. Studies show that nanozymes can be ideal candidates for ROS scavenging in periodontitis. Here, we design a multipath anti-inflammatory mesoporous polydopamine@cerium oxide nanobowl (mPDA@CeO2 NB) with multienzyme mimicking properties, which combines the advantages of both CeO2 NP and mPDA NB for synergistically eliminating reactive oxygen species (ROS), including hydroxyl radical (•OH), hydrogen peroxide (H2O2), and superoxide (O2•-). Besides, the erythrocyte-like structure of mNBs makes them a facility for cell uptake, and the mesopores can load both hydrophobic and hydrophilic drugs for combined anti-inflammatory therapy. In vitro and in vivo experiments prove that the combination of CeO2 and mPDA can synergistically achieve multiple complementary ROS eliminations and suppression of ROS-induced inflammation. Moreover, the ROS regulation plus anti-inflammatory drugs in one mPDA@CeO2 NB prevents the progression of periodontitis in a mouse model. Therefore, the design of mPDA@CeO2 NB with these excellent properties provides a therapeutic strategy for inflammatory diseases.

Application of enhanced recovery after surgery care protocol in the perioperative care of patients undergoing lumbar fusion and internal fixation.

BACKGROUND: To explore the effects and deficiencies of the enhanced recovery after surgery (ERAS) care protocol on patients undergoing lumbar fusion and internal fixation in perioperative care. METHODS: A total of 166 patients with lumbar fusion and internal fixation were collected and divided into two groups, among which 86 patients received ERAS care protocol were attributed into ERAS group, while the other 80 patients received traditional perioperative care protocol were assigned to control group. Then, the degree of pain, self-care ability and the degree of recovery were assessed using the visual analogue scale (VAS), Barthel index (BI) rating scale and the Sino-version Oswestry Disability Index (ODI) questionnaire, respectively. Moreover, further analysis was performed based on patients' different age, gender, body mass index (BMI) and education of patients in ERAS group. RESULTS: The hospitalization time and the incidence of complication in the ERAS group were obviously lower than those in control group (both, P < 0.05). There was no significant difference in hospitalization expenses between the two groups (P > 0.05). The BI score of the ERAS group was higher than that of the control group (P < 0.05), and the percentage of ODI score in ERAS group was significantly downregulated in comparison with that in control group (P < 0.05). Intra-group analysis in ERAS showed that, compared with older patients, younger patients had higher BI scores (P < 0.05) and lower ODI scores (P < 0.05); meanwhile, overweight patients had lower BI scores (P < 0.05), and the ODI score decreased with the increase in education level of the patients. CONCLUSIONS: ERAS care protocol can significantly shorten the hospitalization time and reduce the occurrence of postoperative complications of patients, significantly enhance the self-care ability of patients after discharge and promote the rapid recovery of patients after surgery.

Two new quinones and six additional metabolites with potential anti-inflammatory activities from the roots of Juglans mandshurica.

Two new quinones, 4-(5-hydroxy-1,4-dioxo-1,4-dihydronaphtha-len-3-ylamino)-butyric acid methyl ester (compound 1) and 1,3-dimethoxycarbonyl-8-hydroxy-9,10-anthraquinone (2), and six known compounds (3-8) were isolated from the roots of Juglans mandshurica Maxim., a member of the Juglandaceae family. The chemical structures of the compounds were elucidated by nuclear magnetic resonance spectroscopy and compared with data from the literature. The isolated compounds were evaluated for their ability to inhibit the production of nitric oxide, tumour necrosis factor-α, and interleukin-6 by the mouse macrophage RAW 264.7 cell line after lipopolysaccharide stimulation in vitro. We found that compounds 1-4 exhibited potent anti-inflammatory effects, as indicated by suppression of lipopolysaccharide-stimulated nitric oxide and cytokine production with 50% inhibitory concentrations between 20.09 µM and 27.63 µM. These results identify two novel quinones from J. mandshurica with potential utility as anti-inflammatory compounds.

A new triterpenoid and other constituents with cytotoxic activity from the roots of Sanguisorba officinalis L.

Sanguisorba officinalis L. is a traditional herbal plant that belongs to the genus Sanguisorba and the family Rosaceae. A new ursane-type triterpenoid, 3-oxo-urs-11, 13(18)-dien-19, 28-olide (1), two known ursane-type triterpenoids (3 - 4) and three known oleanane-type triterpenoids (2, 5 - 6) were isolated from the roots of S. officinalis by silica gel column and MPLC. Their structures were identified by interpretation of spectroscopic data (1 D NMR, 2 D NMR, HR-ESI-MS) and comparison with those reported in the literature. Compound 2 was isolated from the Rosaceae family, compounds 3-5 were obtained from the genus Sanguisorba, and compound 6 was obtained from the S. officinalis for the first time. Additionally, all of the isolated compounds were evaluated for their cytotoxic activity against three human cancer cells. Compound 3 showed better cytotoxic activity against A549, HeLa, SK-Hep1 cells than the other compounds with IC50 values of 48.58 ± 1.88, 47.84 ± 2.01, 42.31 ± 2.43 µM, respectively.