Discovery of dual S-RBD/NRP1-targeting peptides: structure-based virtual screening, synthesis, biological evaluation, and molecular dynamics simulation studies

Article

Author: Shen, Xiaozhou ; Li, Jindong ; Niu, Miaomiao ; Gao, Yi ; Gao, Junyi ; Zou, Yunting ; Hu, Chunfang ; Xia, Yang ; Guo, Ting

Both receptor-binding domain in spike protein (S-RBD) of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and human neuropilin-1 (NRP1) are important in the virus entry, and their concomitant inhibition may become a potential strategy against the SARS-CoV-2 infection. Herein, five novel dual S-RBD/NRP1-targeting peptides with nanomolar binding affinities were identified by structure-based virtual screening. Particularly, RN-4 was found to be the most promising peptide targeting S-RBD (K_d = 7.4 ± 0.5 nM) and NRP1-BD (the b1 domain of NRP1) (K_d = 16.1 ± 1.1 nM) proteins. Further evidence in the pseudovirus infection assay showed that RN-4 can significantly inhibit the SARS-CoV-2 pseudovirus entry into 293 T cells (EC₅₀ = 0.39 ± 0.09 μM) without detectable side effects. These results suggest that RN-4, a novel dual S-RBD/NRP1-targeting agent, holds potential as an effective therapeutic to combat the SARS-CoV-2 infection.

01 Dec 2019·TrialsQ4 · MEDICINE

Effect of acupuncture on insomnia in menopausal women: a study protocol for a randomized controlled trial

Q4 · MEDICINE

ArticleOA

Author: Yin, Xuan ; Lao, Lixing ; Yin, Ping ; Bogachko, Anna ; Liang, Tingting ; Li, Shanshan ; Xu, Shifen

BACKGROUNDThe National Institutes of Health estimates the prevalence of insomnia in menopausal women at 40-50%. Some studies have shown that acupuncture might be effective in treating primary insomnia and insomnia related to depression and stroke. Although there are some programs supporting insomnia during the menopausal transition, there are few randomized controlled trials (RCT) to provide evidence regarding their effectiveness. We design a RCT of suitable sample size to verify the effectiveness of acupuncture in patients with insomnia during the menopausal transition and to form an optimized acupuncture treatment protocol.METHOD/DESIGNIn this randomized, single-site, single-blind, placebo-controlled trial, 84 eligible patients will be recruited and randomly assigned to either the acupuncture group (n = 42) or the sham control group (n = 42) in a 1:1 ratio. Participants will receive a total of 18 treatment sessions for eight consecutive weeks. Treatments will be given three times per week in the first four weeks, twice a week for the next two weeks, and finally once weekly for the final two weeks. Treatment will utilize eight main acupoints (GV20, GV24, GV29, RN6, RN4, SP6, HT7, EX-HN22) and extra two acupoints based on syndrome differentiation. The primary outcome will be assessed using the Pittsburgh Sleep Quality Index (PSQI). The secondary outcomes will be measured by sleep parameters recorded in the Actigraphy (SE, TST, SA), Insomnia Severity Index (ISI), Self-Rating Anxiety Scale (SAS), Self-Rating Depression Scale (SDS), and Menopause Quality of Life (Men-QOL). The primary outcomes will be assessed at baseline, week 4, week 8, and the first and third month after the end of treatment.DISCUSSIONIf the results confirm that acupuncture is effective and safe for the treatment on insomnia in menopausal women, this positive outcome could provide evidence for clinical application.TRIAL REGISTRATIONChinese Clinical Trial Registry, ChiCTR1800018645 . Registered on 10 January 2018.

01 Jan 1975·Folia Pharmacologica Japonica

Influence of alfalfa meal on experimental hyperlipidemia

Article

Author: Yanaura, Saizo ; Sakamoto, Mitsuo

The influence of alfalfa meal on hyperlipidemia induced by dietary cholesterol was examined and changes in serum total cholesterol (TC), triglycerides (TG) and non-esterified fatty acid (NEFA) in rabbits were recorded. Serum lipid levels of groups treated with alfalfa meal (R-1) as well as those not treated (R-2) were found to be elevated. TC of R-1 was lower than that of R-2. The inhibition effect of alfalfa meal on elevation of TC was apparent to a certain extent. The inhibition effect of alfalfa meal on elevation of TG and NEFA was greater than that of TC, thus it is suggested that alfalfa meal can be successfully utilized for experiments with lipids, when the rabbit is the experimental animal of choice. Effect of riboflavine-2,3,4,5-tetranicotinate (RN-4) on changes of TC, TG and NEFA in rats fed 1% cholesterol diet was also examined. RN-4 was mixed in the diet (0.5, 0.25 and 0.125%). TG levels in groups treated with RN-4 (Rt-2, Rt-3 and Rt-4) were lower than previously observed.

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Indication	Highest Phase	Country/Location	Organization	Date
Wounds and Injuries	Phase 1	-	Renovo Ltd.	-

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