The apoptosis was observed under a fluoroscope when the tested tumor cells were treated with the supernatant derived from the liquid culture of an actinomyces strain AK 11, which had showed cell toxicity by means of MTT assay, and was further confirmed by the correspondent band of ”DNA ladder” in the agarose gel electrophoresis. In a bioassay employed nude mouse, the pure compound produced by the strain AK 11 showed tumor inhibition in rates of 52.01% and 33.64% corresponding to the dosages of 0.016 ?g?kg -1 and 0.008 ?g?kg -1 ip, respectively. According to the indexes IC 50 of human hepatocarcinoma SMMC7721 and stomach cancer MGC 803 cells, it was estimated that the inhibition effect of the pure compound was slightly stronger than that of Adriamycin. The results showed high antitumor effect of the tested compound from the strain AK 11. When the cells were treated with AK 11, it was found by flow cytometry analysis that cell division was ceased at S phase due to the DNA synthesis block .

Carotid Body Tumor ; diagnosis ; therapy ; Humans

Animals ; Intestines ; cytology ; drug effects ; physiology ; Meperidine ; pharmacology ; Mice ; Mice, Inbred Strains ; Muscle, Smooth ; drug effects ; physiology ; Rabbits

Acupuncture Therapy ; Adult ; Antidepressive Agents, Tricyclic ; therapeutic use ; Clomipramine ; therapeutic use ; Combined Modality Therapy ; Electroacupuncture ; Female ; Humans ; Male ; Middle Aged ; Obsessive Behavior ; therapy

Aged, 80 and over ; Humans ; Male ; Maxillary Sinus Neoplasms ; pathology ; Neoplasms, Muscle Tissue ; pathology

We designed and synthesized eighteen lycorine derivatives with five different structural types, and evaluated their antiviral activities on a HCoV-OC43-infected H460 cell model. Structure-activity relationships suggested that the introduction of appropriate substituents on the 6N atom of lycorine was beneficial to activity. Compound 6a gave a good activity with the half effective concentration (EC₅₀) and selectivity index (SI) values of 2.36 μmol·L^-1 and 16.52, respectively. Surface plasmon resonance (SPR) result indicated that 6a might target the non-structural protein 12 (NSP12) subunit in RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 with the dissociation constant (K_D) value of 1.36 μmol·L^-1. Molecular docking indicated that 6a might act on nidovirus RdRp-associated nucleotidyltransferase (NiRAN) catalytic center of NSP12, distinct from the mechanism of nucleoside-like drugs such as remdesivir. This study provides scientific data for the development of lycorine derivatives into a new class of anti-SARS-CoV-2 small molecule inhibitors.

Objective To observe the effects of Fengshi Bitong Prescription (FSBT) on cytokines in serum and Fas/FasL mRNA expression system in synovium; To discuss relevant mechanism of action. Methods Rats were given foot intradermal injection of bovine type Ⅱ collagen emulsion to establish collagen-induced arthritis (CIA) model. After successful modeling, they were randomly divided into 6 groups: normal control group, CIA model group, tripterygium glycosides group, FSBT high-, medium-, and low-dose groups. Each medication group was given relevant medicine for gavage for 14 d. The weight and arthritis scores of CIA rats were observed. Serum levels of IL-1β, IL-15, and TGF-β1 were detected by ELISA. Expressions of Fas and FasL mRNA in synovium of CIA rats were detected by real-time PCR. Results Compared with model group, the foot arthritis score and serum levels of IL-15 in FSBT high- and medium-dose groups significantly decreased (P<0.01), and the serum level of TGF-β1 significantly increased (P<0.05). Expression of Fas significantly decreased and FasL significantly increased in FSBT high-dose group (P<0.05). Conclusion FSBT may have certain immune regulation effects on rheumatoid arthritis. Its mechanism may be in regulating Fas/FasL apoptosis system, thereby inducing apoptosis of synovial cells and inhibiting synovial hyperplasia.

Animals ; Cell Death ; Hepatic Stellate Cells ; cytology ; Humans ; Liver Cirrhosis

Objective To study the clinical significance and changes of plasma nitric oxide (NO) and cyclic adernosine monophosphate(cAMP)/cyclic guanosine monophosphate(cGMP) ratio in children with asthma.Methods NO,cAMP,cGMP levels and changes of cAMP/cGMP in 40 asthmatic children in acute attack stage and restoration stage and in 23 health children were measured by nitric acid reductase method and radioimmunoassay.Results 1.the amount of NO 3-/NO 2-in the plasma of asthmatic children in acute attack stage was obviously higher than that in restoration stage and in normal control group(P0.05);6.the results of linear correlation analysis showed that there were positive correlations between plasma NO 3-/NO 2- and plasma cGMP levels in acute attack stage (r=0.401 P