OBJECTIVETo evaluate the efficacy and safety of Jinying Capsule (JC) in treating pelvic inflammatory disease patients with accumulated damp-heat syndrome (ADHS).

METHODSTotally 328 patients were recruited in a prospective, positive drug parallel controlled, and multi-center clinical trial. Of them 213 patients in the treatment group took JC (0.5 g per capsule), 4 capsules each time, 3 times per day, while 115 patients in the control group took Kangfuyan Capsule (KC, 0.4 g per capsule), 3 capsules each time, twice per day. The course of treatment was 4 weeks for all. Scores of Chinese medical syndromes, visual analogue scale (VAS) of the lower abdominal pain, and European quality of life-five dimension scale (EQ-5D) were observed before treatment and after 4 weeks of treatment.

RESULTSThere were 204 patients in the treatment group and 109 in the control group who completed this trial. The total effective rate of Chinese medical syndrome was 89.71% (183/204 cases) in the treatment group and 76.15% (83/109 cases) in the control group (P < 0.01). Compared with before treatment in the same group, EQ-5D scores increased, and VAS scores of the lower abdominal pain decreased in the two groups after treatment. EQ-5D scores was 0.857 ± 0.157 in the treatment group, obviously higher than that in the control group (0.753 ± 0.126, P < 0.05). VAS scores of the lower abdominal pain was 2.14 ± 1.23 in the treatment group, lower than that in the control group (2.33 ± 1.24), but with no statistical difference between the two groups (P > 0.05). No adverse reaction occurred in the two groups.

CONCLUSIONJC was superior to KC in improving Chinese medical syndrome and quality of life of pelvic inflammatory disease patients with accumulated damp-heat syndrome.

Capsules ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Hot Temperature ; Humans ; Medicine, Chinese Traditional ; Pelvic Inflammatory Disease ; drug therapy ; Phytotherapy ; Prospective Studies ; Quality of Life ; Safety ; Syndrome

OBJECTIVETo study the effects of cool restrain stress on the accumulation of eosinophils and expression of Th cytokines in rat nasal mucosa with allergic rhinitis model.

METHODSFifty healthy female rats were randomly divided into 5 groups: control group, allergic rhinitis (AR) group, AR plus stress group, stress plus AR group and simultaneous stress-AR group. Cool restrain stress, AR model and simultaneous stress-AR were made. Nasal mucosa of septum from rats of five groups were stained routinely by haematoxylin eosin (HE) and immunohistochemistry respectively. The density of eosinophils and expression of interleukin (IL)2, IL-6 were observed by using software of image analysis systems under microscope.

RESULTSThe density of eosinophiles and IL-6 in the nasal mucosa of stress-AR group were significantly higher than those in AR [(14.1 +/- 3.2) for eosinophiles, and (15.3 +/- 4.8) for IL-6 ] and were also significantly higher than those in control groups [(2.3 +/- 1.4) for eosinophiles, and (4.9 +/- 2.4) for IL-6)], and the differences reached statistical significance. (F were respectively 7.06, 7.14, 8.54, 8.20, P were respectively < 0.05 or < 0.01), but no significant differences of the three groups (AR plus stress, stress plus AR and simultaneous stress-AR groups) were found (F were respectively 2.90 and 3.20, P > 0.05). The expression of IL-2 in nasal mucosa of stress-AR group was significantly reduced compared with AR and control groups (F were respectively 7.27, 7.32, P were respectively < 0.05 or < 0.01). But there were also no significant differences of the three groups (AR plus stress, stress plus AR and simultaneous stress-AR groups, F = 3.12, P > 0.05).

CONCLUSIONSThe abnormal infiltration and accumulation of eosinophiles and the differences in expression of IL-2 and IL-6 which represented Th1 and Th2 cytokines in rats nasal mucosa varied in different groups. The eosinophiles and IL-6 were rarely expressed in control group and moderately expressed in AR group, but significantly expressed in cool restrain groups. The IL-2 representing Th1 cytokines were reduced in cool restrain stress gruops. All these results indicated that cool restrain stress might play a role in inducing rat allergic rhinitis.

Animals ; Eosinophils ; metabolism ; Interleukin-2 ; Interleukin-6 ; metabolism ; Nasal Mucosa ; metabolism ; Rats ; Rhinitis, Allergic ; metabolism ; Rhinitis, Allergic, Perennial ; metabolism

Photodynamic therapy (PDT), because of its good targeting, minimal invasion, and safety, is becoming a very active area in cancer prevention and treatment, in which the photosensitizers have proved to be the core element for PDT. We developed a new HPLC method for analyzing porphyrin photosensitizers using Shiseido Capcell PAK C18 (150 mm x 4.6 mm, 5 µm) as the column at 30 °C, methanol-1% aqueous solution of acetic acid as the mobile phase in a flow rate of 1.0 mL · min(-1) in a gradient elution mode, and the detection wavelength at 380 nm. This method, showing good specificity, precision, accuracy and robusty via methodology validations, can be applied to the purity test and assay of porphyrin photosensitizers, and has played a key guide role in the R&D of the new porphyrin photosensitizer--sinoporphyrin sodium.
Chromatography, High Pressure Liquid ; Photochemotherapy ; Photosensitizing Agents ; chemistry ; Porphyrins ; chemistry

To discover novel antitumor fluoroquinolone lead compounds from a rational modification for antibacterial fluoroquinolones, a fused heterocyclic ketone corresponding to thiazolo[2,3- b][1,2,4]triazolone used as a bioisosteric replacement of the C-3 carboxylic acid group of ciprofloxacin 1, and further modification by a Claisen condensation reaction with substituted benzaldehydes formed novel fluoroquinolone C-3 fuse heterocyclic α, β-unsaturated ketones as the title compounds (6a-6r), separately. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS, and the in vitro anti-proliferative activity against human hepatoma Hep-3B cells, pancreatic Capan-1 cells and leukemia HL60 cells was evaluated by a MTT assay. The preliminary results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. In particular, compounds carrying an electron-withdrawing carboxyl (6k, 6m) or sulfonamide substituent (6q, 6r) attached to benzene ring were comparable to or better than constractive drug doxorubicin against Capan-1 cells. As such, it suggests that it is favorable for a fused heterocyclic α, β-unsaturated ketone scaffold instead of the C-3 carboxylic acid group to improve the antitumor activity of fluoroquinolones.
Anti-Bacterial Agents ; Antineoplastic Agents ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Ciprofloxacin ; analogs & derivatives ; Fluoroquinolones ; chemical synthesis ; pharmacology ; HL-60 Cells ; Humans ; Ketones ; pharmacology ; Structure-Activity Relationship

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.
Amides ; chemical synthesis ; pharmacology ; Antineoplastic Agents ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Fluoroquinolones ; chemical synthesis ; pharmacology ; HL-60 Cells ; Humans ; Ketones ; chemical synthesis ; pharmacology ; Rhodanine ; chemical synthesis ; pharmacology

To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.
Anti-Bacterial Agents ; chemistry ; Antineoplastic Agents ; pharmacology ; Cell Line, Tumor ; Ciprofloxacin ; chemistry ; Doxorubicin ; pharmacology ; HL-60 Cells ; Humans ; Ketones ; pharmacology ; Sulfides ; pharmacology ; Triazoles ; pharmacology

Angiogenesis, the expansion of preexisting blood vessels, is a complex process required for tumor growth and metastasis. Although current antiangiogenic strategies have shown promising results in several cancer types, identification of additional antiangiogenic targets is required to improve the therapeutic response. Herein, we show that the microtubule-binding protein CLIP-170 (cytoplasmic linker protein of 170 kDa) is highly expressed in breast tumor samples and correlates positively with blood vessel density. Depletion of CLIP-170 significantly impaired vascular endothelial tube formation and sprouting in vitro and inhibited breast tumor growth in mice by decreasing tumor vascularization. Our data further show that CLIP-170 is important for the migration but not the proliferation of vascular endothelial cells. In addition, CLIP-170 promotes the polarization of endothelial cells in response to the angiogenic stimulus. These findings thus demonstrate a critical role for CLIP-170 in tumor angiogenesis and suggest its potential as a novel antiangiogenic target.
Animals ; Breast Neoplasms ; blood supply ; metabolism ; pathology ; Cell Line, Tumor ; Cell Movement ; Cell Polarity ; Female ; Human Umbilical Vein Endothelial Cells ; Humans ; MCF-7 Cells ; Mice ; Mice, Nude ; Microtubule-Associated Proteins ; antagonists & inhibitors ; genetics ; metabolism ; Microtubules ; metabolism ; Neoplasm Proteins ; antagonists & inhibitors ; genetics ; metabolism ; Neovascularization, Pathologic ; RNA Interference ; RNA, Small Interfering ; metabolism ; Transplantation, Heterologous

Objective:To analyze the gene mutation, clinical manifestations and prognosis of children with steroid resistant nephrotic syndrome (SRNS), and to provide reference for the treatment of hereditary SRNS in children.Methods:The clinical data of 29 patients with SRNS and whole exon sequencing (WES) diagnosed in Xi′an Children′s Hospital from January 1, 2018 to December 31, 2020 were retrospectively analyzed.Results:In 29 cases of SRNS with genetic testing, 10 cases (34.5%) were gene mutations, including 2 cases of congenital nephrotic syndrome. The onset age of the patients with gene mutation ranged from 0.1 to 10.7(4.06±3.73)years, and the median age of onset was 3.3 years. The clinical type was mainly nephritis (8/10), and the pathological type was mainly focal segmental glomerulosclerosis (FSGS) (5/7). The main mutant genes were NPHS1 (2 cases), NPHS2 (2 cases), WT1 (2 cases), SMARCAL1 (1 case), COQ8B (1 case), TRPC6 (1 case) and COL4A3 gene (1 case). The main types of genetic variation were missense mutations, and 6 (60%) cases were new mutations that had never been reported in the database containing human pathogenic mutations before. Compared with the non-gene mutation group, 24 hour urinary protein was higher [(177.92±164.59)mg/(kg·24 h) vs (84.99±40.79)mg/(kg·24 h)] in gene mutation group, with statistically significant difference ( P<0.05). In the gene mutation group, there were 2 cases of complete remission, including 1 case of complete remission treated with coenzyme Q10, 1 case of partial remission, and 8 cases of immunosuppression treatment, with an effective rate of 2/8, while in the non-gene mutation group, the effective rate of immunosuppression treatment was 17/19, with statistically significant difference in prognosis between the two groups ( P<0.05). Conclusions:The pathological type of children with hereditary SRNS is mainly FSGS, which are often ineffective to immunosuppressive therapy, poor prognosis and easy to progress to end-stage renal disease. Gene detection is of great significance for etiological diagnosis, treatment and prognosis evaluation in children with SRNS.

OBJECTIVETo provide theoretic warrant and technical reference for Salvia miltiorrhizr standardization planting, by carrying out various systemic studies such as observation of seeds configuration fabric, idiosyncrasy of water absorption and groping germinating conditions.

METHODIn the study of configuration fabric, seeds were observed and taken photos by scanning electronic microscope, and heft method was used for measuring changes of water absorption velocity and dehydration velocity. Seeds germination conditions were probed into under the national test regulations for crop seeds and related prescription from international standards.

RESULT(1) There was a layer of slime about 10-20 microm thickness covering epicarp of Danshen seeds. The slime formed as diamond meshwork (reseau) and the weight of it was 8%-10% of total seeds weight. (2) The speed of water absorption of seeds was extremely rapid. The weight of seeds could increase above 10 times as original while the dehydration velocity was quite low. (3) The optimal temperature for the seeds germination is around 25 degrees C, and the germination rate of the new seeds gained yearly was above 75%, but the rate would decrease sharply as years went by. It was also found that the seeds germination power and exponent of vigor were quite high under the temperature transformation between 23 degrees C, 28 degrees C. Such treatments as pre-cool, PEG treatment and infusing with GA3 could increase the rate of seeds germination capacity obviously.

Germination ; physiology ; Plants, Medicinal ; anatomy & histology ; growth & development ; physiology ; Salvia miltiorrhiza ; anatomy & histology ; growth & development ; physiology ; Seeds ; anatomy & histology ; physiology ; ultrastructure ; Temperature ; Water

OBJECTIVESTo detect the expressions of Tec tyrosine kinase in hepatocellular carcinoma and the levels of phosphorylation of tyrosine kinase in liver cancer tissues, paracancerous tissues and normal liver tissues and to find the significance of their differences.

METHODS200 specimens of tissues, including liver cancer tissues, surrounding liver tissues not more than 1.5 cm from the cancers, and normal liver tissues were investigated for Tec protein expression and Tec phosphorylation by tissue microarrays and immunohistochemistry (SP method).

RESULTSThe positive immunohistochemical stainings of Tec in cancerous tissues and non-cancerous tissues showed no obvious differences, nevertheless, the immunostaining levels in liver cancer tissues were much higher than in non-cancerous tissues and they correlated with the grading of tumors (P < 0.05). The phosphorylation of Tec was significantly expressed in liver cancer tissues (73%) in comparison with other tissues (42%, 10% both P < 0.05), but it did not correlate with any clinicopathological characteristics.

CONCLUSIONOverexpression of Tec is associated with the tumorigenesis and development of liver cancer; inhibiting Tec or degrading Tec phosphorylation directly might affect the progression of liver cancer.

Adult ; Aged ; Aged, 80 and over ; Carcinoma, Hepatocellular ; metabolism ; Female ; Humans ; Liver Neoplasms ; metabolism ; Male ; Middle Aged ; Neoplasm Proteins ; genetics ; metabolism ; Phosphorylation ; Protein-Tyrosine Kinases ; genetics ; metabolism