The HIV-1 capsid protein plays a crucial role in viral infectivity, assembling into a fullerene cone that encloses the viral RNA and it has gained attention as a promising therapeutic target. Research has been focused on the spatial structures of capsid proteins in recent years, and peptides and small molecules targeting capsid have been discovered. In this article, it summarizes the structure information of capsid protein, analyzes and compares the binding information of different peptides and small molecules targeting capsid. At the same time we give the perspective to the future drug discovery based on the protein-protein interaction during the maturation process.
Capsid ; chemistry ; Drug Discovery ; HIV Infections ; drug therapy ; HIV-1 ; chemistry

The HIV-1 capsid protein plays a crucial role in viral infectivity, assembling into a fullerene cone that encloses the viral RNA and it has gained attention as a promising therapeutic target. Research has been focused on the spatial structures of capsid proteins in recent years, and peptides and small molecules targeting capsid have been discovered. In this article, it summarizes the structure information of capsid protein, analyzes and compares the binding information of different peptides and small molecules targeting capsid. At the same time we give the perspective to the future drug discovery based on the protein-protein interaction during the maturation process.

Objective To determine that atorvastatin might have anti-inflammatory effects in acute coronary syndromes(ACS) with C-reactive protein(CRP) reduction.Methods Ninety-two patients with ACS were assigned to three groups: high dose atorvastatin group(31 cases),taking atorvastatin 40 mg daily.Standard dose atorvastatin group(31 cases),taking atorvastatin 10 mg daily,and control group(30 cases),only receiving conventional therapy.CRP levels,lipid profiles were measured at first and fifth day and 1 month later.Results The study suggested:(1)CRP levels significantly decreased from baseline to the fifth day and 1 month later in high dose atorvastatin group(P

OBJECTIVETo study the effect of Morinda officinalis (MO) extract on cytoxan (CTX) -impaired spermatogenesis of adult male SD rats.

METHODSWe randomly divided 56 adult male SD rats into seven groups of equal number: blank control, CTX model, CTX + NS, CTX + 10 g/kg MO, CTX + 20 g/kg MO, CTX + 30 g/kg MO, and CTX + 40 g/kg MO. We made the models of impaired spermatogenesis in the SD rats by intraperitoneal injection of CTX and treated the animal models by intragastric administration of MO at the concentrations of 10, 20, 30, and 40 g per kg per d, respectively. After two weeks of medication, we observed the changes in the body weight, testicular and epididymal indexes, and microstructure of the testis tissue, measured the mean seminiferous tubule diameter (MSTD) , and obtained testicular biopsy scores (TBS) in different groups, followed by comparative analyses.

RESULTSAfter treatment, the CTX + NS group showed no remarkable differences in the body weight ([234.83 ± 28.77] g) and epididymal index (2.71 ± 0.34) from those of the four CTX + MO groups, but exhibited a significantly lower testicular index ([12.15 ± 1.04] g) than those in the CTX + 20 g/kg MO ([13.71 ± 0.97] g), CTX + 30 g/kg MO, ([13.30 ± 0.29] g), and CTX + 40 g/kg MO group ([13.48 ± 0.51] g) (P < 0.05). Light microscopy revealed obvious pathological changes of the testis tissue in the CTX + NS group and significantly ameliorated structures of the seminiferous tubules in the CTX + MO 10, 20, 30, and 40 g/kg groups, with the MSTD of (204.78 ± 11.03), (216.55 ± 10.93), (218.03 ± 11.23), and (218.59 ± 14.06) μm, respectively, and the TBS of 9.03 ± 0.39, 9.69 ± 0.26, 9.83 ± 0.18, and 9.89 ± 0.11, respectively, all significantly higher than (189.74 ± 8.55) μm and 5.95 ± 1.21 in the CTX + NS group (P < 0.05). The efficacy of MO extract was increased in a concentration-dependent manner.

CONCLUSIONMorinda officinalis extract can repair cytoxan-induced damage to rat spermatogenesis, with may achieve the best effect at the concentrations of 30 and 40 g per kg per d.

Animals ; Body Weight ; drug effects ; Cyclophosphamide ; toxicity ; Epididymis ; drug effects ; Male ; Morinda ; chemistry ; Mutagens ; toxicity ; Plant Extracts ; administration & dosage ; pharmacology ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Seminiferous Tubules ; drug effects ; pathology ; Spermatogenesis ; drug effects ; Testis ; drug effects ; ultrastructure

Objective To investigate the physicochemical property of Pae-6’O-benzene sulfonate ( CP-25 ) . Meth-ods The CP-25 physicochemical property was evaluated by appearance, Lieberman-Burchard reaction, thin-layer chromatogram, Ultraviolet Spectrophotometry ( UV) , solubility and stability. The content of CP-25 was assayed by high performance liquid chromatography. Results The CP-25 had color response featured by terpenoid, and its maximum UV absorption wavelength was 220 nm. CP-25 was slightly soluble in water and petroleum ether. The main influence factor of CP-25 stability was humidity. Conclusion The present study provides experimental basis for quality standard and formulation design of CP-25 .

Objective To investigate the degradation kinetics of paeoniflorin-6-O’- benzenesulfonate ( CP-25 ) in vitro. Methods The homogenates of liver and intestine were prepared in vitro, and concentrations of CP-25 in ho-mogenates were detected by HPLC. Results CP-25 was obviously degradable in liver and intestine homogenates, and half life of degradation was decreased when levels of homogenates increased;the metabolisms of CP-25 in dif-ferent homogenates of intestine were diverse, the metabolic actions in duodenum and colon were weaker than those of jejunum and ileum. Conclusion Oral administration of CP-25 suffers first pass elimination from intestine and liver, which suggests the absorption of CP-25 could be further improved by appropriate pharmaceutical preparations.

Background Suprachoroidal hemorrhage (SCH)is a rare but devastating complication of ophthalmic surgery,and it is crucial to be aware of the risk factors and select effective treatment. Objective Present study was to assess the treatment and risk factors of SCH induced by intraocular surgery. Methods Retrospective case series were carried out to investigate the clinical data of 15 eyes from 15 patients with SCH at Peking Union Medical College Hospital.The risk factors of SCH were analyzed.Written informed consent was obtained before any medical examination and treatment.SCH was occurred in 10 eyes during intraocular surgery,while the SCH was diagnosed in other 5 eyes 1-3 days after operation.Surgical drainage was carried out in 8 eyes,of which 3 eyes combined with vitrectomy besides surgical drainage and other 5 eyes were treated with medication alone.Results SCH was completely removed and absorbed in 12 eyes.The visual acuity was improved in 6 eyes,unchanged in 6 eyes and decreased in 3 eyes.Nine eyes complicated with retinal detachment and reattached in 6 eyes after treatment.Seven eyes combined with hypermyopia,6 eyes combined with glaucoma,and 1 eye was aphakia.Four patients combined with hypertension,and 2 patients had diabetes mellitus. Conclusions SCH induced by intraocular surgery develops rapidly and violently,and it can result in vision loss without effective treatment.Suturing surgical incision immediately,applying hypertonic agents and sclerotomy drainage are the urgent approaches to treat SCH.Medicines and/or sclerotomy could be optional according to the amount of bleeding and other ocular complication.The risk factors of SCH include myopia,glaucoma and the instantly dropping of intraocular pressure.

Animals ; Arteritis ; complications ; immunology ; Coronary Artery Disease ; etiology ; pathology ; Coronary Vessels ; pathology ; Models, Animal ; Rabbits

Objective To study the management of Fournier's gangrene.Methods Data of 9 patients were reviewed retrospectively and were discussed according to the treatment,and outcome.U-shaped stents with poly hole and two-end drainage were used in 4 cases in whom the infection was spread along the penis,into the scrotum,up to the abdominal wall and into the perineum.Results We have treated 9 cases in the last 21 years.The patients received surgical treatment including incisions,aggressive debridement,drainage,irrigation,and antibiotic therapy.Left uncovered,the testes were protected in either a thigh or abdominal wall pouch and back in the scrotum resconstructed later with a myocutaneous medial thigh flap.When U-shaped stents was used,redunant debriding was no more necessary.The temperature and hemogram regain quickly,and the average hospitalization days decreased to 14 days.Conclusions Aggressive debridement and broad-spectrum antibiotics remain the hallmarks of treatment.Orchidectomy was erroneously part of the treatment of Fournier's gangrene.The remarkable draining effect of U-shaped stents could promote tissue healing.

To evaluate the safety and efficacy of transrectal high-intensity focused ultrasound (HIFU) in the treatment of benign prostatic hyperplasia (BPH), serial studies were conducted in 150 BPH patients before and 30 min, 1, 2, 6 and 12 month(s) after Sonablate-500 HIFU treatment. A silicon-coated indwelling 16F latex catheter was placed during the determination of the therapy zone. Preoperative and postoperative evaluations were made by using the international prostate symptom score (IPSS), quality of life (QOL), uroflowmetric findings and transrectal ultrasound, and incidence of complications. The cystourethrography was done in 23 patients within 1 year postoperatively. The results showed that after HIFU treatment, IPSS and QOL scores were significantly decreased at 1, 2, 6 and 12 month(s) (P<0.01). Maximum urine flow rate (6.0 to 17.2 mL/s, P<0.01), PVR (75.0 to 30.3, P<0.01) and prostatic volume (65.0 to 38.1 mL, P<0.05) were significantly improved 12 months after the operation. Recurrent urinary retention (n=2) and urethrorectal fistula (n=1) occurred at the 15(th) postoperative day. The duration of the HIFU prostate ablation was 25-90 min. The mean time for an indwelling catheter was 3-19 days. These data demonstrate that treatment of BPH with Sonablate-500 HIFU is safe and effective.
Prostatic Hyperplasia/diagnosis ; Prostatic Hyperplasia/*therapy ; Ultrasound, High-Intensity Focused, Transrectal/adverse effects ; Ultrasound, High-Intensity Focused, Transrectal/instrumentation ; Ultrasound, High-Intensity Focused, Transrectal/*methods