Journal of Chinese Pharmaceutical Sciences

Safety and tolerability of available drugs for hyperuricemia: a critical review and an update on recent developments

Gong Fang, Wenxi Li, Jie Zhang, Qinghua Ke, Xinggui Zhu, Lihua Long, Changhai Li

2022, 31(6): 397-411. DOI: 10.5246/jcps.2022.06.035

Asbtract ( 256 )

HTML ( 12)

PDF (1420KB) ( 56 )

References | Related Articles | Metrics

Hyperuricemia (HUA) is a metabolic disease caused by excessive production of serum uric acid (sUA) or decreased excretion of sUA in the body. HUA is an independent risk factor for chronic kidney disease, hypertension, cardiovascular and cerebrovascular diseases, and diabetes mellitus. Timely and effective treatment for reducing sUA plays a key role in reducing urate deposition, preventing gout attacks, and reducing kidney damage and the occurrence of other accompanying diseases. Four pharmacological methods can be used to treat HUA: decrease urate production, increase urate excretion, prevent urate formation, and catabolize urate. To provide a reference for clinical treatment and new medical research for HUA, the drugs and potential drugs for HUA were reviewed in the present work.

Network pharmacology and metabolomics-based detection of the potential pharmacological effects of the active components in Chrysanthemum morifolium 'Chuju'

Weiping Zhao, Qi Ge, Zijun Ding, Leizhi Pan, Ziqing Gu, Yang Liu, Hua Cai

2022, 31(6): 412-428. DOI: 10.5246/jcps.2022.06.036

Asbtract ( 234 )

HTML ( 7)

PDF (12133KB) ( 63 )

Figures and Tables | References | Related Articles | Metrics

Chrysanthemum morifolium 'Chuju' is a famous medicinal species in traditional Chinese medicine. 'Chuju' contains various active ingredients that can be used to treat multiple diseases without toxic side effects. In the present study, we combined metabolomics and network pharmacology to further explore the active ingredients in 'Chuju', as well as the target and pharmacological mechanisms of the active ingredients. A visualized network analysis model based on chemistry, pharmacokinetics, and pharmacology was constructed to predict the potential pharmacological mechanism of 'Chuju'. A total of 424 metabolites of 'Chuju' were identified, of which 21 ingredients had positive pharmacological effects after ADME screening. The network pharmacology revealed that acacetin and beta-sitosterol in 'Chuju' could act on GSK3B, MAPK14, ADRA1R, and NOS2 to regulate diabetes mellitus, Alzheimer's disease, breast cancer, and inflammatory diseases. These results indicated the potential pharmacological effects of the active components in 'Chuju'.

Natural plant-derived 3,4-dihydroxybenzaldehyde ameliorates reproductive damage of male mice

Hongning Zhang, Shuying Han, Xiaoping Pu, Chunna An

2022, 31(6): 429-440. DOI: 10.5246/jcps.2022.06.037

Asbtract ( 191 )

HTML ( 2)

PDF (3247KB) ( 26 )

Figures and Tables | References | Related Articles | Metrics

In the present study, we studied the effects of 3,4-dihydroxybenzaldehyde, derived from Salvia miltiorrhiza Bunge, on mouse sperm survival and sperm membrane integrity in vitro and on mouse reproductive damage induced by cyclophosphamide in vivo. 3,4-Dihydroxybenzaldehyde (0.01, 0.1, and 1 mg/mL) improved sperm survival rate and sperm membrane integrity in separated mouse sperm (all P < 0.05). In cyclophosphamide-treated male mice (60 mg/kg/d through intraperitoneal injection for 5 d), 3,4-dihydroxybenzaldehyde (40 mg/kg/d through intragastric gavage for 35 d) increased the testis index, epididymis index, and sperm nuclear maturity (all P < 0.05). 3,4-Dihydroxybenzaldehyde also improved testis morphology characterized by orderly arranged layers of spermatogenic cells, numbers of sperm in the lumen, normal mesenchymal cells, and close and tidy arrangement of the seminiferous tubules. 3,4-Dihydroxybenzaldehyde also increased testicular superoxide dismutase activity and elevated DJ-1 expression. In addition, it decreased the expression of ICAM-1 and enhanced the expressions of VCAM-1, PEDF, VEGF, and PPARγ. These findings indicated that 3,4-dihydroxybenzaldehyde increased mouse sperm survival and sperm membrane integrity in vitro and reduced mouse reproductive damage induced by cyclophosphamide via DJ-1 and other targets in vivo. 3,4-Dihydroxybenzaldehyde might thus be useful for treating male reproductive damage and antineoplastic cyclophosphamide-induced reproductive toxicity.

The relationship between the contents of 13 amino acids in brain tissues and the progression of NAFLD via C57BL/6 model mice

Suqiong Huang, Jingyuan Wan, Tingting Du, Tao Gong, Jing Zhang, Xinhui Jiang

2022, 31(6): 441-451. DOI: 10.5246/jcps.2022.06.038

Asbtract ( 156 )

HTML ( 2)

PDF (2249KB) ( 14 )

Figures and Tables | References | Related Articles | Metrics

Non-alcoholic fatty liver disease (NAFLD) is the steatosis of liver parenchyma unrelated to alcoholism, autoimmunity, and viral infection. It is also a metabolism-related syndrome, which has an unseparated relationship with adipose tissue dysfunction and obesity. Hepatic encephalopathy (HE) is one of the severe complications of chronic liver disease and one of the end-stage syndromes of liver disease. Some researchers have suggested that NAFLD, like other forms of liver injury, may be related to the metabolic disorder of branched-chain amino acids (BCAAs), which have been approved to be associated with HE influencing ammonia and energy metabolism. However, several studies have revealed the relationship among amino acids in serum, HE, and chronic liver disease; there are few studies on the contents of amino acids in brain tissues of an animal model with NAFLD. In the present research, we established a NAFLD mouse model with C57BL/6 mice and determined the contents of 13 amino acids in brain tissues of model mice by HPLC-FLD derivatization method using ortho-phthalaldehyde (OPA) to explore the relationship between the contents of amino acids in brain tissues and the progression of NAFLD. Moreover, the study showed that the changes of amino acid contents in the brain of the C57BL/6 mice were associated with the advancement of NAFLD, and this change might be related to the mechanism of HE.

The antioxidant activity and total phenolic and total flavonoid contents of Pyracantha fortuneana fruit can be improved by solid-state fermentation with Rhizopus oryzae and Penicillium commune

Jianwei Dong, Xuejiao Li, Chen Yang, Yanqing Zhang, Huifang Zhou, Yali Li

2022, 31(6): 452-460. DOI: 10.5246/jcps.2022.06.039

Asbtract ( 133 )

HTML ( 3)

PDF (2318KB) ( 14 )

Figures and Tables | References | Related Articles | Metrics

Cancer metastasis is a process with multi-step complexity and apparent randomness. In this study, we aimed to establish a stochastic mathematical model to describe the random process of cancer metastasis and predict the drug effect of QAP14 on metastasis in a mouse model. The data of lung metastases on the 22^nd day after cancer cell implantation with or without the treatment of QAP14, a new chemical compound, were collected in 4T1 breast cancer BALB/c mice. Based on the exponential growth of the primary tumor and metastatic loci, a joint distribution model of metastasis size and number was developed. Disease progression of metastasis and preclinical efficacy of QAP14 were modeled. Parameters M and m representing maximum and minimum of metastasis volume were 3.24 and 0.0184 mm³, respectively. The metastasis growth rate γ and metastasis promotion time ρ were estimated and fixed to be 0.0216 d^–1 and 7.8 d, respectively. The efficacy of QAP14 acted on metastasis promotion time and metastasis growth rate constant in an exponential term, and the effect parameter Effect_ρ and Effect_γ were 16.6 and 0.327 g/mg, respectively. In the present study, we comprehensively characterized the random process of lung metastasis and efficacy of QAP14 in 4T1 breast cancer mice, which might provide a useful reference for the establishment of a clinical population model of cancer metastasis.

Solubility enhancement of ethyl p-methoxycinnamate under nanoscale confinement

Revika Rachmaniar, Dolih Gozali, Camellia Panatarani, Wahyu Priyo Legowo, Sohadi Warya, Taofik Rusdiana

2022, 31(6): 461-470. DOI: 10.5246/jcps.2022.06.040

Asbtract ( 165 )

HTML ( 4)

PDF (2140KB) ( 70 )

Figures and Tables | References | Related Articles | Metrics

The low solubility of ethyl p-methoxycinnamate (EPMC) inhibits its absorption in the gastrointestinal tract, impairing its pharmacological effect. The solubility of EPMC can be increased by utilizing a carrier in the type of mesoporous silica nanoparticles (MSN). In the present study, we aimed to confine EPMC under the nanoscale of MSN (MSN-EPMC) to increase the water solubility of EPMC. MSN was prepared using sodium silica as a precursor and Tween 80 and Span 80 as templates. Briefly, 500 mg MSN was dispersed into 2% w/v EPMC solution, stirred at 100 r/min for 24 h, and dried at 60 °C. The results showed that the MSN formed had a particle size of 87.1305 nm, a surface area of 68.86 m²/g, a pore diameter of 20.45 nm, and a pore volume of 0.352 cm³/g. EPMC was successfully confined under the nanoscale of MSN. MSN-EPMC had an amorphous structure, a loading capacity of 10.6%, and a loading efficiency of 18.18%. The solubility of MSN-EPMC was increased by 2.63 folds at 30 min compared with EPMC. The amorphous structure of MSN-EPMC was responsible for the enhancement of the water solubility. It could be concluded that the confining of EPMC in MSN had the potential to increase the solubility of a water-soluble isolate of a plant.

Research progress of sacubitril/valsartan in heart failure patients with preserved ejection fraction

Jingjing Cao, Shujuan Zhao, Chenglong Zhao, Peizhi Ma

2022, 31(6): 471-477. DOI: 10.5246/jcps.2022.06.041

Asbtract ( 130 )

HTML ( 4)

PDF (1338KB) ( 27 )

References | Related Articles | Metrics

With the launch of sacubitril/valsartan (ARNI), there are new options for the treatment of heart failure (HF). However, ARNI is currently only used in HF patients with reduced ejection fraction (HFrEF). No evidence shows that no modern treatment can reduce mortality in HF patients with preserved ejection fraction (HFpEF). Therefore, it is urgently necessary clarify whether ARNI can be used in the treatment of HFpEF. In the present study, we summarized the research progress of ARNI in the treatment of HFpEF.