Journal of Chinese Pharmaceutical Sciences

An overview of Pu-erh tea and its health-promoting effects of lipid-lowering and anti-obesity

Eric Wei Chiang Chan, Siu Kuin Wong, Hung Tuck Chan

2021, 30(8): 623-633. DOI: 10.5246/jcps.2021.08.050

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As a dark tea, Pu-erh tea (PET) is produced from sun-dried leaves of Camellia sinensis var. assamica mainly in Yunnan Province of China. Many microorganisms are involved in the fermentation of PET. Among them, Aspergillus niger is most important. It is believed that the longer the preservation period, the better is the quality and taste of PET, which is commercially available as loose, compressed or instant tea leaves. Chemical components of PET include flavones, flavanols, flavonols, phenolic acids, alkaloids and methylxanthines. In this overview, the lipid-lowering and anti-obesity effects of PET were discussed based on animal models and human trials, and our study provided some insights into possible mechanisms of bioactive compounds, such as theabrownin, catechins, lovastatin and gallic acid. Other bioactivities of PET and some information on Fuzhuan brick tea were also included. Sources of information cited were from Google Scholar, PubMed, PubMed Central, Science Direct, J-Stage, PubChem, Directory of Open Access Journals (DOAJ), and China National Knowledge Infrastructure (CNKI).

Synthesis, cytotoxicity assay, and molecular docking study of hydroxychalcone derivatives as potential tyrosinase inhibitors

Aris Stiawan, Eti Nurwening Sholikhah, Yehezkiel Steven Kurniawan, Yoga Priastomo, Jumina

2021, 30(8): 634-644. DOI: 10.5246/jcps.2021.08.051

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In this work, we studied the synthesis, cytotoxicity assay, and molecular docking of hydroxychalcone derivatives as tyrosinase inhibitors. Synthesis of chalcone derivatives was carried out through a Claisen-Schmidt condensation reaction between acetophenone and benzaldehyde derivatives under alkaline conditions for 48 h. The synthesized products were characterized by using Fourier transform infrared (FTIR), gas chromatography-mass spectrometry (GC-MS), proton and carbon nuclear magnetic resonance (¹H and ¹³C NMR) spectrometer. The in vitro inhibitory activity was evaluated against tyrosinase enzyme by employing L-3,4-dihydroxyphenylalanine (L-DOPA) as the substrate. We successfully synthesized 4-hydroxychalcone (HC) and 4-hydroxy-3-methoxychalcone (HMC) with a yield of 60% and 76%, respectively. While the tyrosinase inhibitory test of HC and HMC gave the IC₅₀ value of 64.35 and 21.56 μg/mL, respectively, demonstrating that their inhibitory activities against tyrosinase enzyme were better compared with kojic acid and hydroquinone as the positive controls. We also found that HC gave 2025 μg/mL as the IC₅₀ value against Vero cells, confirming that it was not toxic to the normal cell line. The molecular docking study gave the root-mean-square deviation value of less than 2 ?. Furthermore, the binding energies of hydroxychalcone derivatives were found as –30.13 and –31.38 kJ/mol, showing that those compounds could be potentially used as the alternative tyrosinase inhibitors in medical application.

In vitro metabolism and inhibitory effects of atractylenolide II on various hepatic CYPs in HLMs

Xulong Chen, Zhengge Liao, Cheng Li, Guoyong Huang, Yunyan Song, Wei Dong, Abid Naeem, Xinli Liang

2021, 30(8): 645-656. DOI: 10.5246/jcps.2021.08.052

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In the present study, we aimed to investigate the interaction between atractylenolide II (AT-II) and CYP450 enzyme in human liver microsomes, and to lay a theoretical foundation for predicting the possible interaction of AT-II in combination with drugs. The chemical inhibition experiment was carried out with specific inhibitors to clarify the CYP450 subtypes affecting the metabolism of AT-II, and the mechanism, kinetics, and type of inhibition of CYP450 enzyme by AT-II were studied by using the probe-based determination method of human liver microsome system with the related data of IC50 and K_i as evaluation indexes. The metabolism of AT-II was affected by CYP1A2, CYP2C9 and CYP3A4 inhibitors, and the highest inhibition rates were 41.35%, 41.97% and 82.45%, respectively. The IC₅₀ values of AT-II to five subtypes of P450 CYP2C9, CYP1A2, CYP2C19, CYP3A4 and CYP2D6 were 69.7, 84.3, 92.4, 173.8 and 190.1 μmol/L, respectively. The K_i values of AT-II to five subtypes of P450 CYP2C9, CYP1A2, CYP2C19, CYP3A4 and CYP2D6 were 190.6, 179.1, > 200, 72.2 and 66.8, respectively. Among these enzymes, AT-II exhibited non-competitive inhibition on CYP1A2, showed competitive inhibition on CYP2C9 and CYP3A4, and displayed mixed AT-II inhibition on CYP2C19 and CYP2D6. CYP1A2, CYP2C9 and CYP3A4 were involved in the AT-II metabolism, and AT-II exhibited different inhibitory mechanisms and strengths for the five subtypes of CYP450.

Acute oral toxicity test and assessment of rhynchophylline in mice

Lanlan Hu, Huijing Zhang, Le Zhang, Jianlin Tang

2021, 30(8): 657-665. DOI: 10.5246/jcps.2021.08.053

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As the main alkaloid constituent of Uncaria species, rhynchophylline has drawn extensive attention in recent years for its antihypertensive and neuroprotective activities. However, toxicity study of the rhynchophylline is still lacking. In the present study, oral acute toxicity of rhynchophylline was conducted in Kunming mice. The mice were orally treated with 520.00, 442.00, 375.70, 319.34 and 271.44 mg/kg of rhynchophylline for 14 d. The general behavior, body weight changes, toxic reaction, and death were recorded, and histopathological analyses were performed. The acute toxicity was evaluated by the assessment of the median lethal dose (LD₅₀). The acute toxicity study showed that no significant difference was found in the body weight of the mice in the control group and those in the drug group. However, the mice treated with rhynchophylline showed obvious abnormal symptoms and mortality. The median lethal dose (LD₅₀) of orally administered rhynchophylline was 308.08 mg/kg. The histopathological results showed that the mice in the high-dose rhynchophylline group displayed toxic effects in the brain, liver, lung, and kidney. The results of the current study indicated that rhynchophylline could not be taken at a high dose. Collectively, our current findings provided a strong basis for further clinical investigation.

The reversal effect of capsaicin on doxorubicin-resistant breast cancer cells

Yi Zhou, Ting Wang, Jiajia Zhao, Xuehua Jiang

2021, 30(8): 666-674. DOI: 10.5246/jcps.2021.08.054

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Overexpression of P-glycoprotein (P-gp), encoded by the MDR1 gene, in tumor cells curtails the efficacy of chemotherapy, leading to multidrug resistance (MDR), which can be reversed by the P-gp inhibitor. Capsaicin, the principal pungent component of hot chili, is a reported P-gp inhibitor with anti-cancer properties. In the present study, we aimed to evaluate the MDR reversal effect of capsaicin. The MCF-7/DOX cells were treated with capsaicin for a short term (3 h) or long term (72 h). The cytotoxicity studies were completed by using the SRB method. RT-PCR method was utilized to evaluate the effect of capsaicin on the expression of MDR1 at the mRNA level. The accumulation and subcellular distribution studies were implemented to further investigate the reversal effect of capsaicin. The effect of capsaicin on the ATP production of mitochondria was also evaluated. The results of the cytotoxicity study indicated that capsaicin (50 μM) reversed the resistance of MCF-7/DOX cells to doxorubicin (DOX) with the reversal fold of 4.68, and concentration-dependently down-regulated the expression of MDR1 at the mRNA level after long-term (72 h) incubation. After short-term (3 h) incubation, capsaicin reversibly and concentration-dependently increased the accumulation of DOX into MCF-7/DOX cells and induced a different subcellular distribution of DOX compared with verapamil as a positive control. The ATP production of mitochondria was also concentration-dependently inhibited by capsaicin. In conclusion, capsaicin was capable of reversing the resistance of MCF-7/DOX cells to DOX, making it a promising lead compound for MDR reversal.

Anti-inﬂammatory effects of diaporisoindole B in LPS-stimulated RAW 264.7 macrophage cells via MyD88 activated NF-κB and MAPKs pathways

Hongju Liu, Jing Li, Huiyi Xie, Lingling Wang, Zhizhen Zhang, Chong Yan

2021, 30(8): 675-685. DOI: 10.5246/jcps.2021.08.055

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Diaporisoindole B (DPB), an isoprenylisoindole alkaloid isolated from the mangrove endophytic fungus Diaporthe sp. SYSU-HQ3, has been proved to inhibit the production of nitric oxide (NO) in lipopolysaccharide (LPS)-challenged RAW 264.7 mouse macrophages, showing potent anti-inflammatory effects. In this study, we further investigated the anti-inflammatory effects of DPB and explored the possible mechanisms in LPS-challenged RAW 264.7 mouse macrophages. The results showed that DPB (3.125, 6.2, 12.5 and 25 μM) could significantly reduce LPS-induced levels of PGE2, and inhibit the expressions of iNOS and COX-2 in a dose-dependent manner. In addition, DPB also inhibited LPS-induced production of inflammatory cytokines, including TNF-α, IL-1β, IL-6. Moreover, we further investigated signal transduction mechanisms by which DPB exerted anti-inflammatory effects. DPB could affect LPS-mediated nuclear factor kappa B (NF-κB) signaling pathway activation via down-regulating the upstream myeloid differentiation protein 88 (MyD88) at the protein level. Additionally, DPB also strongly inhibited the phosphorylation of mitogen-activated protein kinases (MAPKs), including extracellular signal-regulated kinase (ERK) 1/2, c-Jun N-terminal kinase (JNK) and p38. Therefore, DPB might exert anti-inflammatory effects by suppressing NF-κB activation and MAPKs pathways via down-regulating MyD88 in RAW 264.7 cells.

Analysis of anti-infection therapeutic schedule analysis for neonatal Streptococcus agalactiae meningitis and discussion on the indications for drug withdrawal

Haiyan Wu, Tao Wang, Qian Wang, Lin Tang

2021, 30(8): 686-691. DOI: 10.5246/jcps.2021.08.056

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The clinical manifestations of neonatal GBS meningitis are as follows: non-specificity, long hospital stay, easy to cause neurological complications, and sequelae. Clinical pharmacist participated in the anti-infective treatment of a neonatal Streptococcus agalactiae meningitis whose cerebrospinal fluid was still abnormal when the drug was stopped. According to the PK/PD characteristics of antibacterial drugs, the permeability of the blood-brain barrier, and the adjustment of the antibiotic dose, the reasons for the decrease in the number of cerebrospinal fluid cells after vancomycin treatment were analyzed. Clinical pharmacists also analyzed the efficacy of linezolid in the treatment of neonatal bacterial meningitis, and discussed the indications for stopping medication when the cerebrospinal fluid is abnormal, so as to improve the safety and effectiveness of antibiotics in the treatment of neonatal bacterial meningitis.

Effects of linagliptin on inflammatory factors and arteriosclerosis in patients with newly diagnosed type 2 diabetes mellitus

Rui Li, Yanru Kong

2021, 30(8): 692-698. DOI: 10.5246/jcps.2021.08.057

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In the present study, we aimed to investigate the effects of linagliptin on inflammatory factors and carotid intima-media thickness (CIMT) in newly diagnosed type 2 diabetes mellitus (T2DM) patients with carotid atherosclerotic disease (CAD). A total of 326 patients with newly diagnosed T2DM complicated with CAD were randomly divided into two groups. There were 163 patients in the control group, who were treated with metformin monotherapy. There were 163 patients in the experimental group, who were treated with metformin in combination with linagliptin. The CIMT before and after treatment was measured by color Doppler ultrasound, and the contents of IL-6 and IL-1β before and after treatment were detected by ELISA. The levels of inflammatory factors and CIMT before and after treatment were compared between the two groups, and the correlation between IL-6, IL-1β and CIMT was studied. After 24 weeks of treatment, the levels of inflammatory factors and CIMT in the experimental group were significantly lower compared with the control group (P < 0.01), and the serum levels of IL-6 and IL-1β were positively correlated with CIMT. In the present study, we concluded that linagliptin could improve the levels of inflammatory factors and CIMT in newly diagnosed T2DM patients with CAD, and IL-6 and IL-1β might participate in the occurrence and development of CAD by influencing CIMT.

The research group of Professor Qing Xia has developed gene codon extension technology to treat nonsense mutation rare diseases

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center

2021, 30(8): 699-700.

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