Visible-Light-Initiated Catalyst-Free Radical Annulation Reactions of 1,6-Enynes and Aryl Sulfonyl Bromide to Assemble Sulfonation/Bromination Succinimide Derivatives.

In the present study, the environment-friendly visible-light-promoted strategy is used to perform an efficient, simple, and straightforward photocatalytic succinimide derivative synthesis from the reaction of 1,6-enynes and aryl sulfonyl bromide at room temperature under air ambient conditions. This method features mild conditions, broad substrate scope, high yields, and excellent configurational selectivity. In addition, all the atoms of the substrates involved in the reaction converge in the product structures, showing a high atomic economy. Moreover, the most important characteristic of this study is that no photocatalyst and additives are used, while the key factor that triggers the reaction is visible light, indicating that this study has an important practical value.

Construction of Spiro[benzo[a]acridine-12,4'-imidazolidine]-2',5'-dione Derivatives via Ring-Opening and Recyclization of Isatins and C-OH Cleavage of 2-Naphthol.

An efficient three-component reaction to access spiro[benzo[a]acridine-12,4'-imidazolidine]-2',5'-dione derivatives has been developed through the ring-opening and recyclization process of isatins and dehydroxylation of 2-naphthol, which is different from their conventional reaction modes. Experimental observations suggest that p-toluenesulfonic acid is the key factor that promotes the success of this synthetic strategy. The research provided a novel approach for the construction of spiro compounds from isatins and 2-naphthol in organic synthesis.

Modified cornstalk biochar can reduce ammonia emissions from compost by increasing the number of ammonia-oxidizing bacteria and decreasing urease activity.

This study examined how the addition of modified cornstalk biochar (CB) affected ammonia (NH3) emissions during composting. Four treatments were established, including a control (CK) with layer manure and sawdust only, and the CK mixtures adding 10% HNO3 CB (NA), 10% H2O2 CB (HP) and 10% HNO3- H2O2 CB (MI). As the results showed, NH3 emissions was reduced by 47.83% (NA), 61.69% (HP) and 45.69% (MI) when the modified CB used as a compost additive (P < 0.05). According to the data analysis, the addition of modified CB significantly increased the number of ammonia-oxidizing bacteria (AOB), inhibited urease activity and decreased the abundance of narG and nirS at rising temperatures and high temperatures (P < 0.05). Redundancy analysis demonstrated a negative correlation between NH3 emissions and AOB and a positive correlation with urease activity, narG and nirS. Thus, the modified CB helped reduce NH3 emissions by regulating nitrification processes.

How to continue lipid-lowering therapy in patients with coronary heart disease and severe liver dysfunction?: A case report of plaque regression by a combination of Chinese and Western Medicine.

RATIONALE: Atherosclerotic cardiovascular disease (ASCVD), including coronary heart disease (CHD), atherosclerotic stroke and peripheral vascular disease, has become the most deadly chronic noncommunicable disease throughout the world in recent decades, while plaque regression could reduce the occurrence of ASCVD. Traditional Chinese Medicine (TCM) has been widely used for prevention and treatment of these diseases. In the perspective of TCM, phlegm and blood stasis are considered to be leading pathogenesis for CHD. Hence, activating blood circulation and dissipating phlegm, which is of great benefit to regress plaque, have been regarded as general principles in treatment. PATIENT CONCERNS: A 36-year-old man presented with a 3-month history of intermittent exertional chest pain. Coronary angiography revealed 60% stenosis of the proximal left anterior descending coronary artery. Liver function showed: alanine transaminase (ALT):627U/L, aspartate transaminase (AST):243U/L. DIAGNOSES: CHD and hepatitis B with severe liver dysfunction. INTERVENTIONS: The patient should have been treated with high-intensity statin therapy. Actually, due to severe liver dysfunction, Huazhirougan granule instead of statins was administered. In addition, he was treated with TCM according to syndrome differentiation for two and a half years. OUTCOMES: The chest pain disappeared and other symptoms alleviated as well after treatment. Coronary computed tomographic angiography revealed no stenosis in the proximal left anterior descending coronary artery. ALT and AST level returned to normal (ALT:45U/L,AST:24U/L). LESSONS: For patients with CHD and severe hepatic dysfunction, antilipidemic drugs such as statins are not recommended. This case suggested that TCM might fill a gap in lipid-lowering therapy. Thus, we could see that statins were not the only drug for plaque regression and the effect of TCM in treating coronary artery disease cannot be ignored.

Chinese Patent medicine to treat a 32-year-old man with sinus bradycardia and cardiac sinus arrests: A case report.

RATIONALE: Sinus bradycardia refers to a sinus heart rate <60 bpm. Cardiac sinus arrests refer to the omission of atrial activation caused by transient cessation of impulse generation at the sinoatrial node. Normally, drugs such as atropine, isoproterenol, dopamine, dobutamine, or epinephrine can be used for the acute treatment of bradycardia. Temporary pacing is used for treating severe symptomatic bradycardia due to a reversible cause. Permanent cardiac pacing is used for chronic therapy of bradycardia. However, for traditional Chinese medicine (TCM), benefiting qi and nourishing yin and activating blood circulation is the general principle in treatment and show remarkable curative effects. PATIENT CONCERNS: A 32-year-old man was found to have 1-degree atrioventricular block and sinus bradycardia during a physical examination. He reported suffering from palpitation and shortness of breath occasionally. An ambulatory electrocardiogram showed sinus arrhythmia, sinus bradycardia, and significant sinus arrhythmia. The minimum heart rate was 33 bpm (beats per minute). The number of sinus arrest was 42 and the maximum RR interval was 2216 ms. DIAGNOSES: The patient was diagnosed with bradyarrhythmia in Western medicine and "palpitation" in TCM. INTERVENTIONS: The patient was treated with methods of benefiting qi and nourishing yin and activating blood circulation along with warming yan for nearly 5 months. CPM (Chinese patent medicine) such as Yixinshu capsule, Bingdouling oral liquid, Zhenyuan capsule, Zhibaidihuang pills were used for treatment. At the same time, he was suggested to change his lifestyles including falling asleep before 10:00 PM and abandoning spicy diets. OUTCOMES: The symptoms of palpitation and shortness of breath disappeared. The minimum heart rate increased from 33 to 42 bpm and sinus arrests did not occur. The maximum RR interval decreased from 2216 to 1650 ms and the remarkable sinus arrhythmia had improved obviously. LESSONS: This case report shows that TCM can be an effective alternative therapy for sinus bradycardia and cardiac sinus arrests. CPM may have been a successful intervention in arrhythmias.

Granule of BU-XIN RUAN-MAI Attenuates the Patients' Angina Pectoris of Coronary Heart Disease via Regulating miR-542-3p/GABARAP Signaling.

OBJECTIVE: Coronary heart disease (CHD) has been regarded as a serious and common disease in the modern society. This study aims to investigate the effect of Granule of BU-XIN RUAN-MAI (BXRM) on angina pectoris of coronary heart disease and to explore the molecular mechanisms underlying Granule of BU-XIN RUAN-MAI-mediated protective activity against this disease. METHODS: The effects of Granule of BU-XIN RUAN-MAI on clinical symptoms of patients' angina were indicated by hemorheology indicators including high shear of blood viscosity, low shear of blood viscosity, plasma viscosity, erythrocyte rigidity index, D-D dimer, fibrinogen content, and lipid content. The effects of Granule of BU-XIN RUAN-MAI on isoprenaline-induced myocardial cell injury were determined by conducting H&E staining and by performing ELISA to examine the serum content of MDA, SOD, Na+/K+-ATPase, cAMP, and the content of inflammatory factors in isoprenaline-induced rats. Meanwhile, western blot and real time PCR were used to determine the expression of genes involved in oxidation and energy metabolism, and real time PCR was also used for determination of miR-542-3p expression. Luciferase reporter assay was conducted to test the binding sites of miR-542-3p on GABARAP 3'UTR. The chemical compositions of Granule of BU-XIN RUAN-MAI were determined by liquid LC-QTOF-MS. RESULTS: Granule of BU-XIN RUAN-MAI significantly attenuated the clinical symptoms of patients' angina by improving the patients' heart rate and by decreasing the level of hemorheology indicators and also by reducing the serum content of TC, TG, LDL, and elevated HDL content. H&E staining demonstrated that Granule of BU-XIN RUAN-MAI ameliorated the myocardial ischemia in a dose-dependent manner. Besides, Granule of BU-XIN RUAN-MAI downregulated serum MDA content and upregulated the content of SOD, Na+/K+-ATPase, and cAMP in isoprenaline-induced rats. Granule of BU-XIN RUAN-MAI significantly improved oxidation stress by increasing PPARα expression, and it inhibited inflammation by downregulating expression and contents of IL-6, IL-1ß, and TNF-α. Then, Granule of BU-XIN RUAN-MAI-containing serum increased the SOD content, and reduced the MDA content in angiotensin II-stimulated HUVEC cells. The granule of BU-XIN RUAN-MAI-containing serum obviously downregulated protein expressions of P40phox, P47phox, and P67phox in plasma membrane, and it significantly increased protein levels of P40phox, P47phox, and P67phox in the cytoplasm of HUVEC cells. Furthermore, GABARAP was reduced in heart tissues of ISO-induced rats and in angiotensin II-stimulated cell lines, and GABARAP was required for the inhibitory activity of Granule of BU-XIN RUAN-MAI on oxidation and inflammation in vivo and in vivo. GABARAP could be upregulated by Granule of BU-XIN RUAN-MAI by inhibiting the expression of miR-542-3p, which may significantly enhance oxidation and inflammation by targeting GABARAP in cardiomyocytes. Moreover, the silencing of GABARAP could obviously reverse the granule of BU-XIN RUAN-MAI-mediated protective activity against coronary heart disease, and interfering GABARAP expression also could partly block the anti-miR-542-3p-controlled oxidation and inflammation in cardiomyocytes. Besides, salidroside, loganin, and polydatin were the main compounds of granules of BU-XIN RUAN-MAI. CONCLUSION: Granule of BU-XIN RUAN-MAI is an excellent prescription for treatment of coronary heart disease by suppressing inflammation and NAPDH-mediated oxidative stress. The miR-542-3p/GABARAP axis is required for Granule of BU-XIN RUAN-MAI, exhibiting its protective activity against the pectoris of coronary heart disease.

JYYS Granule Mitigates Renal Injury in Clinic and in Spontaneously Hypertensive Rats by Inhibiting NF-κB Signaling-Mediated Microinflammation.

INTRODUCTION: Hypertensive renal damage is a chronic and life-threatening kidney disease all over the world. The traditional Chinese medicine Jiang Ya Yi Shen (JYYS) granule has been a perfect drug for patients with hypertensive renal injury in clinic for 20 years in China. However, the molecular mechanism of JYYS granule remains unknown in treatment of this disease. METHODS: The clinic data were from this study's patients. The clinical symptoms of patients were indicated by (N-Acetyl-ß-D-Glucosaminidase) NAG, (albumin) Alb, and (ß2-microglobin) ß2-MG content in urinary of patients, and renal artery's hemodynamic parameters including (pulse index) PI, mean velocity of the arterial blood (Vm), minimum velocity of the diastolic stage (Vdmin) and peak velocity of the systolic wave (Vsmax). To further observe the effect of JYYS granule on renal damage, the rats were included in six groups: normal rats (WKY), spontaneously hypertensive rats (SHR), positive drug-treated rats (Benazepril), low dose JYYS (L), middle dose JYYS (M), and high dose JYYS (H). Then, we observed the effect of JYYS on renal function, renal tubules, inflammatory cell infiltration, and small artery thickening, and we explored the potential mechanism of JYYS in treatment of renal injury. RESULTS: JYYS significantly improved the clinic symptoms of patients with hypertensive nephropathy by downregulating NAG, Alb, and ß2-MG content in urinary of patients and by decreasing renal artery's hemodynamic parameters including PI, Vm, Vdmin, and Vsmax. In SHR, JYYS significantly improved renal function including creatinine clearance rate, urinary albumin/creatinine, ß2-MG/creatinine and arteria caudalis pressure in SHR. Secondly, light and electron microscopic examinations told that after administration of JYYS and Benazepril, the mesangial region exhibited no hyperplasia and renal capsule did not expanded, and there no abnormalities were observed in renal tubules, inflammatory cell infiltration and small artery thickening in SHR. Thirdly, JYYS exhibited its protective role by inhibiting nuclear factor kappa beta signaling-mediated micro-inflammation cytokines including interleukin 6 (IL-6), tumor necrosis factor α (TNF-α), intercellular cell adhesion molecule-1 (ICAM-1), and monocyte chemotactic protein 1 (MCP-1) in SHR. CONCLUSION: JYYS is a promising prescription of Chinese medicine for patients with hypertension and hypertensive renal damage.