Anti-acetylcholinesterase activity of the aglycones of phenolic glycosides isolated from Leonurus japonicus

Objective: To find the genuine structure with anti-acetylcholinesterase(anti-AChE)from the phenolic glycosides abundant in Leonurus japonicus(Lamiaceae).The assay for anti-AChE activity is often used to lead anti-Alzheimer's drugs. Methods: The five phenolic glycosides, tiliroside, leonurusoside C, 2'''-syringoylrutin, rutin, and lavanduliofolioside were isolated from L. japonicus. The activities of the glycosides were relatively low. Seven compounds including p-coumaric acid, caffeic acid, hydroxytyrosol, salidroside, syringic acid, kaempferol, and quercetin, which are produced by the hydrolysis of the five glycosides, were also assayed for anti-AChE activity. Results: Of those seven compounds, the five compounds other than salidroside and syringic acid exhibited potent anti-AChE activities.In particular,the IC50s of caffeic acid and quercetin were (1.05 ± 0.19)and (3.58 ± 0.02)μg/mL, respectively. Rutin was the most abundant flavonoid in the extract(9.18 mg/g as measured by HPLC). Conclusion: The substances with potent anti-AChE were caffeic acid, quercetin, p-coumaric acid, kaempferol, and hydroxytyrosol that can be produced from their glycosides.

Blood Glucose Reduction by Combination of Andrographis paniculata (Burm. f.) Ness Herbs and Azadirachta indica A. Juss Leaves in Alloxan-Induced Diabetic Rats.

Andrographis paniculata (Burm. f.) Ness and Azadirachta indica A. Juss are Indonesian local plants that are potentially developed as antihyperglycemic agents. This study was aimed to explore antihyperglycemic effect of herbal extract combination of A. paniculata (Burm. f.) Ness and A. indica A. Juss in alloxan-induced rats compared to single extract treatment. Diabetic condition was induced with an intraperitoneal injection of 150 mg/kgBW alloxan monohydrate in the rats. After stable diabetic condition, the rats were administered either with single or extract combination for 15 consecutive days. Blood glucose profiles in both preprandial and postprandial were monitored at the day of 5, 10, and 15. Analysis of blood glucose level was performed using colorimetric method of GOD-PAP. In the study, preprandial and postprandial blood glucose levels of alloxaninduced rats could be decreased after administration of the herbal extract combination of A. paniculata (Burm. f.) Ness and A. indica A. Juss. The extract combination exhibited higher hypoglycemic effects than this of the single extract treatment. In conclusion, the combination of A. paniculata (Burm. f.) Ness and A. indica A. Juss is potential to develop as an antidiabetic agent.

Predictors of Unachieved LDL Levels in Ischemic Stroke Patients Treated with Statins in Yogyakarta Indonesia.

Ischemic stroke occurs due to barriers in cerebral vascular. The barriers are manifestation of atherosclerosis formation. Statins are widely used in patients with high level of LDL. The aim of the study was to investigate the factors that influence the Unachieved LDL levels in ischemic stroke patients treated with statin. The study was an analytical research performed using a nested case-control study. The subjects were ischemic stroke patients based on inclusion criteria, and treated with statin. The patients were classified into case group if the result of medical record and the stroke register showed the LDL level of the patients was >100 mg/dL. Whereas the ischemic stroke patients with LDL level <100 mg/dL were classified into control group. Clinical characteristics were investigated in the study including gender, age, comorbid conditions, co-medication, initial LDL levels, amount of comorbid and characteristics of statin treatment. The results were then analyzed using bivariate and multivariate analysis. In the study, 236 patients of ischemic stroke met the inclusion criteria. The results showed that patients with highest initial LDL level (p=0.003; OR=2.618; CI95%=1.398 – 4.904) and patients with more than one comorbid (p=0.006; OR=3.058; CI95%=1.376 – 6.796) had the most significant contributions on Unachieved LDL level. However, gender, age, comorbid conditions, co-medication, and characteristics of statin treatment did not have specific contribution on Unachieved LDL level. The predictor factors that play significant role in Unachieved LDL level in ischemic stroke patients were patients with a very high initial LDL level (≥190 mg/dL) and patients with one more than comorbid.

Anti-diabetic effect of a combination of andrographolide-enriched extract of Andrographis paniculata (Burm f.) Nees and asiaticoside-enriched extract of Centella asiatica L. in high fructose-fat fed rats.

Traditionally, a combination of medicinal plants is commonly used for lowering blood glucose in diabetic patients in order to provide additional benefits of the single drug. A. paniculata and C. asiatica are two traditional medicines form South Asian and Southeast Asain countries consumed by people for treating daibates mellitus and its complications. Hyperglycemia in the rats was stimulated by high fructose-fat diet that consists of 36% fructose, 15% lard, and 5% egg yolks in 0.36 g/200 g body weight for 70 days. The rats were orally administered with the combination of andrographolide-enriched extract of A. paniculata (AEEAP) leaves and asiaticoside-enriched extract of C. asiatica (AEECA) herbs from day 70 for 7 days. Antidiabetic activity was evaluated by estimating mainly the blood glucose levels and other parameters such as HDL, LDL, cholesterol and triglyceride. The results showed that combination at the ratio of 70:30 exhibited a promosing antidiabetic effect in high-fat-fructose-fed rat, and exhibited sinergistic effects on blood cholesterol and HDL levels. It can be concluded that its antidiabetic effect was better than that of single treatment of AEEAP or AEECA. That combination was also potential to develop as a blood glucose-lowering agent for diabetic patients.

Quinine-induced arrhythmia in a patient with severe malaria.

It was reported that there was a case of severe malaria patient with jaundice who presented with arrhythmia (premature ventricular contraction) while getting quinine infusion was reported. A man, 25 years old, was admitted to hospital with high fever, chill, vomiting, jaundice. The patient was fully conscious, blood pressure 120/80 mmHg, pulse rate 100 x/minute, regular. On admission, laboratory examination showed Plasmodium falciparum (++++), total bilirubin 8.25 mg/dL, conjugated bilirubin 4.36 mg/dL, unconjugated bilirubin 3.89 mg/dL, potassium 3.52 meq/L Patient was diagnosed as severe malaria with jaundice and got quinine infusion in dextrose 5% 500 mg/8 hour. On the second day the patient had vomitus, diarrhea, tinnitus, loss of hearing. After 30 hours of quinine infusion the patient felt palpitation and electrocardiography (ECG) recording showed premature ventricular contraction (PVC) > 5 x/minute, trigemini, constant type--sinoatrial block, positive U wave. He was treated with lidocaine 50 mg intravenously followed by infusion 1500 mg in dextrose 5%/24 hour and potassium aspartate tablet. Quinine infusion was discontinued and changed with sulfate quinine tablets. Three hours later the patient felt better, the frequency of PVC reduced to 4 - 5 x/minute and on the third day ECG was normal, potassium level was 3.34 meq/L. He was discharged on 7th day in good condition. Quinine, like quinidine, is a chincona alkaloid that has anti-arrhythmic property, although it also pro-arrhythmic that can cause various arrhythmias, including severe arrhythmia such as multiple PVC. Administration of parenteral quinine must be done carefully and with good observation because of its pro-arrhythmic effect, especially in older patients who have heart diseases or patients with electrolyte disorder (hypokalemia) which frequently occurs due to vomiting and or diarrhea in malaria cases.