Phytotherapy Research

The antiulcerogenic effect of two flavonoids, quercetin and naringenin, in acute gastric ulcer (cold‐restraint and pylorus‐ligated) has been investigated. In both models quercetin and naringenin presented a significant decrease in ulcer index with respect to the control group. Nevertheless, in the Shay‐ligated method no decrease in either volume, acidity or pepsin were observed, however, a significant difference was found in histamine secretion values.

Cnidium monnieri(L.) Cusson is a Chinese medicine which is used widely by traditional medicine doctors. Osthol is a major bio‐activity compound of the herb. In this study, osthol was isolated fromC. monnieriand itsin vitroandin vivoantitumor effects studied. The results of thein vitrostudy showed: that osthol inhibited the growth of HeLa, in a time‐ and concentration‐dependent manner, with IC₅₀values of 77.96 and 64.94 µmfor 24 and 48 h, respectively; that osthol had lower cytotoxic effects in primary cultured normal cervical fibroblasts; and that increased DNA fragmentation and activated PARP in HeLa after treatment with osthol which could induce apoptosis. The results of thein vivomodel showed that the survival days of the P‐388 D1 tumor‐bearing CDF₁mice were prolonged (ILS% = 37) after osthol (30 mg/kg) was given once a day for 9 days. Based on these results, it is suggested that osthol could inhibit P‐388 D1 cellsin vivoand induce apoptosis in HeLa cellsin vitro, and that osthol is good lead compound for developing antitumor drugs. However,C. formosanumYabe of Taiwan's endemic plants contained little osthol, with no imperatorin, and its major components were different from that ofC. monnieri. Therefore, it is suggested thatC. formosanumalso may possess economic worth. Copyright © 2006 John Wiley & Sons, Ltd.

Despite the high levels of polyphenolic phytochemicals in grain sorghum and its position as a major food staple, there has been a lack of research on its effects on both animal and human health and disease prevention. These phenolic compounds, mainly located in the bran fraction, result in the plant having substantial antioxidant properties. This study examined the effect of ethanol extracts of several varieties of sorghum (S. bicolor) bran on albumin glycation, a non‐enzymatic process thought to be important in the pathogenesis of many diabetic complications. Sorghum brans with a high phenolic content and high antioxidant properties inhibited protein glycation, whereas sorghum brans that are low in these properties did not inhibit this process. Ethanol extracts of wheat, rice or oat bran did not inhibit protein glycation. Although one high phenolic sorghum bran variety (sumac) inhibited protein glycation by approximately 60%, it produced only a 20% decrease in methylglyoxal mediated albumin glycation. These results suggest that certain varieties of sorghum bran may affect critical biological processes that are important in diabetes and insulin resistance. These results distinguish select sorghum brans from the common food brans and suggest a nutraceutical rationale for its human consumption. Copyright © 2008 John Wiley & Sons, Ltd.

Garlic is widely used as a spice. Garlic extracts exert anticancer and antiinflammatory effects, but its antiobesity efficacy studies have produced conflicting results. The antiobesity effects of thiacremonone, a sulfur compound isolated from garlic, was evaluated in obese db/db mice. Thiacremonone was orally administrated to mice for 3 weeks. The thiacremonone‐treated db/db mice showed a loss of body weight and decrease in blood triglyceride and glucose levels compared with the control mice. Histological analysis further revealed that thiacremonone significantly decreased lipid accumulation in the fatty livers of treated db/db mice. It was observed that GLUT‐4 expression and glucose uptake were up‐regulated by thiacremonone in 3T3‐L1 adipocytes. Thiacremonone treatment also suppressed expression levels of acetyl‐CoA carboxylase (ACC) and fatty acid synthase (FAS), which are involved in lipid metabolism, in the liver of db/db mice. In addition, thiacremonone enhanced peroxisome proliferator‐activated receptor γ (PPARγ) expression in the fatty liver. Taken together, these results suggest that thiacremonone may play a vital role in improving the management of obesity and related metabolic syndromes via inhibition of lipid accumulation. Copyright © 2012 John Wiley & Sons, Ltd.

Scopoletin is a bioactive component in many edible plants and fruits. This study investigated the effects of scopoletin on hepatic steatosis and inflammation in a high‐fat diet fed type 1 diabetic mice by comparison with metformin. Scopoletin (0.01%, w/w) or metformin (0.5%, w/w) was provided with a high‐fat diet to streptozotocin‐induced diabetic mice for 11 weeks. Both scopoletin and metformin lowered blood glucose and HbA_1c, serum ALT, TNF‐α and IL‐6 levels, glucose intolerance, and hepatic lipid accumulation compared with the diabetic control group. Scopoletin or metformin down‐regulated hepatic gene expression of triglyceride (Pparg, Plpp2, and Dgat2) and cholesterol (Hmgcr) synthesis as well as inflammation (Tlr4, Myd88, Nfkb1, Tnfa, and Il6), while it up‐regulated Cyp7a1 gene. Hepatic PPARγ and DGAT2 protein levels were also down‐regulated in scopoletin or metformin group compared with the control group. Scopoletin or metformin also inhibited hepatic fatty acid synthase and phosphatidate phosphohydrolase activities. These results suggest that scopoletin protects against diabetes‐induced steatosis and inflammation by inhibiting lipid biosynthesis and TLR4‐MyD88 pathways. Copyright © 2017 John Wiley & Sons, Ltd.

Diabetes is the most prevalent disorder in the world characterized by uncontrolled high blood glucose levels and nephropathy is one of the chief complications allied with hyperglycemia. Vanillic acid; the main bioactive compound derived from natural sources such as vegetables, fruits and plants possesses various pharmacological activities such as antioxidant, anti‐inflammatory and anti‐proliferative. The current study was designed to investigate the antidiabetic and renoprotective effects of vanillic acid by its various pharmacological activities. Streptozotocin (50 mg/kg)/nicotinamide (110 mg/kg) was used to induce diabetes in rats. Oral administration of vanillic acid once daily for 6 weeks (25, 50 and 100 mg/kg) significantly reduced the hyperglycemia, increased liver enzymes and normalized lipid profile that was altered in diabetic rats. Moreover, vanillic acid attenuated the impaired renal function as evidenced by a reduction in serum creatinine, urea, uric acid and urinary microproteinuria levels with a concomitant increase in urinary creatinine clearance in the nephropathic rats. Diabetic rats showed a marked increase in thiobarbituric acid reactive substances (TBARS) and superoxide anion generation (SAG) along with decreased reduced glutathione (GSH) in the renal tissue which was ameliorated in the vanillic acid‐treated rats. Histopathologically, vanillic acid treatment was associated with reduced damage with normalized structural changes in renal tissue. Furthermore, treatment groups showed the suppression of upregulation of nuclear factor (NF)‐κB, tumor necrosis factor (TNF)‐α, cyclo‐oxygenase (COX)‐2 and up‐regulation of Nuclear factor‐erythroid 2‐related factor 2 (Nrf‐2) in the renal tissue. In conclusion, vanillic acid's ameliorative impact on diabetic nephropathic rats may be attributed to its powerful free radical scavenging property, down‐regulation of NF‐κB, TNF‐α, COX‐2 and up‐regulation of Nrf‐2 proteins in renal tissue.

Chúng tôi đã điều tra ảnh hưởng của chiết xuất nước từ hoa khô của Hibiscus sabdariffa L. và anthocyanins (HAs) của Hibiscus (một nhóm sắc tố tự nhiên có trong bao calyx khô của H. sabdariffa) đối với độc tính gan do paracetamol gây ra ở chuột. Chiết xuất nước được cung cấp thay cho nước uống trong 2, 3 hoặc 4 tuần liên tiếp, và HAs được cho uống với các liều 50, 100 và 200 mg/Kg trong năm ngày liên tiếp. Paracetamol được cho uống với liều 700 mg/Kg để gây độc tính gan vào cuối quá trình điều trị bằng chiết xuất nước và HAs. Sáu giờ sau đó, chuột được giết thịt và chức năng gan của chúng được đánh giá qua các xét nghiệm sinh hóa và mô học. Sau 4 tuần sử dụng (nhưng không phải 2 hoặc 3 tuần), chiết xuất đã cải thiện đáng kể một số xét nghiệm chức năng gan, nhưng không làm thay đổi mô học của các chuột được điều trị bằng paracetamol hoặc thời gian ngủ do pentobarbiton gây ra. Ở liều 200 mg/Kg, mô học gan và các chỉ số sinh hóa cho thấy tổn thương gan được phục hồi về mức bình thường. Liều thấp hơn không có tác dụng. Chờ thêm đánh giá về độ an toàn và hiệu quả, HAs có khả năng được sử dụng trong việc làm giảm độc tính gan do paracetamol gây ra.

Bacterial adhesion to the cell surface is a crucial step before infection can take place. Inhibition of bacterial binding offers a novel preventive approach against infections. Cranberry (Vaccinium macrocarpon Ait.) juice has been found to have antiadhesive activity against different bacteria. Streptococcus pneumoniae is an important pathogen and the most common cause for pneumonia, meningitis, and otitis media. In this study the inhibitory activity of cranberry (Vaccinium oxycoccos L.), bilberry (Vaccinium myrtillus L.) and crowberry (Empetrum nigrum and Empetrum hermaphroditum L.) juice fractions against pneumococcal binding was tested using human bronchial cells (Calu‐3) as an adhesion model. In addition, the antimicrobial activity of the berry juice fractions was tested. It was found that the studied berry juice fractions had antiadhesion activity and cranberry juice was the most active. The adhesion inhibition activity of cranberry juice was nearly 90% at a concentration of 8.7 mg/g of soluble solids. The antimicrobial activity of the studied berry juice fractions was found to be remarkable; pneumococcal growth was inhibited totally at a concentration of ∼86 mg/g. Both antiadhesion and antimicrobial activities were reduced after solid‐phase extraction of the berry juices, which may suggest molecular synergistic effects of the berry juice molecules against S. pneumoniae. The findings indicate that cranberry, bilberry and crowberry juices have potential against pneumococcal infections.

Kaempferide (KF) is a compound of flavonoids from Alpinae oxyphylla Miq, and the herb itself is used as a classical tonic agent. This paper aims to investigate the effects of KF on cognitive function impairment and neurodegeneration in the mouse model of Alzheimer's disease induced by intracerebroventricular (ICV) injection of Aβ_1–42. The mice were treated with KF at doses of 0.02 and 0.2 mg/kg/day (ICV) for five consecutive days after Aβ_1–42 exposures. The behavioral test results showed that KF could prevent cognitive decline in mice induced by Aβ_1–42 as assessed by the locomotor activity test, Y‐maze test, and Morris water maze test. Furthermore, the activities of superoxide dismutase and malondialdehyde in the hippocampus and cerebral cortex were elevated by KF administration. Results of hippocampus slices showed that neurons were integrated and regularly arranged in the groups, which were administered along with KF. In addition, we found KF could boost brain‐derived neurotrophic factor (BDNF)/tropomyosin receptor kinase B (TrkB)/cAMP response element‐binding (CREB) protein signal in the hippocampus. All results illustrated that KF could exert neuroprotective effects at least partly through alleviating oxidative stress and enhancing the BDNF/TrkB/CREB pathway in Aβ_1–42‐induced mice.

Given the evidence for detoxifying/antioxidant enzyme‐inducing activities by alantolactone (AL) and isoalantolactone (IAL), the purpose of this study was to investigate the effects of AL and IAL on Aβ_25–35‐induced cell death in mouse cortical neuron cells and to determine their effects on scopolamine‐induced amnesia in mice. Our data demonstrated that both compounds effectively attenuated the cytotoxicity of Aβ_25–35 (10 μM) in neuronal cells derived from the mouse cerebral cortex. It was also found that the production of intracellular reactive oxygen species, including superoxide anion induced by Aβ_25–35, was inhibited. Moreover, the administration of the sesquiterpenes reversed scopolamine‐induced cognitive impairments as assessed by Morris water, Y‐maze, and the passive avoidance tests, and the compounds decreased acetylcholinesterase (AChE) activities in a dose‐dependent manner. Interestingly, AL and IAL did not improve scopolamine‐induced cognitive deficit in Nrf2^−/− mice, suggesting that memory improvement by sesquiterpenes was mediated not only by the activation of the Nrf2 signaling pathway but also by their inhibitory activity against AChE. In conclusion, our results showed that AL and IAL had neuroprotective effects and reversed cognitive impairments induced by scopolamine in a mouse model. Therefore, AL and IAL deserve further study as potential therapeutic agents for reactive oxygen species‐related neurodegenerative diseases. Copyright © 2017 John Wiley & Sons, Ltd.