In-vitro antioxidant,in-vivo anti-inflammatory,and acute toxicity study of Indonesian propolis capsule from Tetragonula sapiens

Propolis is widely used as traditional medicine since ancient times. It was necessary to conduct the pre-clinical study because of its relevant curative properties. This study aimed to investigate in-vitro antioxidant, standardize quality parameters, study acute toxicity, and determine in-vivo anti-inflammatory. Three spectrophotometric methods were used to determine antioxidant activity. The standardization includes physical, chemical, and microbiological evaluation. Furthermore, an acute toxicity test was conducted using 20 female Sprague Dawley (SD) strain rats divided into 4 groups with different dose of propolis. The in vivo anti-inflammatory test was carried out using the carrageenan induction method on rats' soles. A total of 36 female SD rats were classified into 6 groups as follows, Group normal, negative control, diclofenac sodium, and three propolis groups (72; 144; and 288 mg/kg BW). The results demonstrated the IC₅₀ values of the DPPH and ABTS scavenging activity 9.694 ppm and 2.213 ppm, respectively. The FRAP reducing power was 189.05 mg AaE/g. The physical appearance of propolis capsule was vegicaps as white – white, size 0, with light brown granule. Moreover, the content weight was 418.88 mg with a disintegration time of 7 min 53 s, while the water, flavonoid, and polyphenol contents were 9.07%, 1.59%, and 98.0821 mg GAE/g respectively. The content of heavy metal and microbial contamination were not detected. The acute toxicity results showed LD₅₀ ≥ 5 g/kg BW, no toxicity symptoms, and no abnormalities in all rats. The anti-inflammatory inhibition percentage for groups III, IV, V, and VI was 11.86%, 6.53%, 7.81%, and 6.63% respectively, while the anti-inflammatory drugs effectiveness percentage compared to positive controls were 55.00%, 65.83%, and 55.83% respectively. Based on these results, it can be concluded that propolis capsules fulfilled the standardization requirements, and it is likely to be non-toxic, and effective as antioxidant and anti-inflammatory.     

Inhibitory effect of resveratrol dimerized derivatives on nitric oxide production in lipopolysaccharide-induced RAW 264.7 cells

Four types of resveratrol dimerized analogues were synthesized and evaluated in vitro on LPS-induced NO production in RAW 264.7 cells. The results showed that several compounds, especially those containing 1,2-diphenyl-2,3-dihydro-1H-indene core (type I), exhibited good inhibitory activities. Among 25 analogues, 12b showed a significant inhibitory activity (49% NO production at 10 μM, IC₅₀ = 3.38 μM). Further study revealed that compound 12b could suppress LPS-induced iNOS expression, NO production, and IL-1β release in a concentration-dependently manner. The mechanism of action (MOA) involved for its anti-inflammatory responses was through signaling pathways of p38 MAPK and JNK1/2, but not ERK1/2.     

Recent advances in marine drug research

Structures and properties of promising marine anti-cancer, anti-inflammation and anti-infectious (HIV, HSV, malaria, leishmania) compounds reported during 2008–2011 are discussed. Wherever possible, attempts have also been made to highlight their possible biogenesis or structure–activity relationships (SAR). Since the stress is on identifying and short-listing potential drug molecules, this review is restricted to only those compounds exhibiting promising in vitro activity, the arbitrary cut off being IC₅₀ < 15 μM, reported during the above period.     

Adenostemmoic acid B suppresses NO production by downregulating the expression and inhibiting the enzymatic activity of iNOS

Adenostemmoic acid B (AB) is a major compound found in Adenostemma lavenia; it shows anti-melanogenic, anti-inflammatory, and cytotoxic activities. By modifying the 19th position (carboxy: involved in the avoidance of cytotoxicity) of AB, we succeed to separate these activities. Short-chain alkylation of the carboxy group enhanced anti-melanogenic activity, while long-chain alkylation (hydrophobic) resulted in the suppression of nitric oxide (NO) production and inducible NO synthase (iNOS) expression without anti-melanogenic activity. Re-modification of hydrophilic properties in these long-chain derivatives restored anti-melanogenic activity but did not suppress NO production. Unexpectedly, AB and derivatives with long chains linked by an anhydride bond were new iNOS inhibitors. These results suggest that AB modulates multiple physiological activities by regulating different targets, including iNOS.     

小茴香挥发油的抗炎镇痛作用

目的:研究小茴香挥发油的抗炎、镇痛作用,为指导临床合理用药提供科学依据。方法:应用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足肿胀2种动物模型进行抗炎药效学实验;采用醋酸致小鼠扭体反应进行镇痛实验。结果:小茴香挥发油能显著抑制上述各种动物模型的炎症反应及醋酸引起的小鼠扭体反应。结论:小茴香挥发油具有抗炎和镇痛作用。     

小茴香挥发油的抗炎镇痛作用

目的：研究小茴香挥发油的抗炎、镇痛作用,为指导临床合理用药提供科学依据。方法：应用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足肿胀2种动物模型进行抗炎药效学实验;采用醋酸致小鼠扭体反应进行镇痛实验。结果：小茴香挥发油能显著抑制上述各种动物模型的炎症反应及醋酸引起的小鼠扭体反应。结论：小茴香挥发油具有抗炎和镇痛作用。     

中医药的抗炎机制在治疗肝纤维化中的作用

肝脏是人体腹腔内最大的实体器官,对维持机体的基本生理功能起着至关重要的作用。肝脏疾病是威胁人类健康的常见病多发病。全球约有10%人口受到不同程度的肝脏疾病的危害,其中,肝纤维化往往成为这些疾病的晚期病理特征。由于肝纤维化的发病机制复杂,尚无有效的合成类药物能够治疗肝纤维化。中药治疗肝纤维化具有多靶点和副作用小的优势。本文综述了肝纤维化的病理特征与诱发炎症的关系,讨论了中药治疗肝纤维化的单味中药、传统配方及其化学活性成分的抗炎症机制。     

Violacin A,a new chromanone produced by Streptomyces violaceoruber and its anti-inflammatory activity

A new chromanone derivative, named violacin A (1), was isolated from the fermentation broth of Streptomyces violaceoruber as a potential anti-inflammatory compound. The structure of violacin A was established using comprehensive NMR spectroscopic data analysis together with UV, IR, and MS data. The anti-inflammatory effects and action mechanisms of violacin A were investigated in vitro. The results demonstrated that violacin A attenuated the production of NO, IL-1β, IL-6, and TNF-α as well as inhibited the expression of iNOS in LPS-induced RAW 264.7 cells. Additionally, Western blot and qRT-PCR results revealed that 1 down-regulated pro-inflammatory cytokines expression correlated with the suppression of NF-κB signaling pathway.     

Activated protein C--an anticoagulant that does more than stop clots

Activated protein C (APC) is a glycoprotein derived from its precursor, protein C and formed by the cleavage of an activation peptide by thrombin bound to thrombomodulin. Originally thought to be synthesized exclusively by the liver, recent reports have shown that protein C is synthesized by endothelial cells, keratinocytes and some hematopoietic cells.APC functions as a physiological anticoagulant with cytoprotective, anti-inflammatory and anti-apoptotic properties. In vitro and preclinical data have revealed that APC exerts its protective effects via an intriguing mechanism requiring endothelial protein C receptor and the thrombin receptor, protease-activated receptor-1. Remarkably, even though APC cleaves this receptor in an identical fashion to thrombin, it exerts opposing effects.Recently approved as a therapeutic agent for severe sepsis, APC is now emerging as a potential treatment for a number of autoimmune and inflammatory diseases including lung disorders, spinal cord injury and chronic wounds. The future pharmacologic use of APC holds remarkable promise.     

Synthesis and anti-inflammatory activity of N-phthalimidomethyl 2,3-dideoxy- and 2,3-unsaturated glycosides

3,4,6-Tri-O-acetyl-D-galactal, 3,4,6-tri-O-acetyl-D-glucal and 3,6,2',3',4'6'-hexa-O-acetyl-D-lactal were reacted with N-hydroxymethylphthalimide and boron trifluoride etherate to produce the corresponding phthalimidomethyl unsaturated glycosides via Ferrier rearrangement. When the galactal derivative was used, a non-Ferrier rearrangement product was also isolated as a minor product under classical Ferrier conditions. Phthalimidomethyl deoxy glycosides were readily prepared by hydrogenation of the unsaturated glycosides. Following deacetylation, the anti-inflammatory activities of these compounds were tested on mice and three were found to possess potent activity compared to hydrocortisone sodium succinate (HSS).