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Asiatic acid

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https://www.readbyqxmd.com/read/28053540/a-novel-synthetic-asiatic-acid-derivative-induces-apoptosis-and-inhibits-proliferation-and-mobility-of-gastric-cancer-cells-by-suppressing-stat3-signaling-pathway
#1
Gang Wang, Yue Jing, Lingsen Cao, Changchang Gong, Zhunan Gong, Xiangrong Cao
Activation of the transcription factor, signal transducers and activators of transcription 3 (STAT3), has been linked to the proliferation and migration of a variety of human cancer cells. These actions occur via the upregulation or downregulation of cell survival and tumor suppressor genes, respectively. Importantly, agents that can suppress STAT3 activation have the potential for use in the prevention and treatment of various cancers. In this study, an Asiatic acid (AA) derivative, N-(2α,3β,23-acetoxyurs-12-en-28-oyl)-l-proline methyl ester (AA-PMe), is reported to dose dependently suppress constitutive STAT3 activation in gastric cancer cells...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28004603/asiatic-acid-attenuates-pre-neoplastic-lesions-oxidative-stress-biotransforming-enzymes-and-histopathological-alterations-in-1-2-dimethylhydrazine-induced-experimental-rat-colon-carcinogenesis
#2
Aktarul Islam Siddique, Vijay Mani, Sivaranjani Arivalagan, Nisha Susan Thomas, Namasivayam Nalini
Asiatic acid (AA), a pentacyclic triterpenoid derived from the tropical medicinal plant Centella asiatica is known to exhibit numerous pharmacological properties. We hypothesized that AA will have chemopreventive potential against 1,2-dimethylhydrazine (DMH)-induced experimental colon carcinogenesis in male Wistar rats. Rats were arbitrarily divided into six groups. Group I rats were processed as control. Group II rats received AA (8 mg/kg b.w., p.o.) and groups III-VI rats received subcutaneous injections of DMH (20 mg/kg b...
December 22, 2016: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/28003581/triterpenes-suppress-octanoylated-ghrelin-production-in-ghrelin-expressing-human-gastric-carcinoma-cells
#3
Kensuke Nakajima, Shigeru Oiso, Takuhiro Uto, Osamu Morinaga, Yukihiro Syoyama, Hiroko Kariyazono
Ghrelin is an appetite-stimulating peptide hormone with an octanoyl modification at serine 3 that is essential for its orexigenic effect. Ghrelin O-acyltransferase (GOAT) is the enzyme that catalyzes ghrelin acylation using fatty acyl-coenzyme A as a substrate. We previously developed an assay system based on the AGS-GHRL8 cell line that produces octanoylated ghrelin in the presence of octanoic acid, and demonstrated that some fatty acids suppressed octanoylated ghrelin production. Recent studies have reported that triterpenes have anti-obesity effect...
2016: Biomedical Research
https://www.readbyqxmd.com/read/28001462/comparative-pharmacokinetics-between-madecassoside-and-asiaticoside-presented-in-a-standardised-extract-of-centella-asiatica-eca-233-and-their-respective-pure-compound-given-separately-in-rats
#4
Patcharaporn Hengjumrut, Tosapol Anukunwithaya, Mayuree H Tantisira, Boonyong Tantisira, Phisit Khemawoot
1. ECa 233, the standardised extract of Centella asiatica, contains not less than 80% triterpenoid glycosides, in a madecassoside:asiaticoside ratio of 1.5 (±0.5):1. 2. The pharmacokinetic comparison of madecassoside and asiaticoside was performed in rats following intravenous and oral administration of ECa 233, or an equivalent dose of the individual compounds. Blood, tissues, urine and faeces were collected after dosing to determine drug and metabolite levels using liquid chromatography-tandem mass spectrometry...
January 18, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27992940/pharmacokinetics-of-a-standardized-extract-of-centella-asiatica-eca-233-in-rats
#5
Tosapol Anukunwithaya, Mayuree H Tantisira, Boonyong Tantisira, Phisit Khemawoot
ECa 233, a standardized extract of Centella asiatica, has been found to exhibit various positive neurological effects and to have a good safety profile. The present study aimed to explore the disposition kinetics of ECa 233, containing madecassoside (53.1 %) and asiaticoside (32.3 %), in rats. The extract was intravenously or orally administered at doses from 50 to 200 mg/kg. Plasma, tissues, urine, and feces were collected at time points from 0 to 48 h after dosing. The levels of madecassoside and asiaticoside, as well as their postulated triterpenic metabolites, madecassic acid and asiatic acid, in biological samples, were simultaneously measured by liquid chromatography-tandem mass spectrometry...
December 19, 2016: Planta Medica
https://www.readbyqxmd.com/read/27955745/asiatic-acid-pectin-hydrogel-matrix-patch-transdermal-delivery-system-influences-parasitaemia-suppression-and-inflammation-reduction-in-p-%C3%A2-berghei-murine-malaria-infected-sprague-dawley-rats
#6
Greanious Alfred Alfrd Mavondo, Musabayane Cephas Tagumirwa
OBJECTIVE: To report the influence of transdermal delivery of asiatic acid (AA) in Plasmodium berghei-infected Sprague Dawley rats on physicochemical changes, %parasitaemia and associated pathophysiology. METHODS: A topical once-off AA (5, 10, and 20 mg/kg)- or chloroquine (CHQ)-pectin patch was applied on the shaven dorsal neck region of Plasmodium berghei-infected Sprague Dawley rats (90-120 g) on day 7 after infection. Eating and drinking habits, weight changes, malaria effects and %parasitaemia were compared among animal groups over 21 d...
December 2016: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/27893605/synergistic-combinations-of-five-single-drugs-from-centella-asiatica-for-neuronal-differentiation
#7
Jinjin Lin, Hui Jiang, Xianting Ding
To identify alternatives of nerve growth factor, which could promote NF68 protein expression and contribute toward neuronal differentiation, five compounds namely: asiatic acid, madecassic, madecassoside, quercetin, and isoquercetin, obtained from Centella asiatica, were examined for their neuronal differentiation effects on PC12 cells. C. asiatica has been applied as an effective herbal medicine for the treatment of various diseases, including depression. According to a statistical design of experiments, both single compound and compound combinations were evaluated...
January 1, 2017: Neuroreport
https://www.readbyqxmd.com/read/27852215/transcriptome-analysis-revealed-the-dynamic-oil-accumulation-in-symplocos-paniculata-fruit
#8
Qiang Liu, Youping Sun, Jinzheng Chen, Peiwang Li, Changzhu Li, Genhua Niu, Lijuan Jiang
BACKGROUND: Symplocos paniculata, asiatic sweetleaf or sapphire berry, is a widespread shrub or small tree from Symplocaceae with high oil content and excellent fatty acid composition in fruit. It has been used as feedstocks for biodiesel and cooking oil production in China. Little transcriptome information is available on the regulatory molecular mechanism of oil accumulation at different fruit development stages. RESULTS: The transcriptome at four different stages of fruit development (10, 80,140, and 170 days after flowering) of S...
November 16, 2016: BMC Genomics
https://www.readbyqxmd.com/read/27779647/asiatic-acid-inhibits-lactate-induced-cardiomyocyte-apoptosis-through-the-regulation-of-the-lactate-signaling-cascade
#9
Changzheng Gao, Fen Wang, Zhiqiang Wang, Jing Zhang, Xiangjun Yang
The lactate signaling cascade has recently been linked to mitochondrial energy metabolism and cardiomyocyte apoptosis in several cardiovascular diseases. Asiatic acid (AA) exhibits a variety of pharmacological effects, including antioxidant and anti-apoptotic effects. In this study, we investigated the protective effects of AA against the lactate-induced apoptosis of cardiomyocytes, as well as its mechanisms of action. Neonatal rat cardiomyocytes were pre-treated with 20 µM AA for 24 h, followed by exposure to 20 mM lactate for a further 24 h...
December 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/27762142/synthesis-structural-studies-and-cytotoxic-evaluation-of-novel-ursolic-acid-hybrids-with-capabilities-to-arrest-breast-cancer-cells-in-mitosis
#10
Banita Pattnaik, Jerripothula K Lakshmi, Rachineni Kavitha, Bharatam Jagadeesh, Debanjan Bhattacharjee, Nishant Jain, Uppuluri V Mallavadhani
Some novel chemically modified frameworks of ursolic acid have been designed and synthesized. The key step was the cycloaddition of azidopropyl-3β-hydroxy-urs-12-en-28-oate with the appropriate C28 propargyl esters of ursolic, corosolic, asiatic, oleanolic, and betulinic acid under Click reaction conditions, and the products were obtained in 74-84% yields. In view of their intriguing structural diversity, they have been subjected to detailed 1D and 2D NMR studies and their structures are thoroughly assigned...
October 20, 2016: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/27725350/cardiorespiratory-effects-of-isoflurane-in-asiatic-black-bears-ursus-thibetanus-anesthetized-with-intramuscular-medetomidine-and-zolazepam-tiletamine
#11
Dong-Hyuk Jeong, Jeong-Jin Yang, Seong-Hoon Seok, Dong-Joo Song, Seong-Chan Yeon
The objective of this study was to determine the dose-dependent effects of isoflurane on various cardiovascular parameters and the stable range of isoflurane concentrations in Asiatic black bears (Ursus thibetanus). Seven Asiatic black bears were intramuscularly injected with medetomidine, zolazepam, and tiletamine (MZT) to induce anesthesia and anesthesia was maintained by administering isoflurane in 100% oxygen (4 l/min) without mechanical ventilation. Several cardiovascular parameters were measured at five end-tidal isoflurane concentrations (0...
September 30, 2016: Journal of Veterinary Medical Science
https://www.readbyqxmd.com/read/27703505/computational-approach-for-predicting-the-conserved-b-cell-epitopes-of-hemagglutinin-h7-subtype-influenza-virus
#12
Xiangyu Wang, Qi Sun, Zhonghua Ye, Ying Hua, Na Shao, Yanli Du, Qiwei Zhang, Chengsong Wan
An avian-origin influenza H7N9 virus epidemic occurred in China in 2013-2014, in which >422 infected people suffered from pneumonia, respiratory distress syndrome and septic shock. H7N9 viruses belong to the H7 subtype of avian-origin influenza viruses (AIV-H7). Hemagglutinin (HA) is a vital membrane protein of AIV that has an important role in host recognition and infection. The epitopes of HA are significant determinants of the regularity of epidemic and viral mutation and recombination mechanisms. The present study aimed to predict the conserved B-cell epitopes of AIV-H7 HA using a bioinformatics approach, including the three most effective epitope prediction softwares available online: Artificial Neural Network based B-cell Epitope Prediction (ABCpred), B-cell Epitope Prediction (BepiPred) and Linear B-cell Epitope Prediction (LBtope)...
October 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27647752/resistance-to-citrus-canker-induced-by-a-variant-of-xanthomonas-citri-ssp-citri-is-associated-with-a-hypersensitive-cell-death-response-involving-autophagy-associated-vacuolar-processes
#13
Roxana A Roeschlin, María A Favaro, María A Chiesa, Sergio Alemano, Adrián A Vojnov, Atilio P Castagnaro, María P Filippone, Frederick G Gmitter, José Gadea, María R Marano
Xanthomonas citri ssp. citri (X. citri) is the causal agent of Asiatic citrus canker, a disease that seriously affects most commercially important Citrus species worldwide. We have identified previously a natural variant, X. citri A(T) , that triggers a host-specific defence response in Citrus limon. However, the mechanisms involved in this canker disease resistance are unknown. In this work, the defence response induced by X. citri A(T) was assessed by transcriptomic, physiological and ultrastructural analyses, and the effects on bacterial biofilm formation were monitored in parallel...
September 20, 2016: Molecular Plant Pathology
https://www.readbyqxmd.com/read/27618936/asiatic-acid-influences-parasitaemia-reduction-and-ameliorates-malaria-anaemia-in-p-berghei-infected-sprague-dawley-male-rats
#14
G A Mavondo, B N Mkhwananzi, M V Mabandla, C T Musabayane
BACKGROUND: Current malaria treatment is either "anti-parasitic", "anti-infectivity" or both without addressing the pathophysiological derangement (anti-disease aspect) associated with the disease. Asiatic acid is a natural phytochemical with oxidant, antioxidant and anti-inflammatory properties whose effect on malarial and accompanying pathophysiology are yet to be investigated. Asiatic acid influence in P. berghei-infected Sprague Dawley rats on %parasitaemia and malarial anaemia were investigated...
September 13, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27605220/protective-effects-of-asiatic-acid-against-spinal-cord-injury-induced-acute-lung-injury-in-rats
#15
Wu Jiang, Maoqiang Li, Fan He, Wangxiang Yao, Zhenyu Bian, Xuepeng Wang, Liulong Zhu
The biological effects of asiatic acid (AA) on spinal cord injury (SCI)-induced acute lung injury (ALI) have not been investigated. We aimed to investigate the therapeutic efficacy and molecular mechanisms of AA on SCI-induced ALI. One-hundred and fifty Sprague-Dawley rats were randomly assigned to five groups: sham, SCI, SCI + dexamethasone (Dex, 2 mg/kg), SCI + AA (30 mg/kg), and SCI + AA (75 mg/kg). The influences of AA on histologic changes, pulmonary edema, neutrophil infiltration and activation, proinflammatory cytokine production, oxidative stress, and Nrf2 and NLRP3 inflammasome protein expression were estimated...
December 2016: Inflammation
https://www.readbyqxmd.com/read/27593768/effect-of-asiatic-acid-on-the-treatment-of-spinal-cord-injury-an-experimental-study-in-rats
#16
Oktay Gurcan, Ahmet Gurhan Gurcay, Atilla Kazanci, Salim Senturk, Ebru Bodur, Ebru Umay Karaca, Omer Faruk Turkoglu, Murat Bavbek
AIM: Spinal cord injury (SCI) is a devastating condition of the central nervous system. Today any therapeutic agent has not been proved to heal this complex condition yet. Asiatic acid (AA), which has been used in the far Eastern countries as an anti-inflammatory agent, antioxidant and wound healing therapeutic for years. We investigated efficiency of AA administration just after spinal cord injury in rats. MATERIAL AND METHODS: Adult male Sprague-Dawley rats ( n =32) were drafted in to Four experimental groups (Laminectomy, Laminectomy+ Trauma, Vehicle, AA) ramdomly...
October 2, 2015: Turkish Neurosurgery
https://www.readbyqxmd.com/read/27494684/asiatic-acid-inhibits-pulmonary-inflammation-induced-by-cigarette-smoke
#17
Jae-Won Lee, Hyun Ah Park, Ok-Kyoung Kwon, Yin-Gi Jang, Ju Yeong Kim, Bo Kyung Choi, Hee Jae Lee, Sangwoo Lee, Jin-Hyub Paik, Sei-Ryang Oh, Kyung-Seop Ahn, Hyun-Jun Lee
Asiatic acid (AA) is one of the major components of Titrated extract of Centella asiatica (TECA), which has been reported to possess antioxidant and anti-inflammatory activities. The purpose of this study was to investigate the protective effect of AA on pulmonary inflammation induced by cigarette smoke (CS). AA significantly attenuated the infiltration of inflammatory cells in bronchoalveolar lavage fluid (BALF) of CS exposure mice. AA also decreased ROS production and NE activity, and inhibited the release of proinflammatory cytokines in BALF...
October 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27486096/accelerated-stability-studies-on-dried-extracts-of-centella-asiatica-through-chemical-hplc-hptlc-and-biological-activity-analyses
#18
Ishtdeep Kaur, Nancy Suthar, Jasmeen Kaur, Yogita Bansal, Gulshan Bansal
Regulatory guidelines recommend systematic stability studies on a herbal product to establish its shelf life. In the present study, commercial extracts (Types I and II) and freshly prepared extract (Type III) of Centella asiatica were subjected to accelerated stability testing for 6 months. Control and stability samples were evaluated for organoleptics, pH, moisture, total phenolic content (TPC), asiatic acid, kaempherol, and high-performance thin layer chromatography fingerprints, and for antioxidant and acetylcholinesterase inhibitory activities...
October 2016: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/27446228/identification-of-centella-asiatica-s-effective-ingredients-for-inducing-the-neuronal-differentiation
#19
Hui Jiang, Guoshuai Zheng, Junwei Lv, Heyu Chen, Jinjin Lin, Yiyang Li, Guorong Fan, Xianting Ding
Centella asiatica, commonly known as Gotu kola, has been widely used as a traditional herb for decades. Yet, the study on which compounds or compound combinations actually lead to its brain benefits remains scarce. To study the neuroprotection effects of Centella asiatica, neuronal differentiation of PC12 cells was applied. In our pilot study, we isolated 45 Centella asiatica fractions and tested their abilities for inducing neuronal differentiation on PC12 cells. The most effective fraction showed robust induction in neurite outgrowth and neurofilament expression...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27416552/selective-killing-of-cancer-cells-with-triterpenoic-acid-amides-the-substantial-role-of-an-aromatic-moiety-alignment
#20
Sven Sommerwerk, Lucie Heller, Julia Kuhfs, René Csuk
2,3-Di-O-acetyl-triterpenoic acid derived amides possessing a (2β, 3β) configuration in ring A and two acetyl groups were previously shown to possess high cytotoxicity for human tumor cell lines but to exhibit low cytotoxicity for non-malignant mouse fibroblasts. In this study, augustic acid (1) and 2-epi-corosolic acid (2) were chosen as starting points for the synthesis of analogs. While augustic acid derived 3-quinolinyl amide 9 gave low EC50 values in SRB assays but was cytotoxic for all lines, the isomeric 4-isoquinolinyl amide 21 was very cytotoxic for the tumor cell lines but significantly less cytotoxic for the mouse fibroblasts NIH 3T3...
October 21, 2016: European Journal of Medicinal Chemistry
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