In vivo antitumoural activity and composition of an oil extract of Brazilian propolis

The present study aimed to evaluate in vivo and in vitro the antitumoural activity of a propolis extract obtained with edible vegetable oil and its fractions and also to investigate its chemical composition by LC–MS and LC–MS/MS. To evaluate the toxicological aspects related to the propolis extract treatment, hematological, biochemical, histopathological and morphological analyses of treated animals were performed. All propolis extracts showed an in vivo antitumour activity in the experimental model with a moderate toxicity effect at experimental exposure levels. The oil extract was as effective as the ethanolic extract at inhibiting tumour growth. In vitro assays showed that the whole oil extract produced better inhibition of tumour cells than its fractions. LC–MS and LC–MS/MS identified four phenolic acids and three flavonoids. The anticancer potential of the oil extract of propolis has been demonstrated and the edible vegetable oil was shown as an attractive alternative solvent to extract bioactive natural propolis components.     

Enhancement of the Antitumour Activity for the Synthesised Dodecylcysteine Surfactant using Gold Nanoparticles

In this paper, the surfactant dodecylcysteine hydrochloride was synthesised. The surface parameters of the synthesised surfactant were studied using a surface tension technique. The surface parameters show a good surface activity of the prepared surfactant in aqueous solution. The self-assembling behaviour of the synthesised surfactant comparing with that of cysteine compound on the prepared gold nanoparticles was confirmed using transmission electron microscope (TEM) measurements. The effect of self-assembling of this surfactant on the size of gold nanoparticles was studied using TEM images. The antitumour activity of the prepared surfactant without and with the gold nanoparticles was investigated. The results show that the antitumour activity of the prepared surfactant was enhanced with the presences of the gold nanoparticles.

Three sulphated polysaccharides isolated from the mucilage of mud snail, Bullacta exarata philippi: Characterization and antitumour activity

Three sulphated polysaccharides, coded as BEMPA, BEMPB₁, BEMPB₂, were extracted from the mucilage of mud snail of Bullacta exarata and purified by DEAE-cellulose ion-exchange and size-exclusion chromatography. Structural analysis of purified polysaccharides by chemical and biochemical methods revealed BEMPA was a high (1→3,4)-linked mannose-containing polysaccharide with molecular weight of 22,977 Da. BEMPB₁, with molecular weight of 64,117 Da, was a high (1→3)-linked arabinose-containing polysaccharide. BEMPB₂ was mainly composed of (1→3,4)-linked mannose with molecular weight of 47,507 Da. The comparison between sulphated polysaccharides and their desulphated products showed that sulphate substitutions of BEMPB₁ were deduced to be at the C-3 of (1→4)-linked mannose, while sulphate substitutions of BEMPA and BEMPB₂ were at C-4 of (1→3)-linked mannose. Furthermore, BEMPA exhibited highest inhibitory effects on growth of B-16 melanoma cells, and IC₅₀ were 31.1 μg/mL.     

Structural characterisation of polysaccharides from Tricholoma matsutake and their antioxidant and antitumour activities

In this study, polysaccharides from Tricholoma matsutake (TM-P) were purified using a DEAE-Sepharose fast flow column and three polysaccharide fractions (TM-P1, TM-P2 and TM-P3) were obtained. The chemical composition and structural characteristics of TM-P2 were quite different from those of TM-P1 and TM-P3. TM-P2 consisted of glucose, galactose and mannose with a molar ratio of 5.9:1.1:1.0. The glycosidic linkages were mainly composed of 1,6- and 1-linked glucose. Furthermore, TM-P2 showed the strongest in vitro antioxidant and antitumour activities. The oxygen radical absorbance capacity (ORAC) of TM-P2 was 2100.44 μmol Trolox/g. The antiproliferative activities of TM-P2 (4.0 mg/ml) on the growth of HepG2 and A549 cells were 67.98% and 59.04%, respectively.     

Infusion and decoction of wild German chamomile: Bioactivity and characterization of organic acids and phenolic compounds

Natural products represent a rich source of biologically active compounds and are an example of molecular diversity, with recognised potential in drug discovery. Herein, the methanol extract of Matricaria recutita L. (German chamomile) and its decoction and infusion (the most consumed preparations of this herb) were submitted to an analysis of phytochemicals and bioactivity evaluation. The antioxidant activity was determined by free radicals scavenging activity, reducing power and inhibition of lipid peroxidation; the antitumour potential was tested in human tumour cell lines (breast, lung, colon, cervical and hepatocellular carcinomas), and the hepatotoxicity was evaluated using a porcine liver primary cell culture (non-tumour cells). All the samples revealed antioxidant properties. The decoction exhibited no antitumour activity (GI₅₀ > 400 μg/mL) which could indicate that this bioactivity might be related to compounds (including phenolic compounds) that were not extracted or that were affected by the decoction procedure. Both plant methanol extract and infusion showed inhibitory activity to the growth of HCT-15 (GI₅₀ 250.24 and 298.23 μg/mL, respectively) and HeLa (GI₅₀ 259.36 and 277.67 μg/mL, respectively) cell lines, without hepatotoxicity (GI₅₀ > 400 μg/mL). Infusion and decoction gave higher contents of organic acids (24.42 and 23.35 g/100 g dw). Otherwise, the plant methanol extract contained the highest amounts of both phenolic acids (3.99 g/100 g dw) and flavonoids (2.59 g/100 g dw). The major compound found in all the preparations was luteolin O-acylhexoside. Overall, German chamomile contains important phytochemicals with bioactive properties (mainly antitumour potential selective to colon and cervical carcinoma cell lines) to be explored in the pharmaceutical, food and cosmetics industries.     

Purification, antitumour and immunomodulatory activity of water-extractable and alkali-extractable polysaccharides from Solanum nigrum L.

The water-extractable and the alkali-extractable polysaccharides from Solanum nigrum L. (named SNLWP and SNLAP, respectively) and their four polysaccharide sub-fractions (SNLWP-1, SNLWP-2, SNLAP-1 and SNLAP-2), were isolated and purified by ethanol precipitation, dialysis, anion-exchange and gel filtration chromatography. Antitumour and immunomodulatory activity of the polysaccharides was evaluated by determining the survival time, the ascites volume, the weight of immune organ and the level of cytokine (IL-2, IL-10 and IFN-γ) of H₂₂-bearing mice, respectively. The results showed that SNLWP-1, SNLAP-1 and SNLAP-2 had significant antitumour and immunomodulatory activity, whereas SNLWP-2 hardly demonstrated the activity. SNLWP-1 contained galactose and arabinose as main sugar components, and both SNLAP-1 and SNLAP-2 were rich in xylose, galactose and arabinose. SNLWP-2 was rich in glucose. In conclusion, SNLWP-1, SNLAP-1 and SNLAP-2 have potent antitumour activity which may be associated with their potent immunostimulating effect and monosaccharide composition.     

啤酒酵母胞壁多糖抑制肿瘤作用的实验研究

目的:通过动物实验探讨啤酒酵母胞壁多糖对肿瘤的抑制作用。方法:采用现代分离提取技术从啤酒废酵母中分离纯化出酵母胞壁多糖;通过小鼠移植性肿瘤试验探讨酵母胞壁多糖在体内的抑瘤作用,并对其进行半致死量测定。结果:酵母胞壁多糖能显著抑制HCa-F25/A16肝癌和Lewis肺癌的瘤重(在剂量为0～200mg/kg·d范围内抑制率随剂量增加而增加,当剂量超过200mg/kg·d时,抑制率反而下降);该多糖小鼠口服时的半致死量LD_(50)为3077.86(mg/kg)。结论:使用本工艺获得的样品,其酵母胞壁多糖的含量为86.5％;酵母胞壁多糖对Hca-F25/A16肝癌和Lewis肺癌具有显著的抑制作用;急性毒理实验说明酵母胞壁多糖是一种安全低毒、值得开发的保健食品的原料资源。     

~(14)C-标记1,2-双-(3,5-二氧哌嗪基)乙烷[ICRF_(154)]的合成

A.M.Greighton 1969年合成了双酰胺环ICRF_(154),然后改变化学结构合成了ICRF_(159,193)等衍生物。对其抗肿瘤(肉瘤S_(180)),白血病L_(1210),腺癌175,肿瘤walker_(256)进行药物筛选。ICRF_(154)口服对实验肿瘤有效,Dr.Hellmann临床试用发现不活泼。由于它在水和有机溶剂中不溶解,认为体内吸收很差或不吸收。我所将ICRFF_(154)用于临床治疗银宵病疗效显著。~(14)C-标记ICRF_(154)可为进行吸收、分布、排泄研究提供标记化合物。     

Nutrients,phytochemicals and bioactivity of wild Roman chamomile: A comparison between the herb and its preparations

Roman chamomile, Chamaemelum nobile L. (Asteraceae), has been used for medicinal applications, mainly through oral dosage forms (decoctions and infusions). Herein, the nutritional characterisation of C. nobile was performed, and herbal material and its decoction and infusion were submitted to an analysis of phytochemicals and bioactivity evaluation. The antioxidant activity was determined by free radicals scavenging activity, reducing power and inhibition of lipid peroxidation, the antitumour potential was tested in human tumour cell lines (breast, lung, colon, cervical and hepatocellular carcinomas), and the hepatotoxicity was evaluated using a porcine liver primary cell culture. C. nobile proved to be an equilibrated valuable herb rich in carbohydrates and proteins, and poor in fat, providing tocopherols, carotenoids and essential fatty acids (C18:2n6 and C18:3n3). Moreover, the herb and its infusion are a source of phenolic compounds (flavonoids such as flavonols and flavones, phenolic acids and derivatives) and organic acids (oxalic, quinic, malic, citric and fumaric acids) that showed antioxidant and antitumour activities, without hepatotoxicity. The most abundant compounds in the plant extract and infusion were 5-O-caffeoylquinic acid and an apigenin derivative. These, as well as other bioactive compounds, are affected in C. nobile decoction, leading to a lower antioxidant potential and absence of antitumour potential. The plant bioactivity could be explored in the medicine, food, and cosmetic industries.     

Bioactivity and chemical characterization in hydrophilic and lipophilic compounds of Chenopodium ambrosioides L.

The bioactive properties (antioxidant and antitumour activities, and hepatotoxicity) of the infusion and methanolic extracts of Chenopodium ambrosioides L., a plant commonly used in Portuguese folk medicine, were compared. The chemical composition in hydrophilic (sugars, organic acids and phenolic compounds) and lipophilic (fatty acids and tocopherols) fractions were determined. In general, the infusion revealed higher antioxidant activity, while the methanolic extract was the only one showing antitumour effects against colon, cervical and hepatocellular carcinoma cell lines. No toxicity in non-tumour cells was observed either for the infusion or the extract. The studied plant proved to be a good source of natural antioxidants and other bioactive compounds, which may have industrial use. As far as we know, this is the first detailed chemical characterization and bioactivity evaluation of C. ambrosioides methanolic extract and infusion.