Antiproliferative potential of solidagenone isolated of Solidago chilensis

ABSTRACT Plants are considered among the main sources of biologically active chemicals. The species Solidago chilensis Meyen, Asteraceae, is native to the southern parts of South America, where the aerial parts of the plant are commonly used for the treatment of inflammatory conditions. However, the effects of S. chilensis on human cancer cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of the hydroalcoholic and dichloromethane extracts of S. chilensis, as well as their chemical constituents quercitrin and solidagenone against the five human tumor cell lines in vitro. The dichloromethane extract showed a promisor antiproliferative effects in vitro, especially against glioma cell line. Besides, the hydroalcoholic extract and quercitrin were inactive. The diterpene solidagenone showed highly potent antiproliferative effects against breast (MCF-7), kidney (786-0), and prostate cancer (PC-3) cells (total growth inhibition: TGI < 6.25 µg/ml). Solidagenone meets the theoretical physico-chemical criteria for bioavailability of drugs, according to the "Rule of Five" and, by theorical studies, the observed biological effects were probably related to the interaction of the molecule with nuclear receptors and as an enzymatic inhibitor. This study contributes to chemical study and to the identification of antiproliferative molecules in S. chilensis.

Effects of hydroalcoholic extract of Celtis iguanaea on markers of cardiovascular diseases and glucose metabolism in cholesterol-fed rats

ABSTRACT Celtis iguanaea (Jacq.) Sarg., Cannabaceae, is popularly used in the treatment of diabetes mellitus. However, chemical and pharmacological investigations are lacking. In this study, we investigated the effects of the hydroalcoholic extract from C. iguanaea on markers of cardiovascular diseases and the glucose metabolism in cholesterol-fed rats. Therefore, hypercholesterolemic rats (1% cholesterol) were orally treated with C. iguanaea extract (C-150, CI-300, or CI-600 mg/kg) or simvastatin (4 mg/kg) (n = 6) once a day (30 days) with a hypercholesterolemic diet. A control group (C) was given saline. C. iguanaea extract showed significant decreases in serum levels of total cholesterol, LDL-cholesterol, HMG-CoA-reductase, interleukin-1 and 6, TNF-α and IFN-γ when compared to group C (p < 0.001). Hypoglycemic effects were observed along with a decrease of the activity of sucrase (CI-600), maltase (CI-150, CI-300), and an increase in muscle glycogen levels (CI-300). Antioxidant effects were observed in plasma by the decrease of TBARS and increase of nonprotein thiols levels (CI-600). The histopathological analysis showed a significant decrease in the liver fat area for C. iguanaea extract compared to group C (p < 0.001). Our results suggest that the biological effects of C. iguanaea extract could be related to the flavonoids that possibly exert antioxidant, enzymatic inhibitory, and insulin-mimetic effects.

Antiproliferative effects of pinostrobin and 5,6-dehydrokavain isolated from leaves of Alpinia zerumbet

Abstract Natural products are a major source of drugs for the treatment of cancer. The species Alpinia zerumbet (Pers.) B.L. Burtt & R.M. Sm, Zingiberaceae, is widely distributed in Brazil where it is known as "colônia". The leaves are commonly used in the treatment of hypertension and dyspepsia, however, the effects of A. zerumbet extracts and isolated substances on human cancer cells remain to be elucidated. This study was designed to identify the chemical constituents of hydroalcoholic and dichloromethane extracts from A. zerumbet leaves and to investigate their in vitro antiproliferative activity. The isolated phytochemicals included kaempferol, dihydro-5,6-dehydrokavain, 5,6-dehydrokavain, and pinostrobin. The hydroalcoholic extract inhibited cellular proliferation only at high concentrations, while the dichloromethane extract showed a moderate antiproliferative effect against leukemia and lung tumor cell lines. 5,6-Dehydrokavain showed potent cytostatic activity against glioblastoma cells and a moderate effect on all other tumor cell lines. Pinostrobin showed potent activity against leukemia and breast tumor cell lines and moderate cytostatic effect against ovarian cell. Furthermore, this is the first report on the isolation of kaempferol and pinostrobin from A. zerumbet leaves. Moreover, the purification process described in this study was effective. These results suggest that A. zerumbet leaves are a promising source of anticancer compounds.

Hypolipidemic and antiatherogenic effects of Cynara scolymus in cholesterol-fed rats

ABSTRACT Cynara scolymus L., Asteraceae, are traditionally used to treat dyspepsia. This study evaluated the hypolipidemic and antiatherogenic effects of an aqueous extract prepared from the leaves of C. scolymus in rat's model. Hypercholesterolemic rats (1% cholesterol and 0.5% cholic acid for 15 days) were treated (0.5 ml/200 g) with extract of C. scolymus (150, 300, or 600 mg/kg p.o.; n = 6) or simvastatin (4 mg/kg p.o.; n = 6) once per day for 30 days along with hypercaloric diet. A control group (C) was given water (0.5 ml/200 g; n = 6). A high-cholesterol diet was maintained throughout the treatment period. Rats treated with extract of C. scolymus (150, 300, or 600 mg/kg) and simvastatin showed significant decreases in serum levels of total cholesterol (−46.9%, −51.9%, −44%, and −41.9%, respectively) and low-density lipoprotein-cholesterol (LDL-C; −52.1%, −54.8%, −51.9%, and −46.7%, respectively), compared with group C (p < 0.005). Biochemical analyses revealed significant decrease in the concentration of IL-1, IL-6, TNF-α, IFN-γ, C-reactive protein, oxidized-LDL, and antioxidized-LDL in rats treated with extract of C. scolymus (150, 300, or 600 mg/kg). There were no differences in serum ALT enzyme activity between the groups. Our results suggest that hypolipidemic and antiatherogenic effects could be related with the presence of polar substances present in aqueous extract of C. scolymus.

Hypoglycemic and hypolipidemic effects of Solidago chilensis in rats

AbstractSolidago chilensis Meyen, Asteraceae, is traditionally used to treat inflammation. However, phytochemical and pharmacology investigations are lacking. This study evaluated the hypoglycemic and hypolipidemic effects of hydroalcoholic extract from S. chilensis aerial parts in rats. In oral glucose tolerance tests the rats received saline (0.5 ml/100 g) in control group (C), hydroalcoholic extract (125, 250 or 500 mg/kg p.o.; n = 6) or glibenclamide (10 mg/kg p.o.; n = 6). After 30 min, glucose (4 g/kg) was administered. Rats treated with hydroalcoholic extract 500 demonstrated decreased glucose levels at 180 min (-22.1%), when compared with group C, similar to glibenclamide. Moreover, treatment with hydroalcoholic extract 500 significantly increased the glycogen content in the liver and soleus muscle, and hydroalcoholic extract 250 specifically inhibited the enzyme maltase when compared with group C. Furthermore, all hyperglycemic rats treated with hydroalcoholic extract (125, 250 and 500) exhibited an accentuated decrease in total cholesterol levels (-36.8%, -36.7% and -41.3%, respectively). Our results suggest that hypoglycemic and hypolipidemic effects of hydroalcoholic extract could be associated with increased production and release of insulin as well as with insulinotropic and antioxidant effects.

Controle farmacognóstico das raízes de Heteropteris aphrodisiaca O. Mach. (Malpighiaceae) / Pharmacognostic analysis of the roots of Heteropteris aphrodisiaca O. Mach. (Malpighiaceae)

As raízes de Heteropteris aphrodisiaca, denominadas de " nó-de-cachorro" , pela semelhança morfológica com o pênis canino, são usadas popularmente com ação afrodisíaca, estimulante e no tratamento de disenterias, tendo este estudo o objetivo de caracterizá-las morfoanatômica e fisico-quimicamente. Para as análises foram elaboradas lâminas histológicas e analisados extratos aquosos, hidro-etanólicos e cetônicos obtidos a partir de amostras coletadas no estado do Mato Grosso, nas diferentes estações do ano. Tais raízes são tuberosas, cilíndricas e recobertas por súber estriado de coloração marrom-escura. O córtex, composto por tecido parenquimático, não apresenta elementos esclerificados, mas mostra-se com abundância de drusas e cristais prismáticos de oxalato de cálcio, bem como de idioblastos contendo polifenóis. No xilema secundário são abundantes as fibras gelatinosas, típicas de raízes de espécies do cerrado brasileiro. As análises físico-químicas revelaram maiores perdas por dessecação nas amostras coletadas no verão e na primavera. A água foi considerada o melhor líquido extrator, o teor de cinzas totais das amostras variou de 3,4 por cento no verão a 5,3 por cento no outono, enquanto que os teores de polifenóis totais foram maiores na primavera (10,2 por cento) que nas demais estações, sugere-se esta estação como a mais apropriada para a coleta da droga vegetal. Análises cromatográficas em camada delgada e líquida de alta eficiência foram realizadas empregando-se marcadores flavonoídicos neoastilbina, astilbina e isoastilbina, com valores de Rf de 0,60, 0,68 e 0,74, e tempos de retenção de: 16,44, 16,91 e 18,08 min, respectivamente.

The roots of Heteropteris aphrodisiaca, called " nó-de-cachorro" (dog-knot) for their morphological similarity to the canine penis, are used in popular medicine as an aphrodisiac or stimulant, and to treat dysentery. The objective of the present study was to characterize these roots morphoanatomically and physico-chemically. For the analyses, histological slides were prepared, and aqueous, hydro-ethanol, and ketone extracts were analyzed, from root samples collected in the state of Mato Grosso, in different seasons of the year. The roots are tuberous, cylindrical, and covered with a striated suber. The cortex, composed of parenchymatous tissue, has no sclerified elements, but shows abundant druses and prismatic crystals of calcium oxalate, as well as idioblasts containing polyphenols. In the secondary xylem, gelatinous fibers are abundant, typical for the roots of species of the Brazilian cerrado (savanna). The physical and chemical analyses revealed greater losses through desiccation in the samples collected in spring and summer. Water was the best extraction liquid. Total ash content of the samples ranged from 3.4 percent in summer to 5.3 percent in autumn. Total phenol content was higher in spring (10.2 percent), suggesting this season as the most appropriate to harvest the plant drug. Chromatographic analyses through TLC and HPLC were employed using the flavonoids neoastilbin, astilbin, and isoastilbin as markers. The Rf values were 0.60, 0.68 and 0.74, and the retention time were 16.44, 16.91 and 18.08 min, respectively.