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The native Chilean shrubs Buddleja globosa (Matico) and Ribes magellanicum (Zarzaparrilla) are used widely at a rural level, due to their medicinal properties. Nevertheless, little is known about their secondary metabolites and cytotoxic effect. The aim of this study was to evaluate the content of different compounds like catechin, epicatechin, p-coumaric acid and the antioxidant capacity by ABTS, ORAC, FRAP and DPPH methods. In addition, the cytotoxic activity of both extracts was evaluated against Chinese hamster ovary (CHO-K1) cell lines by MTT and neutral red assays. The results suggest that the most abundant constituent in Budleja globosa and Ribes magellanicum were catechin (682.43 mg/100 g DW) and epicatechin (3362.08 mg/100 g DW) respectively; while the ORAC methodology showed an elevated antioxidant activity for Matico (134147.31 μmol Trolox Eq/100 g DW). On the other hand, both extracts at the assayed concentrations affect the membrane stability and cellular metabolic capacity of the CHO-K1 cell lines. These finding provide a direction for further researches, and suggest the Matico and Zarzaparrilla flower extracts as promising sources of antioxidants, and as research objects through the analyze of their metabolic behavior and antitumoral potential.

Buddleja globosa Hope (Buddlejaceae) is a native species cultivated in Chile, Peru and Argentina. In folk medicine, this plant is frequently used for the treatment of different wounds (internal and external), as well as intestinal and liver diseases. There is growing scientific evidence on the growing conditions for Buddleja globosa and how its cultivation could be optimized. Methods for its vegetative propagation have also been successfully elaborated. The leaves contain phenylpropanoids, iridoids, terpenes and flavonoids. Ethnopharmacological validation studies suggest that phenylpropanoids and flavonoids are the main and most important compounds in defining the therapeutic activity of Buddleja globosa. This chemical composition explains its pharmacological activity as antioxidant, anti-inflammatory, antimicrobial and, in particular, its wound healing effects. Due to its undeniable potential as a domesticated, cultivated medicinal plant and its remarkable chemical composition, it is still necessary to develop its properly standardized, clinically validated phytopharmaceutical products.

The antioxidant and antihemolytic properties contained in the leaves of Buddleja globosa (B. globosa), also known as "Matico," were determined. Aqueous extracts of leaves were assayed in human erythrocytes and molecular models of its membrane. The latter were bilayers built-up of lipids located in the outer and inner leaflets of the erythrocyte membrane. Observations by scanning electron microscopy showed that the extract altered the morphology of erythrocytes inducing the formation of crenated echinocytes. This result implied that the extract components were inserted into the outer leaflet of the cell membrane. This conclusion was confirmed by experiments carried out by fluorescence spectroscopy of red cell membranes and vesicles (LUV) of dimyristoylphosphatidylcholine (DMPC) and by X-ray diffraction of DMPC and dimyristoylphosphatidylethanolamine bilayers. Human erythrocytes were in vitro exposed to HClO, which is a natural powerful oxidant. Results demonstrated that low concentrations of B. globosa aqueous extract neutralized the harmful capacity of HClO. Hemolysis experiments also showed that the extract in very low concentrations reduced hemolysis induced by HClO.

Buddleja globosa is a medicinal shrub native to Chile. Its leaves have been traditionally used for wound and ulcer healing. Different medicinal properties, such as outstanding antioxidant, anti-inflammatory, wound healing and analgesic activities have been shown. Today, all raw materials for pharmaceutical process are coming from wild collection or recently established crops but not from selected plants. Studies of the genetic or environmental variability of the species would permit the optimization of yield and quality factors through the selection of genetic material or suitable production sites and management techniques. To assess which traits are determined genetically some yield related plant and leaf characteristics were studied in three wild populations and the cultivated accessions from the same provenances. The cultivated accessions also included three clones coming from individuals found in rural home gardens. For the cultivation studies individuals were arranged in a randomised block design, and those for the irrigation studies in split plots watered at 20% and 65% field capacity. Plant characteristics such as height and width of the plant, the ratio of both, stem diameter and leaf density differed significantly among natural populations. In leaf characteristics only the presence of stipules showed significant differences. The cultivated progenies or clones may give an idea if these differences among populations are due to environmental or to genetic effects. Compared with other provenances, plants from the coastal provenance Los Ruiles are tallest in both natural populations and cultivated clones and also showed superior leaf yields in spite of their lower leaf density. The hairy leaves may cause allergic reactions at the moment of harvest. This characteristic is not influenced by different irrigation treatments and shows no significant differences between cultivated and wild plants. Because of the significant higher leaf yields per plant in home garden clones we assume that formerly individuals with a higher leaf production were selected for cultivation.

The increase of land use for crop cultivation and forest in South Central Chile, and the increasing wildcrafting of medicinal plants has resulted in a significant reduction of the plant population density of many native and endemic medicinal plants. Their cultivation and domestication is very limited, and there are no regulations or legislation for wildcrafting in Chile. The objectives of this study were to collect genetic material from five native medicinal plants (Adesmia emarginata, Buddleja globosa, Fabiana imbricata, Linum chamissonis, and Sophora macrocarpa), characterize the environmental conditions in which these grow in the Bio-Bio Region, Chile, and to determine the content of specific bioactive molecules. A maximum of 10 accessions of each species were collected in 2003, 2004, and 2005 in a longitudinal and transversal transect of the Bio-Bio Region (36°00′–38°30′S; 71°W). Data of altitude, light conditions, soil chemical and physical characteristics and associated flora of the site collection were recorded. Seed germination requirements and the content of specific bioactive molecules (flavonoids or rutin) were also determined. In general, all these species are adapted to grow in poor soils with different pH values, P and K levels, low organic matter and N content. Flavonoids were determined in both A. emarginata (0.6–1%) and B. globosa (9.7–13.9%) leaves, while rutin concentration was determined in F. imbricata leaves and stems (1.3–5.3%). Results showed great variations for the content of active principles with medicinal activity, which indicates a corresponding variation in the quality of raw materials for the pharmaceutical industry. Due to the fact that information on the domestication, propagation, cultivation and agronomic practices can ensure good pharmaceutical quality, this study provides a basis for further research on Chilean medicinal plants.

Ethnopharmacological relevance Leaf extracts of Buddleja globosa (Buddlejaceae) are used in Chilean folk medicine for wound healing. The anti-inflammatory (topic and per os), analgesic (per os) effects and the antioxidant activity of Buddleja globosa were for the first time reported by us. Aim of the study Assess the antinociceptive activity of the methanol sequential and global extracts using complementary chemical and thermal models of pain, characterize pharmacologically the antinociception induced, evaluate seasonal influence to support Buddleja globosa medicinal use. Materials and methods Global methanol, sequential methanol and ethanol (leaves collected in autumn and summer) extracts were evaluated for oral and topic analgesia in tail flick, formalin and writhing models, verbascoside and 7-O-luteolin glucoside were assayed in tail flick and writhing. Ibuprofen was used as reference. For characterization of induced antinociception, naltrexone, naltrindole, tropisetron, nor-binaltorphimine, prazosin, yohimbine, atropine, and N-nitro- l -arginine methyl ester were used as antagonists and inhibitors drugs. Results Seasonal influence was observed since autumn extract resulted less active. Extracts showed a dose-dependent antinociceptive activity in all assays, the highest effects were obtained for the formalin and writhing test. Verbascoside was more active than ibuprofen in the writhing test (67.6% and 50.0% at equimolar doses) and showed similar effects in the tail flick (topic and oral) near 25% at equivalent doses – ED25 or EC25 – to ibuprofen. Luteolin 7-O-glucoside was slightly more active in the tail flick test and nearly half active than verbascoside in the writhing assay. Effectiveness was higher for the sequential than for global alcoholic extracts, and can be increased by selective blocking of opioid receptors. Global methanol extract seems modulated only by naltrexone. Conclusions Analgesic effect of Buddleja globosa is here demonstrated validating its use in traditional medicine. Season influence is important to be considered.

In vitro tests are now widely employed in ethnopharmacological research because of ethical reasons and their usefulness in bioactive-guided fractionation and determination of active compounds. For many disease conditions, a variety of in vitro tests can now be employed as the biochemical mechanisms underlying disease and healing processes are understood. Approaches to the in vitro investigations of wound healing processes are exemplified by studies on extracts of Buddleja species and three Ghanaian species Spathodea campanulata, Commelina diffusa and Secamone afzelii. Most studies have been carried out on Buddleja officinalis or Buddleja globosa. The extracts have been shown to have anti-inflammatory and antioxidant properties due to flavonoids, triterpenoids, diterpenoids and caffeic acid derivatives. There appears to a slight effect on proliferation of fibroblasts at lower concentrations, but this was not significant, and higher concentrations appeared to be cytotoxic. Novel findings are the ability of Buddleja globosa leaf extracts to induce differentiation in keratinocytes and to alter the profile of proteins produced by cultured fibroblasts. Extracts also had some effect on lattice contraction. The three Ghanaian species examined show a mixture of antimicrobial and antioxidant activities. The evolution over recent years of tests for wound healing, from in vivo tests to cell-based systems and chemical reactions and on to investigations into effects on secondary messengers and protein expression, is described.

Matico (Buddleja globosa Hope) is a native shrub of Chile, whose leaves are widely used in popular medicine due to its excellent wound- and gastric ulcer healing effects. At present it is collected from the wild, resulting in an over-explotation of the natural habitat and great heterogenity of the collected material. The present investigation tried to define the most efficient big scale vegetative propagation methodology. Matico proved to be an easy-rooting species, reaching rooting percents of about 80%. Hormonal treatments with 1000 to 2000 ppm IBA (indole butyric acid) applied at the base of the cuttings promotes and accelerates the rooting process. Time of rooting does not influence the final number of rooted cuttings, although an acceleration of the rooting process and an decrease of the survival in springtime was observed. Studying different types of cuttings, best rooting results were obtained with cuttings from the apical portion of the mother-branch. A mixture of perlite and vermiculite resulted to be the most favorable rooting media. El matico (Buddleja globosa Lam.) es un arbusto nativo de Chile cuyas hojas son muy usadas en medicina popular debido a su gran poder cicatrizante. Actualmente es cosechado de plantas silvestres para su comercializacion, conllevando a una sobrexplotacion del habitat natural y gran heterogeneidad del material. En el presente estudio se busco acotar los metodos mas apropiados para su propagacion vegetativa a gran escala. Resulto ser una especie de facil arraigamiento, lograndose porcentajes de enraizamiento superiores al 80%. La aplicacion de 1000 a 2000 ppm de acido indolbutirico en la base de la estaca favorecio y acelero el enraizamiento. La epoca de enraizamiento no influyo en el numero final de estacas enraizadas. Sin embargo, hubo un aceleramiento del proceso en primavera junto a una disminucion del porcentaje de sobrevivencia. Respecto del tipo de estaca se obtuvieron los mejores resultados con estacas provenientes del apice de las ramas madres y una mezcla de perlita con vermiculita (1:1) resulto ser el sustrato mas favorable para el enraizamiento.

An aqueous extract of Buddleja globosa leaves, used traditionally in Chile for wound healing, was tested for the ability to stimulate growth of fibroblasts in vitro and for antioxidant activity in the same fibroblast cell system challenged with hydrogen peroxide. Low concentrations of the extract gave an increase in fibroblast growth which was not statistically significant but cytotoxicity was observed at concentrations greater than 50 microg/ml. The extract showed strong antioxidant effect and fractionation led to the isolation of three flavonoids and two caffeic acid derivatives, each of which was shown to contribute to the antioxidant effect at concentrations below 10 microg/ml. These activities would accelerate the healing of wounds.

The aim was to produce a tetraploid form of Buddleia globosa to facilitate introgression of yellow flower colour into B. davidii, which is naturally tetraploid. Protocols were established for the micropropagation of B. globosa and tetraploid plants were obtained by application in vitro of colchicine to pre-cultured excised nodal sections. Three concentrations of colchicine were applied (0.01%, 0.05% and 0.1% w/v) for 1, 2 or 3 days. At 0.01% tetraploids were produced only after 2 days of application. All other treatments produced at least one tetraploid. The colchicine technique was extremely effective: of 29 lines tested, 19 were tetraploid and 5 were mixoploid. The vegetative characteristics of these tetraploids are described and the flowering characteristics of the three that flowered.

Ethnopharmacological relevance Buddleja globosa , known as “matico”, is employed in Chile for wound healing. Aim of the study To validate the traditional use of the crude drug through in vivo and in vitro evaluation of the anti-inflammatory, analgesic and antioxidant properties of its extracts. Materials and methods Sequential hexane, dichloromethane, methanol and total methanol extracts were studied using bioguided fractionation. The following activities were investigated: analgesic (writhing test), oral and topic anti-inflammatory (paw- and ear-induced edema), free radical scavenging and antioxidant activities (1,1-diphenyl-2-picrylhydrazyl, DPPH, superoxide anion, lipid peroxidation and xanthine oxidase inhibition). Sodium naproxen, nimesulide, indomethacin were used as reference drugs for in vivo , quercetin and allopurinol for in vitro assays. Results A mixture of α- and β-amyrins was isolated from the hexane extract that showed 41.2% of analgesic effect at 600 mg/kg, inhibited by 47.7 and 79.0% the arachidonic acid (AA) and 12-deoxyphorbol-13-decanoate (TPA)-induced inflammation at 3 mg/20 μL/ear, respectively. A mixture of β-sitosterol, stigmasterol, stigmastenol, stigmastanol and campesterol was isolated from the fraction CD4-N and β-sitosterol-glycoside from the fraction CD5-N, reducing TPA-induced inflammation by 78.2 and 83.7% at 1 mg/20 μL/ear, respectively. The fraction CD4-N at 300 mg/kg also showed analgesic activity (38.7%). The methanol extract at 600 mg/kg per os showed anti-inflammatory effect (61.4%), topic anti-inflammatory (56.7% on TPA) and analgesic activity (38.5%). Verbascoside and luteolin-7- O -glucoside were the major components of the methanol extract; apigenin 7- O -glucoside was also detected. Inhibition of superoxide anion, lipoperoxidation, and DPPH bleaching effect was found in the methanol serial and global extracts. Conclusions The present report demonstrate the analgesic and anti-inflammatory properties of Buddleja globosa and validate its use in Chilean traditional medicine.

Numerous investigations exist about the alterations that oxygen free radicals can provoke on biomolecules; these modifications can be prevented and/or reversed by different antioxidants agents. On the other hand, 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), a stable nitrogen synthetic radical, is used to evaluate the antioxidant capacity of medicinal herbal products; however, the structural changes that this radical provoke on the herbal active principles are not clear yet. In this work, we compared the redox reactivity of oxygen free radicals and DPPH radical on phospholipids and protein thiol groups present in rat liver microsomes. Cu2+/ascorbate was used as generator system of oxygen free radical and as antioxidant, an extract of Buddleja globosa's leaves. Cu2+/ascorbate provoked microsomal lipid peroxidation, microsomal thiols oxidation and oxygen consumption; all of these phenomena were inhibited by B. globosa extract. On the other hand, DPPH was bleached in different extension by the herbal extract and phosphatidyl choline; beside, DPPH decreased microsomal thiols content, but this phenomenon were not prevented by the herbal extract. Furthermore, DPPH did not induce oxygen consumption and neither modified the oxygen consumption induced by Cu2+/ascorbate. Distinct redox mechanisms may explain the differences between the reactivity of DPPH and oxygen free radicals on biomolecules, which is discussed.

Fifteen extracts from nine selected Argentine medicinal plants were tested for their antiplasmodial activity in vitro by assessing their ability to inhibit the uptake of [3H]-hypoxanthine into the Plasmodium falciparum K1 pyrimethamine/chloroquine resistant strain. The methanol extract of Satureja parvifolia showed good antiplasmodial activity (IC(50) 3 microg/ml). Inhibition of the growth of P. falciparum was also observed with aqueous extracts of Buddleja globosa and S. parvifolia.

The aqueous extracts of three species of Buddleja which are used in traditional medicine for the treatment of liver ailments have shown an inhibitory effect against induced cytotoxicity of cultured hepatocytes. Fractionation of one of these extracts, from B. globosa leaves, resulted in the isolation of five iridoids, two phenylpropide glycosides, and a flavonoid glycoside. Two of the iridoids were found to be novel compounds, 7-p-methoxycinnamoylaucubin (1) and 7-p-methoxycinnamoylcatalposide (2). One of the phenylpropides, echinacoside, has not previously been reported from Buddleja. Testing of the isolated compounds in the cultured hepatocyte system indicated that the activity is most likely due to the flavonoid and phenylpropide constituents. Phenylpropide glycosides have not previously been shown to have a liver-protectant effect.

A chloroform extract of the stem bark of Buddleja globosa yielded a mixture of crystalline compounds which were found to be esters of long chain fatty acids and 4-hydroxycinnamyl alcohol or 2-(4-hydroxyphenyl ethanol. This type of ester has been proposed as forming the units of the complex polymer suberin but no individual monomers have been reported until now.

Buddleja species play a minor role in the ethnopharmacology of several areas of the world where they are indigenous. Phytochemical investigation of the genus has been somewhat neglected but a picture is emerging of the type of constituents which are present in reasonable quantities, namely iridoid and flavonoid glycosides. Many of the uses of Buddleja in folk medicine such as a topical antiseptic and a diuretic can be partially explained at least by the known biological activity of compounds identical or similar to those found in the genus. Other reputed uses are, as yet, without explantation due to the incomplete state of knowledge of the chemistry and, to an even greater extent, the pharmacology of Buddleja.