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Schizogyne sericea, well-known as 'salado', is a halophytic shrub widespread on coastal rocks of Tenerife (Canary Islands). This plant is used traditionally as analgesic, astringent, anti-inflammatory and vulnerary agent. In the present work, we have analysed the aqueous and ethanolic extracts of S. sericea for the content of phenolic acids by HPLC-DAD. The dynamic solid-liquid Naviglio® extractor was used to extract the flowering aerial parts. Aqueous extracts showed higher levels of phenolics than ethanolic extracts. S. sericea extracts were rich in chlorogenic and isochlorogenic acids. The Naviglio® extracts obtained were assayed for in vitro biological activities, namely antioxidant, antimicrobial and cytotoxicity on tumour cells by DPPH, ABTS, FRAP, agar disc-diffusion and MTT methods, respectively. Results showed that aqueous extracts, being richer in phenolic acids, are endowed with relevant radical scavenging activity (TEAC values in the range 208-960 μmol TE/g) while ethanolic extracts exhibited noteworthy antiproliferative effects on tumour cells.

In the present work we carried out a phytochemical and biological investigation on three Hypericum species, i.e. Hypericum reflexum, Hypericum canariense and Hypericum grandifolium, from the Canary Islands where they are traditionally used as diuretic, wound healing, vermifuge, sedative and antidepressive agents. The polar extracts of the top flowering aerial parts, prepared by Soxhlet apparatus using a methanol-acetone (1:1) extracting mixture, were analyzed by HPLC-DAD and HPLC-MS for the content of eight biomarkers such as hypericin, hyperforin, chlorogenic acid, rutin, hyperoside, isoquercitrin, quercitrin and quercetin, whereas the hydrodistilled essential oils were analyzed by GC-FID and GC-MS. The three Hypericum species had different results in both polar and volatile constituents, H. reflexum being the only one endowed with a small amount of naphtodianthrones (hypericin and pseudohypericin), and containing high levels of chlorogenic acid, rutin and volatile mono- and sesquiterpenes. After chemical characterization, all products were in vitro biologically assayed for antiproliferative activity on human tumor cell lines by MTT assay, for antioxidant potential by DPPH, ABTS and FRAP assays, and for antimicrobial activity by the agar disc diffusion and microdilution methods. Results revealed interesting bioactivities and differences between polar extracts and essential oils, with the former being endowed with significant antioxidant activity and the latter with comparable inhibition effects on the tumor cells (A375, MDA-MB 231 and HCT 116) to that of cisplatin., (Copyright © 2014 Elsevier B.V. All rights reserved.)

The present study investigated the antinociceptive activity of different extracts prepared from the aerial parts of blossom of Hypericum grandifolium Choisy-a species native to the Macaronesian Region-using the acetic acid-induced writhing, formalin and tail flick test in mice. Oral administration of methanol extract (500 and 1,000 mg/kg p.o.), the aqueous, butanol and chloroform fractions (500 mg/kg p.o.) as well as subfractions F2 and F3 (45 mg/kg p.o.) from the chloroform fraction significantly inhibited acetic acid-induced writhing, with values ranging from 28 to 50% of inhibition. The methanol extract (1,000 mg/kg p.o.) and chloroform fraction (500 mg/kg p.o.) significantly reduced both phases of formalin-induced pain (with inhibition values ranging from 18 to 53%), whereas subfraction F2 (45 mg/kg p.o.) significantly inhibited the late phase (30%). In the tail flick assay, only the chloroform fraction (500 mg/kg p.o.) significantly prolonged the tail flick response. Different constituents, such as flavonoids and benzophenone derivatives, could account for the effects observed. Taking together, the results indicate that Hypericum grandifolium Choisy possesses both peripheral and central antinociceptive activities in mice, suggesting an interesting therapeutic potential for this species in pain diseases.

Aim of the Study: Various species of Hypericum genus have been used in the Canary Islands as sedative, diuretic, vermifuge, wound healing, antihysteric and antidepressant agent. Studies have shown that methanol extract of Hypericum grandifolium Choisy is active in tetrabenazine-induced ptosis and forced swimming tests. In the current study, the aqueous, butanol and chloroform fractions obtained from the methanol extract as well as three sub-fractions derived from the chloroform fraction were evaluated for their central nervous effects in mice, particularly their antidepressant activity., Materials and Methods: The central nervous effect of different fractions and sub-fractions of Hypericum grandifolium was evaluated in mice using various behavioural models including locomotor and muscle relaxant activity, forced swimming test, effect on normal body temperature, barbiturate-induced sleep, tetrabenazine-induced syndrome and 5-hydroxytryptohan-induced head twitches and syndrome., Results: We found that the butanol and chloroform fractions and all sub-fractions showed an antidepressant effect in the forced swimming test, the chloroform fraction being the most active. They produced no effects or only a slight depression of locomotor activity. Chloroform fraction significantly increased the pentobarbital-induced sleeping time, produced a slight but significant hypothermia and antagonized tetrabenazine-induced ptosis, whereas the butanol fraction produced a slight potentiation of 5-HTP-induced head twitches and syndrome., Conclusions: The present results, together with previous pharmacological and phytochemical data, indicated that Hypericum grandifolium possess antidepressant-like effects in mice and that different constituents, such as the flavonoids and the benzophenone derivatives, could be responsible at least in part for the antidepressant effects observed for this species.

A study has been carried out on the chemical composition and in vivo anti-oedematogenic activity of several extracts from Hypericum grandifolium Choisy (Hypericaceae) collected in Tenerife (Canary Islands). The HPLC-MS analysis (HPLC-ESI/MS and HPLC-FT/MS) revealed the presence of hyperforin, flavonoids and probably benzophenone derivatives, while naphthodianthrones were absent. Pharmacological results revealed that the methanol extracts and the aqueous, butanol and chloroform fractions obtained therefrom possess anti-oedematogenic activity against TPA-induced ear oedema and carrageenan-induced paw oedema, the chloroform fraction being the most active. Subfractions derived from the chloroform fraction also showed anti-oedematogenic activity. From these results, it can be suggested that different constituents, such as the flavonoids and the benzophenone derivatives, could be responsible, at least in part, for the anti-oedematogenic effects observed for this species.

The present study investigates the analgesic and topical anti-inflammatory effects of the infusion, methanol extract and fractions of the aerial part in blossom of Hypericum reflexum L. fil. in mice. The acetic acid-induced writhing test, formalin test, tail flick test and the tetradecanoylphorbol acetate (TPA)-induced ear inflammation model in mice were used to determine these effects. Our findings show that oral administration of all extracts tested from this species significantly inhibit acetic acid-induced writhing in mice. Only the methanol extract and chloroform fraction were significantly active in both phases of formalin-induced pain and in the tail flick assays, suggesting that they may have central analgesic properties. On the other hand, the topical treatment of methanol extract, butanol and chloroform fractions of this species significantly reduced the TPA-induced ear oedema. In conclusion, the results indicate analgesic and topical anti-inflammatory activities in mice for the Hypericum species studied.

Different extracts and fractions from Sideritis candicans Ait. var. eriocephala Webb aerial part were investigated for their analgesic, anti-inflammatory and antimicrobial activities in mice. Results indicated that the extracts assayed showed anti-nociceptive activities because they were able to reduce the nociceptive response to chemical pain stimuli, such as in the acetic acid-induced writhing test. Moreover the extracts also possessed anti-inflammatory activity against carrageenan-induced paw oedema and TPA-induced ear oedema, being the chloroform fraction the most active. Further fractionation and analysis of this fraction revealed that the analgesic and anti-inflammatory activities found could be related in part to the presence of phytosterols, alpha and beta amyrin triterpenic derivatives and ent-kaurene type diterpenes in this species, since some of these compounds are endowed with these activities.

The infusions of the aerial parts in blossom of Hypericum canariense, H. glandulosum, H. reflexum and H. grandifolium (Hypericaceae) were evaluated for their pharmacological activity on the central nervous system in mice using various behavioural models including locomotor and muscle relaxant activity, effect on normal body temperature, pentobarbital-induced sleep, oxotremorine and tetrabenazine-induced syndrome, apomorphine-induced hypothermia and 5-hydroxytryptophan-induced head twitches, as well as a forced swimming test. These infusions did not alter significantly the locomotor activity, pentobarbital induced sleeping time and body temperature, with the exception of H. canariense which produced a slight but significant hypothermia. Additionally, no muscle relaxant or anticholinergic activity were observed. These infusions antagonized the ptosis and/or motor depression induced by tetrabenazine as well as shortening the immobility time in the forced swimming test. The observations suggest that the infusions of these Hypericum species possess antidepressant activity in mice, without inducing muscle relaxation, anticholinergic and sedative properties., (Copyright 2002 John Wiley & Sons, Ltd.)

A previous chemical study of Sideritis canariensis var. pannosa demonstrated the presence of some important classes of related organic compounds with anti-inflammatory activities. In the present study, the crude ethanol extract and the chloroformic and aqueous fractions of S. canariensis have been examined for their antimicrobial actions through the disk-diffusion method and for their anti-inflammatory and analgesic effects in several animal models. No relevant antimicrobial activity against the tested microorganisms was found. The chloroformic fraction was the most interesting, exhibiting a good analgesic and anti-inflammatory activity.

The present study examined the effect of several extracts of Visnea mocanera L. on the bleeding time and gastrointestinal transit in mice using the Duke test and charcoal meal method, respectively; they were also investigated in order to examine their renal effects. Results showed that V. mocanera extracts significantly inhibited both the bleeding time and gastrointestinal transit in mice. No diuretic activity of these extracts were detected. In contrast, they significantly reduced the urine volume. The study provides experimental support to the therapeutic advocation of V. mocanera in ethnomedicine for the treatment of diarrhoea and the healing of wounds.

A chemical study of Visnea mocanera leaves was carried out giving lupeol and beta-sitosterol fatty esters, as well as beta-sitosterol and the triterpenic betulinic, ursolic, platanic and 2 alpha,3 beta-dihydroxy-ursan-12-en-28-oic and 2 alpha,3 beta-dihydroxy-olean-12-en-28-oic acids. Studies of the antimicrobial activity of acetone and methanol extracts as well as an aqueous infusion were also performed and the good experimental results obtained justify the folk use of this species as a cicatrizant and vulnerary agent.