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Methanolic extract from red berry-like fruits of Hypericum androsaemum: chemical characterization and inhibitory potential of central nervous system enzymes
No full textHypericum androsaemum is an evergreen shrub spread in the Mediterranean basin and cultivated in several European countries. The plant bears fleshy and berry-like capsules that ripen from red to shiny black. In several European conutries H. androsaemum has been traditionally used as diuretic, hepatoprotective, wound healing and as an antidepressant agent. The aim of the study was to evaluate the pharmaceutical potential of the methanolic extract of H. androsaemum red berries (HASE) through inhibition of CNS enzymes such as monoamine oxidase A (MAO-A), tyrosinase (TYR) and acetylcholinesterase (AChE). HASE was obtained by soxhlet extraction and analyzed by HPLC-DAD for the content of ten bioactive constituents. HASE activities were measured in terms of monoamine oxidase A (MAO-A),tyrosinase (TYR) and acetylcholinesterase (AChE) inhibition. HASE was very rich of shikimic acid and chlorogenic acid, occurring at concentration of 94941.7 and 39059.1 mg/kg,respectively. HASE was able to inhibit MAO-A and TYR in a dose dependent manner, although activity was not superior to positive control substances. On the basis of HASE composition and inhibitory effects on MAO-A and tyrosinase, red berries might represent an alternative Hypericum to obtain pharmacologically active substances
Chemical analysis of the essential oils from Schizogyne sericea growing in different areas of Tenerife (Spain)
No full textSchizogyne sericea, also known as ‘salado’, is a halophytic species widespread throughout all the Canary Islands (Spain), being more common in Tenerife and Gran Canaria. The plant has been traditionally used as analgesic, astringent, anti-inflammatory and vulnerary. The aim of this work was to investigate the chemical variability in the volatile profiles obtained from the flowering aerial parts of S. sericea harvested in different localities (Palm Mar, Los Roques and La Barranquera) of Tenerife characterized by different microclimates. For the purpose, the essential oils were hydrodistilled from the dried aerial parts by a Clevenger-type apparatus and analysed by GC-MS. A similar chemical composition for the oil samples from the different geographic areas was obtained. The aromatic monoterpene hydrocarbon p-cymene (43.0-57.0%) was by far the main component of the oils, with minor amounts of isobornyl acetate (4.5-11.0%), limonene (4.7-5.6%), β-pinene (0.7-5.3%), α-phellandrene (2.2-4.8%) and camphene (1.8-4.5%). Interesting to note was the occurrence of thymol derivatives that may be considered important chemotaxonomic markers of the genus Schizogyne, and, more in general, of the tribe Inulae. The volatile chemical profile obtained for S. sericea was similar to that of S. glaberrima previously studied
Polar Constituents, Essential Oil and Antioxidant Activity of Marsh Woundwort (Stachys palustris L.)
No full textStachys palustris, well‐known as marsh woundwort, is a perennial herb growing in wet environments of Europe. Its tubers, leaves and seeds are eaten raw or cooked. Alike other Stachys species, the plant is also used as a traditional remedy. Despite S. palustris has been consumed for centuries, little is known about its chemical constituents. In this work the main secondary metabolites of S. palustris from Hungary and France have been analysed. From the plant ethanolic extracts, ethanoid glucosides, isoscutellarein derivatives, caffeoyl‐quinic acids and iridoids have been isolated and structurally characterized by NMR. The essential oils were analysed by GC/MS and showed (E)‐phytol, fatty acids and carbonylic compounds as the most abundant compounds. The radical scavenging capacity of plant ethanolic extracts, as evaluated by the DPPH assay, was noteworthy, with IC50 values of 92.08 – 105.42 μg/ml
Analysis of food supplement with unusual raspberry ketone content
Get PDFIn recent years food supplement market increased constantly, including slimming products and against obesity. The case of rasberry ketone (RK) is here reported. HPTLC and HPLC-DAD analyses on a marketed product containing raspberry juice evidenced an abnormal quantity of RK, not in accordance with the juice natural content. The reported data confirm the need of adequate controls on marketed food supplements and the necessity of a complete adherence between labelling and real constitution of the product. Practical Applications: Determining the natural origin and assuring the consumers' safety for raspberry-based food supplement
Comparative toxicity of Helosciadium nodiflorum essential oils and blends of their major constituents against the cabbage looper, Trichoplusia ni (Lepidoptera)
No full texttThe chemical composition of the essential oils from the aerial parts of Helosciadium nodiflorum Apiaceae),obtained from two different localities in Italy, were analyzed by gas chromatography/mass spectrometry(GC/MS). Sample 1 (collected from Sulmona) was dominated by phenylpropanoids (49.1%) with myristicin(49.1%), (Z)--ocimene (19.0%), limonene (7.8%) and terpinolene (7.1%) as major constituents. Sample 2(collected from Colfiorito) was mainly composed of monoterpene hydrocarbons (58.7%) and the maincompounds of the oil were limonene (40.6%), myristicin (24.3%), dillapiol (9.4%) and -pinene (5.5%). Inorder to determine relationships between the chemical composition and insecticidal activity of the oils,comparative and synergistic interactions of the main constituents of H. nodiflorum essential oils wereinvestigated in third-instar larvae of the cabbage looper, Trichoplusia ni, via a contact toxicity bioassay.In the case of sample 1, myristicin was identified as a major active principle while in sample 2, limonene,myristicin and dillapiol were main insecticidal constituents. Several combinations of these compoundswere synergistic when topically applied, especially myristicin and (Z)--ocimene, or limonene
Valorizing overlooked local crops in the era of globalization: the case of aniseed (Pimpinella anisum L.) from Castignano (central Italy)
No full textIn the era of globalization, some local crops are at risk of extinction due to low competitiveness against products coming from foreign markets. This is the case of aniseed (Pimpinella anisum) from Castignano (Marche, central Italy), which was extensively cultivated in central Italy in the XIX century then abandoned after the global market favored products manufactured in Middle East countries. In order to support scientifically the recovery of this local crop, we performed a phytochemical investigation on the essential oil and polar compounds of aniseed cultivated in different fields of Castignano in the years 2013–2015 with the aim to demonstrate its high-quality value. For the purpose, the ‘Castignano ecotype’ samples were compared for essential oil yield, (E)-anethole levels and phenolic content with commercial samples of the Mediterranean area. Furthermore, several phenolic compounds were characterized by HPLC–MSn. Results showed that aniseed cultivated in Castignano contains higher content of essential oil and phenolic compounds than commercial samples, and provided the scientific rationale for its complete recovery and valorization
BIOASSAY-GUIDED FRACTIONATION OF TITHONIA DIVERSIFOLIA SECONDARY METABOLITES AGAINST TRYPANOSOMA BRUCEI
No full textHuman African Trypanosomiasis (HAT, or “sleeping sickness”) is a fatal vector-borne neglected disease caused by the protozoan pathogen Trypanosoma brucei (Tb).1 It is endemic in sub-Saharan Africa and is introduced into the mammalian host by the bite of an infected Tsetse fly (Glossina spp., family Glossinidae). HAT is caused by two distinct subspecies of T. brucei, T. b. gambiense (West Africa; Tbg) and T. b. rhodesiense (East Africa; Tbr), and both forms begin with a haemolymphatic stage and become fatal when the trypanosomes invade the central nervous system (CNS). HAT threatens primarily rural populations with poor medical care and is one of the very few infectious diseases with a mortality rate of 100% if left untreated.Currently existing therapies are either largely based on drugs that are extremely toxic and prone to show severe side effects, or they are not sufficiently available or applicable to the most seriously affected people, where the parenteral administration is inappropriate due to the poor medical infrastructures. Therefore,the search for novel active principles and lead structures for the discovery and development of cost-effective new drugsis hence an extremely urgent task. Medicinal plants represent nowadays a powerful tool for discovery of new lead compounds and standardized herbal medicines against trypanosomiasis.2In Africa, plants have been used traditionally for centuries and are still widely employed to treat sleeping sickness. However, little is known about the treatment of HAT with plant- derived drugs and no trypanocidal molecule from natural origin is currently used against T. brucei infections.3 Therefore, it is of prime importance to investigate plants used in African traditional medicine to treat parasitic diseases. One of them, Tithonia diversifolia (Hemsl.) A. Gray (Asteraceae), known as Mexican sunflower, a shrub or tree widespread distributed in tropical areas of South America, Asia and Africa is commonly used in the traditional medicine by local ethnic groups for treating diabetes, microbiological infections, snakebites, and malaria.4Focusing on the secondary metabolites from T. diversifolia, most reports highlight the sesquiterpene lactones (STL) as the prominent group. Among them, tagitinins are the most representatives in T. diversifolia, with tagitinin C being the lead compound.On the basis of the above-illustrated therapeutic potential, secondary metabolites with antitrypanosomal activity were identified through bioassay-guided fractionation and structurally elucidated by NMR and MS techniques. To achieve these objectives, extracts of various polarities were prepared from the aerial parts of T. diversifolia, and screened against the trypomastigote form of T. brucei (TC221 cell line). The results of this study will be discussed. References
1. Jacobs, R. T.; Nare, B.; Phillips, M. A. Curr. Top. Med. Chem. 2011, 11, 1255−1274.
2. Scotti, L.; Mendonça, F.J.; da Silva, M.S.; Scotti, M.T. Curr. Protein Pept. Sci. 2016, 17, 243-259.
3. Hannaert, V. Planta Med. 2011, 77, 586–597.
4. Orsomando, G.; Agostinelli, S.; Bramucci, M.; Cappellacci, L.; Damiano, S.; Lupidi, G.; Maggi, F.; Ngahang Kamte, S.L.; Biapa Nya, P.C.; Papa, F.; Petrelli, D.; Quassinti, L.; Sorci, L.; Vitali, L.A.; Petrelli, R. Ind. Crops Prod. 2016, 85, 181–189
Polar extracts from the berry-like fruits of Hypericum androsaemum L. as a promising ingredient in skin care formulations
No full textEthnopharmacological relevance: The top flowering aerial parts of the Hypericum species are traditionally used to prepare ointments to heal cuts and burns. Sometimes even the fruits are used for these purposes. Hypericum androsaemum L., commonly known as tutsan or shrubby St. John’s Wort, is a Mediterranean medicinal plant which has been traditionally used to prepare an ointment for treating cuts and wounds.
Aim of the study: To evaluate the extracts obtained from H. androsaemum red berries as functional ingredients for skin care formulations.
Materials and Methods: The methanolic extract was obtained by Soxhlet extraction while the aqueous extract was prepared by decoction; their composition was determined by HPLC analysis. Their biological activities were measured in terms of proliferation and migration of human fibroblasts, inhibition of collagenase activity, and immunomodulatory effects on human peripheral blood mononuclear cells (PBMCs). In addition, we evaluated their photostability by UV spectroscopy and their protective effects against APPH-induced hemolysis in red blood cells (RBC).
Results: The polar extracts contained significant amounts of shikimic (108143.7-115901.3 mg/kg) and chlorogenic acids (45781.1-57002.7 mg/kg). The main components of these extracts made an important contribution to a significant increase in human fibroblast migration. Both extracts were also active as collagenase inhibitors, with the aqueous one showing a greater inhibitory capacity (IC50 value of 88.1 μg/mL), similar to that of chlorogenic acid. The kinetic parameters determined for the enzymatic reaction revealed for both aqueous extract and chlorogenic acid an uncompetitive mechanism of inhibition. The methanolic extract showed important effects on PBMCs by modulating IL-6. Both extracts proved to be photostable in the UVA/B range and protected RBC against peroxidation at low concentrations.
Conclusions: H. androsaemum red berries were proven to contain phytochemicals that improve skin regeneration, hence potentially employable in skin care formulations
Phytochemical characterization of the berry like fruits of Tutsan (Hypericum androsaemum L.)
No full textAn overlooked horticultural crop, Smyrnium olusatrum, as a potential source of compounds effective against African trypanosomiasis
No full textAmong natural products, sesquiterpenes have shown promising inhibitory effects against bloodstream forms of Trypanosoma brucei, the protozoan parasite causing human African trypanosomiasis (HAT). Smyrnium olusatrum (Apiaceae), also known as Alexanders or wild celery, is a neglected horticultural crop characterized by oxygenated sesquiterpenes containing a furan ring. In the present work we explored the potential of its essential oils obtained from different organs and the main oxygenated sesquiterpenes, namely isofuranodiene, germacrone and β-acetoxyfuranoeudesm-4(15)-ene, as inhibitors of Trypanosoma brucei. All essential oils effectively inhibited the growth of parasite showing IC50 values of 1.9-4.0μg/ml. Among the main essential oil constituents, isofuranodiene exhibited a significant and selective inhibitory activity against T. brucei (IC50 of 0.6μg/ml, SI=30), with β-acetoxyfuranoeudesm-4(15)-ene giving a moderate potentiating effect. These results shed light on the possible application of isofuranodiene as an antiprotozoal agent to be included in combination treatments aimed not only at curing patients but also at preventing the diffusion of HAT
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