New Perspectives for the Use of Potentilla alba Rhizomes to Treat Thyroid Gland Impairments.

Potentilla alba is a valuable medicinal plant that has been highly praised even before its first appearance in herbal books; however, it has now been forgotten in Western Europe. Currently, this species is used in Eastern Europe as a remedy to treat dysentery and various thyroid gland dysfunctions. The present review summarizes the advances in the phytochemical, pharmacological, and toxicological research related to this plant species. Clinical trials that have been conducted to date support its traditional use for treating thyroid disorders, although its exact mechanism of action, bioavailability, and pharmacokinetics data are missing.

Recent phytochemical and pharmacological advances in the genus Potentilla L. sensu lato - An update covering the period from 2009 to 2020.

ETHNOPHARMACOLOGICAL RELEVANCE: Potentilla plants are still common herbal medicines used in folk medicine. This review provides an update of research undertaken on Potentilla from 2009 until 2020. AIM OF THE STUDY: This comprehensive review considers biological updates, recent advances in phytochemical and pharmacological research, and toxicological reports on Potentilla sensu lato based on available data since 2009. METHODS: A literature search was conducted using available databases including ScienceDirect, PubMed, Scopus, Web of Science, China National Knowledge Infrastructure and Google Scholar. RESULTS: Until now, more than 210 new and known compounds, including flavonoids, tannins, triterpenes and phenolic compounds, have been confirmed and elucidated for numerous Potentilla species, i.e., in the underground and aerial parts of this genus. Modern pharmacology studies have revealed that those structures are responsible for a broad spectrum of pharmacological activities, such as anti-neoplastic, antihyperglycemic, anti-inflammatory, antioxidant, hepatoprotective, neuroprotective, antibacterial and anti-yeast effects. CONCLUSIONS: However, in vitro studies must be re-considered due to the discovery of urolithins and their origins, including microbiota, which can lead to different results when applying Potentilla species and their extracts to in vivo conditions. Thus, future research should focus more on in vivo and particularly clinical studies to confirm the validity and safety of traditional uses. Particularly, the use of Potentilla alba extracts in the treatment of thyroid gland disorders should be further explored to confirm the underlying mechanism of their action, efficacy and safety. In addition, more clinical studies should focus on Potentilla erecta rhizome extracts for application as herbal remedies against dysentery, diarrhoea and inflammation of the skin.

Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A receptors.

Cardiac-valve regurgitation observed in Parkinson patients treated with the ergoline dopamine receptor agonist 8beta-methylthiomethyl-6-propylergoline (pergolide) has been associated with the agonist efficacy of the drug at 5-hydroxytryptamine(2B) (5-HT(2B)) receptors. 5-HT(2A) receptors may also play a role in pergolide-induced cardiac-valve regurgitation. We studied the pharmacological profile of pergolide and eight derivatives in porcine vascular rings endowed with 5-HT(2B) and 5-HT(2A) receptors to detect the molecular fragment of the pergolide molecule that may be responsible for agonism at these receptors. Pergolide derivatives showed a different substitution pattern at N(6), and the side chain at C(8) was modified by replacement of the sulfur against an oxygen atom. We demonstrate that the potent agonism of pergolide both at 5-HT(2B) and 5-HT(2A) receptors is retained when the N(6) propyl substituent is replaced by ethyl. However, agonism can be converted into antagonism if N(6) propyl is replaced by methyl. The N(6)-unsubstituted derivative was a low efficacy 5-HT(2B) receptor partial agonist and a 5-HT(2A) receptor antagonist. This pharmacological pattern was also applicable for pergolide congeners with an oxygen in the side chain at C(8). 6-Methylpergolide retained agonist efficacy and potency compared with pergolide at human (h) D(2LONG(L)) and hD(2SHORT(S)) receptors as determined by guanosine 5'-O-(3-[(35)S]thio)triphosphate binding. Based on the ability of pergolide to produce potent agonism at 5-HT(2B) receptors and the failure of 6-methylpergolide to act as an agonist but as a potent antagonist, we conclude that the N(6) propyl substituent of pergolide is crucial for 5-HT(2B) receptor agonism and thus a determinant of valvular regurgitation.

An ellagitannin, n-butyl gallate, two aryltetralin lignans, and an unprecedented diterpene ester from Pelargonium reniforme.

The structural diversity of the metabolic pool of Pelargonium reniforme was extended by the characterization of the 1C4-glucose based ellagitannin pelargoniin E, gallic acid n-butyl ester, (-)-4,4',9'-trihydroxy-3',5'-dimethoxy-2,7'-cyclolignan 9-O-beta-glucopyranoside and reniformin, a diterpene ester comprised of a diterpene acid with an uncommon -(CH2)(2)- bridging element linked to 2-(4-hydroxyphenyl)ethansulfonic acid. These metabolites were associated with the known (alpha,beta)-3,4-di-O-galloyl-glucopyranoside, 4,6-dihydroxy-2beta-glucopyranosyloxyacetophenone, 1-O-galloylglycerol, 6'-O-galloylsalidroside and (+)-isolariciresinol-9'-O-beta-glucopyranoside. All structures were established on the basis of spectroscopic methods.

Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes.

Ergot alkaloids act as (partial) agonists or antagonists at serotonergic, dopaminergic and alpha-adrenergic receptors. In contrast to their affinity at serotonergic (5-HT) and dopaminergic receptor subtypes, only limited information is available concerning their interaction with alpha-adrenoceptor subtypes. This especially holds true for native alpha-adrenoceptors. Therefore, we studied the pharmacological profile of 25 ergolines at alpha(1A)-, alpha(1B)- and alpha(1D)-adrenoceptors in vascular rings or strips of rat and guinea pig endowed with these receptors. Contractile responses were studied by measurement of isometric tension changes in rat tail artery (alpha(1A), alpha(1B)), guinea pig spleen (alpha(1B)) and rat thoracic aorta (alpha(1D)). The anti-migraine drugs ergotamine and dihydroergotamine, the anti-parkinsonian drug lisuride and the anti-hyperprolactinemic drug terguride behaved as antagonists or low-efficacy partial agonists at all three alpha(1)-adrenoceptor subtypes with nanomolar receptor affinity. Derivatives of these drugs showed lower affinity at alpha(1)-adrenoceptors than the parent compounds. Each individual ergoline derivative tested showed low discriminatory capability at the subtypes, alpha(1A), alpha(1B), alpha(1D). A low discriminatory power between the subtypes (alpha(1A), alpha(1B), alpha(1D)) seems to be a class effect of the ergolines. The nanomolar affinities of ergotamine, dihydroergotamine and lisuride for alpha(1)-adrenoceptors may affect their effectiveness as anti-migraine and anti-parkinsonian drugs, respectively.

O-Galloyl-C-glycosylflavones from Pelargonium reniforme.

The unique series of C-2''-acylated C-glycosylflavones is extended by the discovery of the C-8-glucosyl derivatives 2''-O-galloylvitexin and 2''-O-galloylorientin and their C-6 analogues 2''-O-galloylisovitexin and 2''-O-galloylisoorientin, representing the first described O-galloyl-C-glycosylflavones. They are accompanied in the aerial parts of Pelargonium reniforme by the known non-galloylated parent analogues vitexin, orientin, isovitexin and isoorientin, as well as several known flavonoid-O-glycosides. The structures of these compounds were established from spectroscopic studies. Differentiation between C-glycosylation at C-6 and C-8 is discussed on the basis of the effects of dynamic rotational isomerism.

Antioxidant properties of phenolic compounds from Pelargonium reniforme.

Flavonoids and hydrolyzable tannins isolated from Pelargonium reniforme were evaluated for their antioxidant ability using a 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical generating system and a luminol-dependent chemiluminescence assay. In both assays, the polyphenols tested showed higher radical scavenging activities than the reference antioxidant, ascorbic acid (IC50 2.6-32.9 microM vs 40.9 microM in the DPPH test, and 2-25 times stronger effects in the chemiluminescence assay). A comparison of the flavonoids and the tannins showed that the latter have more potential than the former. Structural requirements for marked antioxidant activities of hydrolyzable tannins were the presence of galloyl and hexahydroxydiphenoyl groups, and apparently carbonyl (ester) functionalities in oxidatively modified dehydrohexa-hydroxydiphenoyl moieties. For flavonoids, it appeared that a catechol (3',4'-dihydroxy) element in the B-ring were important determinants and that O-glycosides were more effective than flavone-based C-glucosyls. Conspicuously, introduction of a galloyl group significantly enhanced their potentials. The demonstrated marked antioxidant effects of the polyphenols provide a clue for beneficial effects of P. reniforme in the treatment of liver disorders among several ethnic groups in areas of southern Africa.

Health benefits and possible risks of broccoli - an overview.

Chemopreventive effects of broccoli, a highly valued vegetable, have been known for a long time. Several studies have demonstrated that broccoli might be beneficial by reducing the risk for the development of certain forms of cancer. These effects are generally attributed to glucosinolate-derived degradation products like isothiocyanates and indoles which are formed by the hydrolytic action of plant myrosinase and/or glucosidases deriving from the human microbial flora. However, recent in vitro and experimental animal studies indicate that broccoli, its extracts and the glucosinolate-derived degradation products might also have undesirable effects, especially genotoxic activities. However, the relevance of the genotoxic activities to human health is not known yet. This paper gives an overview on genotoxic, anti-genotoxic/chemopreventive, nutritive and antinutritive properties of broccoli, its ingredients and their degradation products. A qualitative comparison of the benefit and risk of broccoli consumption benefit-risk assessment shows that the benefit from intake in modest quantities and in processed form outweighs potential risks. For other preparations (fortified broccoli-based dietary supplements, diets with extraordinary high daily intake, consumption as a raw vegetable) further studies both for potential risks and beneficial effects are needed in order to assess the benefit and risk in the future.

Potentilla--a review of its phytochemical and pharmacological profile.

The genus Potentilla is a member of the family Rosaceae, subfamily Rosoideae, which is mainly distributed in temperate, arctic and Alpine zones of the Northern hemisphere. This genus has been known since ancient times for its curative properties. Extracts of the aerial and/or underground parts have been applied in traditional medicine for the treatment of inflammations, wounds, certain forms of cancer, infections due to bacteria, fungi and viruses, diarrhoea, diabetes mellitus and other ailments. This comprehensive review provides a botanical description of Potentilla species and their phytochemical constituents in the aerial and underground parts. In vitro and in vivo pharmacological studies are reviewed and discussed, focussing on antidiarrhoic, anti-ulcerogenic, anti-neoplastic, antiviral and antimicrobial, antihyperglycemic, anti-inflammatory, spasmolytic, hepatoprotective and antioxidative activities of Potentilla species. Most of the pharmacological effects can be explained by the high amount of tannins and to a lesser extent by triterpenes, present in all plant parts. However, future efforts should concentrate more on in vitro and in vivo studies and also on clinical trials in order to confirm traditional wisdom in the light of a rational phytotherapy. Especially the efficacy of Potentilla erecta rhizome extracts in the treatment of colitis ulcerosa and of viral infections should be further substantiated in clinical studies.

Determination of acute toxicity of the aqueous extract of Potentilla erecta (Tormentil) rhizomes in rats and mice.

Potentilla erecta, the tormentil, and its rhizome extracts have been known for a long time in traditional medicine as a remedy for the treatment of inflammations, wounds, and gastrointestinal disorders. Tormentil rhizomes have also been used as part of alcoholic beverages in Germany, the Ukraine, and Russia. Acute toxicity of an aqueous P. erecta rhizome extract was evaluated with a single dose administered by the intragastric route to rats and mice in dosages of 2.5 g/kg and 6.8 g/kg of body weight, respectively. Further, a single dose of this extract was applied intraperitoneally to rats and mice in dosages of 3.8 and 14.5 g/kg of body weight, respectively. After an observation period of 2 weeks after intragastric administration and 3 days following intraperitoneal administration, no mortality or any changes in appearance, behavior, or body weight occurred for both rats and mice in the high dosages mentioned. Macroscopic and microscopic studies of the internal organs of these rodents revealed no pathological changes. The data are in line with the long-time traditional use of P. erecta rhizome extracts and results from recent clinical trials in which no signs of any toxic effects have been known after the administration of a P. erecta rhizome extract for the treatment of ulcerative colitis in adults and rotavirus-induced diarrhea in children. Thus P. erecta rhizome extracts should be considered safe with respect to acute toxicity when applied to humans.