R. M. Giner

An Update Review of Saffron and its Active Constituents

This paper reviews the literature on recent research on the chemical composition and pharmacological activities of saffron (Crocus sativus) and its active constituents, mainly as antitumoral, hypolipidemic and tissue oxygenation enhancement agents.

Topical anti-inflammatory activity of some Asian medicinal plants used in dermatological disorders.

The topical anti-inflammatory activity of extracts from Cassia angustifolia, Rheum palmatum, Coptis chinensis, Phellodendron amurense and Scutellaria baicalensis, plants used in traditional East Asian medicine against different skin disorders, was studied. Though in different degree, all the extracts significantly inhibited the edema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), in both single or multiple application, oxazolone, and arachidonic acid (AA). None of the extracts inhibited in vitro the activity of phospholipase A(2) (PLA(2)) from Naja naja.

Influence of traditional Chinese anti-inflammatory medicinal plants on leukocyte and platelet functions.

The enzymes 5‐lipoxygenase and elastase are therapeutic targets in dermatological disorders such as psoriasis. Fifteen extracts from traditional Chinese medicinal plants used to treat topical inflammations were screened for their inhibitory effect on lipoxygenase, cyclooxygenase and elastase activity in intact leukocytes and platelets. Astragalus membranaceus, Forsythia suspensa and Poria cocos inhibited 5‐lipoxygenase, with IC50 values of 141, 80 and 141 μg mL−1, respectively. The latter two species, along with Angelica dahurica and Angelica pubescens, also inhibited elastase (IC50 values of 80, 123, 68 and 93 μg mL−1, respectively), while A. pubescens, Atractylodes macrocephala, Lentinus edodes, Rehmannia glutinosa and Paeonia lactiflora selectively inhibited 12‐(S)‐HHTrE production, a valid marker of cyclooxygenase activity. The inhibition of phospholipase A2 activity by P. cocos is discussed. Dehydrotumulosic and pachymic acids, which have been isolated from P. cocos, were shown to inhibit leukotriene B4 release. The results indicate that both P. cocos and F. suspensa are potentially valuable species in the management of skin pathologies involving chronic inflammation.

Anti-inflammatory effects of south american Tanacetum vulgare

In recent years the role of phenolic compounds and sesquiterpene lactones, particularly parthenolide, in the anti‐migraine and anti‐inflammatory effects of Tanacetum parthenium (Asteraceae) has attracted much attention. However, the closely‐related cosmopolitan species T. vulgare has remained outside the mainstream of research in this field.

Lanostanoids from Fungi: A Group of Potential Anticancer Compounds

Lanostanes are a group of tetracyclic triterpenoids derived from lanosterol. They have relevant biological and pharmacological properties, such as their cytotoxic effects via induction of apoptosis. This review compiles the most relevant lanostanoids studied from 2000 to 2011, principally those isolated from Ganoderma lucidum and other related fungi, such as Poria cocos, Laetiporus sulphureus, Inonotus obliquus, Antrodia camphorata, Daedalea dickinsii, and Elfvingia applanata, which have great potential as anticancer agents because of their cytotoxic or apoptotic effects. The compounds were selected on the basis of their proapoptotic mechanisms, through their ability to modify transcriptional activities via nuclear factors or genes and the activation or inhibition of pro- or antiapoptotic proteins; studies based only on their cytotoxicity were excluded from this review in the absence of complementary studies on their mechanisms of action. A total of 81 compounds from Ganoderma lucidum and other species from this genus are included, as well as 96 compounds isolated from other fungi, principally Poria cocos. Some of these compounds were found to arrest the cell cycle in the G1 phase, increase levels of p53 and Bax, or inhibit the phosphorylation of Erk1/2 or the activation of NF-κB and AP-1. Other lanostanes have inhibitory effects on the growth of androgen prostate carcinoma through increasing the expression of p21, which activates the tumor suppressor protein p53, while other compounds have been shown to selectively inhibit topo II activity without affecting topo I. General considerations concerning the chemical structure-biological activities of these compounds are also discussed.

Anti-inflammatory glycoterpenoids from Scrophularia auriculata

The activity of the four glycoterpenoids: two saponins, verbascosaponin A and verbascosaponin, and two iridoids, scropolioside A and scrovalentinoside, isolated from Scrophularia auriculata ssp. pseudoauriculata, were studied in different models of acute and chronic inflammation. Both saponins significantly inhibited the mouse paw edema induced by carrageenan and ear edema induced by single and multiple doses of 12-O-tetradecanoylphorbol 13-acetate (TPA). Verbascosaponin A showed a potency twice as high as that of indomethacin in the acute TPA model. Verbascosaponin A and scropolioside A were active after a long latency period against ethyl phenylpropiolate edema, as are glucocorticoids. When the putative corticoid-like mechanism of the two compounds was studied, verbascosaponin A activity was notably reduced by the mRNA synthesis inhibitor, actinomycin D, while the effect of scropolioside A was partially interfered with by the anti-glucocorticoid drugs used. Both iridoids were active on the delayed type hypersensitivity reaction. They significantly reduced the inflammatory lesion and suppressed the cellular infiltration.

Effect of triterpenoids on the inflammation induced by protein kinase C activators, neuronally acting irritants and other agents.

In order to establish the mode of the anti-inflammatory activity of triterpenoids, 11 naturally occurring compounds were assayed on mouse ear oedema induced by the protein kinase C activators, mezerein, 12-O-tetradecanoylphorbol-13-acetate (TPA), two 12-deoxyphorbol-13-monoesters (13-tetradecanoate (DPT) and 13-phenylacetate (DPP)) and bryostatin 1, and by resiniferatoxin, xylene and arachidonic acid. The effects on bradykinin-induced paw oedema and on the rat skin inflammation caused by hydrogen peroxide were also examined. The oedema induced by mezerein and DPT was reduced to different extents by the triterpenoids administered epicutaneously (0.5 mg per ear). Against DPT-induced oedema, lupane and oleanane derivatives were the most effective compounds. Oleananes and lupanes possessing a carboxyl group were active against bryostatin 1-induced oedema. Most of the triterpenoids were ineffective against the neurogenic inflammation caused by resiniferatoxin and xylene. Many triterpenoids, especially oleanane and lupane alcoholic derivatives, were active against the plantar oedema induced by bradykinin and on the intradermal inflammation induced by hydrogen peroxide. In conclusion, the anti-inflammatory activity of triterpenoids may depend on inhibition of protein kinase C, without any involvement of neurogenic inflammatory mechanisms.

Shikonin reduces oedema induced by phorbol ester by interfering with IκBα degradation thus inhibiting translocation of NF‐κB to the nucleus

Background and purpose:  In the present paper we studied the effect of shikonin on ear oedema induced by 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA), and determined the mechanisms through which shikonin might exert its topical anti‐inflammatory action.

Screening of antiinflammatory medicinal plants used in traditional medicine against skin diseases

The antiinflammatory activity of twelve medicinal plants used against skin disorders were tested in different experimental models of topical inflammation and one in vitro inhibitory test against phospholipase A2 (PLA2) from Naja naja venom. Forsythia suspensa was the most active species on the arachidonic acid (AA) topical test. This last species together with Astragalus membranaceus and Ranunculus sceleratus were the most active on the 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA) acute ear oedema test. Scrophularia auriculata was the most active on multiple topical applications of TPA and on the oxazolone‐induced delayed type hypersensitivity (DTH). Santolina chamaecyparissus was the only species that inhibited PLA2 in vitro.

Natural Triterpenoids as Anti-Inflammatory Agents

Abstract This chapter reviews the natural triterpenes with anti-inflammatory activity, including the traditional ones and the new compounds isolated over the last six years. Triterpenes are widely distributed in plants, and in many cases are the principles responsible for their anti-inflammatory effects. Many of these compounds are active in different in vivo experimental models such as hind paw edema induced by carrageenan, serotonin and phospholipase A 2 ; ear edema induced by phorbol and daphnane esters, ethylphenylpropiolate, arachidonic acid and capsaicin; adjuvant arthritis and experimental models of allergy. Other effects have been studied in vitro , and some triterpenes are active against inflammatory enzymes like 5-lipoxygenase, elastase and phospholipase A 2 . Others inhibit histamine, collagenase and interleukin release, lipid peroxidation and free radical-mediated processes, metabolism of endogenous corticoids, and complement and protein-kinase activities. In certain cases the mechanism of action depends on the skeleton type and/or substituents. For example, β-boswellic acid (ursane-derived) and derivatives markedly inhibit 5-lipoxygenase activity, whereas the principal mechanism of 18β-glycyrrhetinic acid (oleanane-derived) is the inhibition of endogenous corticoid metabolism. Some lanostanes are active against phospholipase A 2 ( e.g. ganoderic and dehydrotumulosic acids), and compounds with highly unsaturated rings can act as anti-peroxidatives ( e.g. celastrol, a tetraunsaturated friedooleanane).