Antiproliferative effects of Ceratonia siliqua L. on mouse hepatocellular carcinoma cell line

Extracts from pods and leaves of carob (Ceratonia siliqua L.) were tested for their ability to inhibit cell proliferation of mouse hepatocellular carcinoma cell line (T1). The two extracts showed a marked alteration of T1 cell proliferation in a dose-related fashion reaching the maximal effect at 1 mg/ml. Moreover, we demonstrated that leaf and pod extracts were able to induce apoptosis in T1 cell lines after 24-h treatment mediating a direct activation of the caspase 3 pathway. HPLC analysis revealed the presence of gallic acid, (-) epigallocatechin-3-gallate and (-) epicatechin-3-gallate in pod and leaf extracts, compounds well known to exert antiproliferative effects. Their concentration reached 6.28 mg/g in carob leaves and 1.36 mg/g in carob pods extract. The discovery that carob pod and leaf extracts contained antiproliferative agents could be of practical importance in the development of functional foods and/or chemopreventive drugs.     

St. John's Wort seed and feverfew flower extracts relieve painful diabetic neuropathy in a rat model of diabetes

Painful diabetic peripheral neuropathy (DPN) is a common complication of diabetes and the few approved therapies for the management of pain have limited efficacy and side effects. With the aim to explore and develop new pharmacological treatments, we investigated the antihyperalgesic properties of St. John's Wort (SJW) and feverfew in streptozotocin (STZ)-diabetic rats. Acute administration of a SJW seed extract reversed mechanical hyperalgesia with a prolonged effect. A SJW extract obtained from the aerial portion of the plant and a feverfew flower extract partially relieved neuropathic pain whereas a feverfew leaf extract was ineffective. The antihyperalgesic efficacy of these herbal drugs was comparable to that of clinically used antihyperalgesic drugs (carbamazepine, lamotrigine, l-acetyl-levocarnitine). Further examinations of SJW and feverfew composition revealed that hyperforin and hypericin might be responsible for the antihyperalgesic properties of SJW whereas the efficacy of feverfew seems to be related to the presence of parthenolide. Rats undergoing treatment with SJW and feverfew did not show any behavioral side effect or sign of altered locomotor activity. Our results suggest that SJW and feverfew extracts may become new therapeutic perspectives for painful DPN.     

Hypotensive action of naturally occurring diterpenes: A therapeutic promise for the treatment of hypertension

Plants have always been an exemplary source of drugs and many of the currently available medicines have been directly or indirectly derived from them. For this reason, the research, development and use of natural products as therapeutic agents, especially those derived from plants, have been increasing in recent years. A great deal of attention has focused on the naturally occurring antispasmodic phytochemicals as potential drugs for the treatment of cardiovascular diseases. Arterial hypertension is a common and progressive disorder that poses a major risk for cardiovascular and renal diseases. Recent data have revealed that the global burden of hypertension is an important and increasing public health problem worldwide and that the level of awareness, treatment and control of hypertension varies considerably among countries. The research on naturally occurring blood pressure-lowering agents is rapidly expanding due to the high potential of such molecules as new antihypertensive drugs. Recently, a great number of plant-derived substances, such as diterpenoids, have been evaluated as possible antihypertensive agents. Naturally occurring diterpenes such as forskolin and stevioside, exhibit vasorelaxant action and inhibit vascular contractility by different mechanisms of action. In this review we will discuss the mechanisms underlying the hypotensive action displayed by diterpenes and their potential use in human hypertension. We will also discuss the use of these compounds in the treatment of glaucoma, which is characterized by increased intraocular pressure (IOP).     

Antibacterial and antifungal activity of Indonesian ethnomedical plants

Methylene chloride and methanol extracts of 20 Indonesian plants with ethnomedical uses have been assessed for in vitro antibacterial and antifungal properties by disk diffusion method. Extracts of the six plants: Terminalia catappa, Swietenia mahagoni Jacq., Phyllanthus acuminatus, Ipomoea spp., Tylophora asthmatica and Hyptis brevipes demonstrated high activity in this bioassay system. These findings should stimulate the search for novel, natural product such as new antibacterial and antifungal agents.     

Global proteomic analysis of Chelidonium majus and Corydalis cava (Papaveraceae) extracts revealed similar defense-related protein compositions

Chelidonium majus and Corydalis cava are phylogenetically closely related (Papaveraceae family). The medicinal and pharmaceutical interest in these plants is based on their synthesis of pharmaceutically important compounds, such as alkaloids, flavonoids, phenolic acids and proteins. C. majus shoot and C. cava tuber extracts have been used in traditional folk medicine to treat many diseases, such as fungal, bacterial and viral infections, liver disorders, fever, post-traumatic, colic, abdominal and menstrual pains and even cancer. This study attempts to perform a global comparative proteomic analysis of pharmacologically important extracts from these two closely related unsequenced plant species to gain insights into the protein basis of these plant organs and to compare their common and specific proteomic compositions.We used a shotgun proteomic approach combined with label-free protein quantitation according to the exponentially modified protein abundance index (emPAI). In total, a mean number of 228 protein identification results were recorded in C. cava tuber extracts and about 1240 in C. majus shoot extracts. Comparative analysis revealed a similar stress and defense-related protein composition of pharmacologically active plant species and showed the presence of different pathogenesis-related and low molecular inducible antimicrobial peptides. These findings could form the basis for further elucidation of the mechanism of the strong pharmacological activities of these medicinal plant extracts.     

Anti-HBV agents derived from botanical origin

There are 350,000 hepatitis B virus (HBV) carriers all over the world. Chronic HBV infection is at a high risk of developing liver cirrhosis and hepatocelluar carcinoma (HCC), and heavily threatened people's health. Two kinds of drugs approved by FDA for anti-HBV therapy are immunomodulators (interferon α, pegylated-interferon α) and nucleos(t)ide analogues (lamivudine, adefovir dipivoxil, entecavir, telbivudine, and tenofovir disoproxil fumarate). These drugs have been proved to be far from being satisfactory due to their low specificity, side effects, and high rate of drug resistance. There is an urgent need to discover and develop novel effective anti-HBV drugs. With vast resources, various structures, diverse biological activities and action mechanisms, as well as abundant clinical experiences, botanical agents become a promising source of finding new anti-HBV drugs. This review summarizes the recent research and development of anti-HBV agents derived from botanical origin on their sources and active components, inhibitory effects and possible toxicities, as well as action targets and mechanisms, and also addresses the advantages and the existing shortcomings in the development of botanical inhibitors. This information may not only broaden the knowledge of anti-HBV therapy, and offer possible alternative or substitutive drugs for CHB patients, but also provides considerable information for developing new safe and effective anti-HBV drugs.     

Advanced glycation inhibition and protection against endothelial dysfunction induced by coumarins and procyanidins from Mammea neurophylla

Advanced glycation end-products (AGEs) are associated with many pathogenic disorders such as pathogenesis of diabetes or endothelial dysfunction leading to cardiovascular events. Therefore, the identification of new anti-AGE molecules or extracts aims at preventing such pathologies. Many Clusiaceae and Calophyllaceae species are used in traditional medicines to treat arterial hypertension as well as diabetes. Focusing on these plant families, an anti-AGE plant screening allowed us to select Mammea neurophylla for further phytochemical and biological studies. Indeed, both DCM and MeOH stem bark extracts demonstrated in vitro their ability to prevent inflammation in endothelial cells and to reduce vasoconstriction. A bioguided fractionation of these extracts allowed us to point out 4-phenyl- and 4-(1-acetoxypropyl)coumarins and procyanidins as potent inhibitors of AGE formation, potentially preventing endothelial dysfunction. The fractionation steps also led to the isolation of two new compounds, namely neurophyllols A and B from the DCM bark extract together with thirteen known mammea A and E coumarins (mammea A/AA, mammea A/AB, mammea A/BA, mammea A/BB, mammea A/AA cycloD, mammea A/AB cycloD, disparinol B, mammea A/AB cycloE, ochrocarpin A, mammea A/AA cycloF, mammea A/AB cycloF, mammea E/BA, mammea E/BB) as well as δ-tocotrienol, xanthones (1-hydroxy-7-methoxyxanthone, 2-hydroxyxanthone) and triterpenes (friedelin and betulinic acid). During this study, R,S-asperphenamate, previously described from fungal origin was also purified.     

Prostaglandins and nitric oxide as molecular targets for anti-inflammatory therapy

Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most used drugs worldwide, in spite of their renal and gastric side effects. Medicinal plants may represent a useful source of new effective therapeutic agents, particularly considering the new findings concerning the mediators of inflammation, such as prostaglandins and nitric oxide. In fact, the discovery of two isoforms of the enzyme cyclooxygenase, which catalyzes the conversion of arachidonic acid to prostaglandins, has opened new interesting perspectives in the treatment of inflammatory diseases. As cyclooxygenase, also nitric oxide synthase, the enzyme which converts L-arginine to nitric oxide, exists in two isoforms. It appears that the constitutive isoforms of both enzymes (cyclooxygenase-1 and constitutive nitric oxide synthase) have a regulatory-physiological role, whereas the inducible isoforms (cyclooxygenase-2 and inducible nitric oxide synthase) are involved in inflammation. A number of medicinal plants have been screened for their ability to inhibit cyclooxygenase-2 and/or inducible nitric oxide synthase activity and/or expression.     

Recent advances in herbal medicines treating Parkinson's disease

Herbal medicines have attracted considerable attention in recent years, which are used to treat Parkinson's disease (PD) in China based on traditional Chinese medicine or modern pharmacological theories. We summarized and analyzed the anti-Parkinsonian activities of herbal medicines and herbal formulations investigated in PD models and provide future references for basic and clinical investigations. All the herbal medicines and herbal formulations were tested on PD models in vitro and in vivo. The relevant compounds and herbal extracts with anti-Parkinsonian activities were included and analyzed according to their genera or pharmacological activities. A total of 38 herbal medicines and 11 herbal formulations were analyzed. The relevant compounds, herbal extracts and formulations were reported to be effective on PD models by modulating multiple key events or signaling pathways implicated in the pathogenesis of PD. The plant species of these herbal medicines belong to 24 genera and 18 families, such as Acanthopanax, Alpinia and Astragalus, etc. These herbal medicines can be an alternative and valuable source for anti-Parkinsonian drug discovery. The plant species in these genera and families may be the most promising candidates for further investigation and deserve further consideration in clinical trials. Active components in some of the herbal extracts and the compatibility law of herbal formulations remain to be further investigated.     

Comparative studies on biological activities of Prunus padus and P. spinosa

Comparative studies on the antibacterial and free radical scavenging activities of the n-hexane, dichloromethane and methanol extracts of the seeds of Prunus padus and P. spinosa have been carried out. General toxicity of these extracts has also been determined.     

Investigation of Alternanthera repens and Bidens odorata on gastrointestinal disease

Alternanthera repens and Bidens odorata are used as medication for gastrointestinal diseases today, mainly in relation to diarrhea; therefore, pharmacological tests with aqueous and ethanol extracts of both species were carried out in mice. Using charcoal meal, the activity of the four extracts on intestinal motility was determined, finding that they inhibit the advance of the gastrointestinal content. Also, the lethal media doses were estimated in order to examine the plants' safety. The data confirmed the validity of the medicinal use for both plant species, contributing to explain the use of these plants as antidiarrheal agents in Mexican traditional medicine.     

Phytocomplexes from liquorice (Glycyrrhiza glabra L.) leaves--chemical characterization and evaluation of their antioxidant, anti-genotoxic and anti-inflammatory activity

Three extracts of different polarities of Glycyrrhiza glabra L. leaves were characterized and evaluated for their antioxidant, anti-genotoxic and anti-inflammatory activity. In total, thirty components have been identified and quantified through the use of liquid chromatography (LC) with ultraviolet-visible diode-array-detector (UV-vis-DAD) and mass spectrometry (MS). The main components belong to the polyphenols family, being flavonoid and dihydrostilbene derivatives. The extracts have been investigated for their antioxidant, anti-genotoxic and anti-inflammatory activities, which are fundamental requirements of efficacious chemo-preventive agents. The ethyl acetate extract proved to be the most valuable, evidently for the conspicuous presence of several polyphenols, namely flavonoids and dihydrostilbenes.     

Alkaloids as potential anti-tubercular agents

An increasing incidence of deaths due to tuberculosis and the known drawbacks of the current existing drugs including the emergence of multi drug-resistant strains have led to a renewed interest in the discovery of new anti-tubercular agents with novel modes of actions. The recent researches focused on natural products have shown a useful way to obtain a potentially rich source of drug candidates, where alkaloids have been found more effective. The present review focuses on current epidemiology of tuberculosis, synergy of the disease with HIV, current therapy, available molecular targets and, highlights why natural products especially alkaloids are so important. The review summarizes alkaloids found active against mycobacteria from the mid-1980s to late 2008 with special attention on the study of structure–activity relationship (SAR).     

植物源木材防腐剂增效技术研究进展

近年来,利用植物提取物制备木材防腐剂已成为木材保护研究领域的热点。单一植物提取物制备木材防腐剂的环境稳定性和防腐性存在局限,导致其应用总体效果较差。文中阐述国内外植物源木材防腐剂的提取物类型及其存在问题,综述利用化学药剂、微囊技术、纳米技术等增效植物源木材防腐剂的研究现状,讨论当前这些技术存在的问题与不足,并展望植物源木材防腐剂的开发应用前景。     

Betula pendula leaves: polyphenolic characterization and potential innovative use in skin whitening products

The research of new tyrosinase inhibitors is currently important for the development of skin whitening agents; particularly, birch leaves extracts are included in many skin cosmetic products. In this study, the potential ability of Betula pendula leaves ethanolic extract (BE) was evaluated on mushroom tyrosinase activity. Results showed that BE was capable to inhibit dose-dependently l-DOPA oxidation catalyzed by tyrosinase. The inhibition kinetics, analyzed by Lineweaver-Burk plots, showed a noncompetitive inhibition of BE towards the enzyme, using l-DOPA as substrate. The inhibitory mechanism of BE as studied by spectrophotometric analysis, demonstrated its ability to chelate copper ion in the active site of tyrosinase. In addition, BE exhibited Fe(2+)-chelating ability (IC(50)=614.12±2.14 μg/mL), reducing power and radical-scavenging properties (IC(50)=137.22±1.98 μg/mL). These results suggest the usefulness of birch leaves extracts in cosmetic and pharmaceutical industries for their skin-whitening and antioxidant effects. Determination of the polyphenolic compounds in BE extracts was afterward achieved by means of high-performance liquid chromatography (HPLC) with photodiode array (PDA) and mass spectrometry (MS) detection. A total of 25 compounds were positively identified, through the complementary analytical information, and are reported in such a matrix for the first time. Knowledge on the qualitative composition and contents of these natural sources in fact represents mandatory information, for rational consumption and correlation of the beneficial effects to the specific amounts.     

Thymoquinone vapor significantly affects the results of Staphylococcus aureus sensitivity tests using the standard broth microdilution method

The broth microdilution (BMD) method is widely used for the determination of minimum inhibitory concentrations of antimicrobial agents, including volatile oils and their components. In this series of various experiments, we have demonstrated the influence of thymoquinone (TQ) vapor on the results of the BMD test performed with Staphylococcus aureus as a model organism. The spread of vapor from the TQ containing wells (32–512 μg/mL) caused the complete inhibition of staphylococcal growth in adjoining wells initially containing bacterium-inoculated pure Mueller–Hinton broth only and thus produced false positive results of the test. The ability of TQ to pass into the adjoined wells was subsequently confirmed by gas chromatography–mass spectrometry, whereas TQ at concentrations up to 84 μg/mL was detected in these wells after five hours. Based on these results, we suppose that vapors of TQ as well as of other naturally occurring volatile compounds and their mixtures (for example essential oils and plant extracts) can significantly influence results of the standard BMD assay. These observations, therefore, call for development of new appropriate BMD method suitable for assessment of antimicrobial activity of volatile substances.     

Therapeutic orchids: traditional uses and recent advances — An overview

Orchids have been used as a source of medicine for millennia to treat different diseases and ailments including tuberculosis, paralysis, stomach disorders, chest pain, arthritis, syphilis, jaundice, cholera, acidity, eczema, tumour, piles, boils, inflammations, menstrual disorder, spermatorrhea, leucoderma, diahorrhea, muscular pain, blood dysentery, hepatitis, dyspepsia, bone fractures, rheumatism, asthma, malaria, earache, sexually transmitted diseases, wounds and sores. Besides, many orchidaceous preparations are used as emetic, purgative, aphrodisiac, vermifuge, bronchodilator, sex stimulator, contraceptive, cooling agent and remedies in scorpion sting and snake bite. Some of the preparations are supposed to have miraculous curative properties but rare scientific demonstration available which is a primary requirement for clinical implementations. Incredible diversity, high alkaloids and glycosides content, research on orchids is full of potential. Meanwhile, some novel compounds and drugs, both in phytochemical and pharmacological point of view have been reported from orchids. Linking of the indigenous knowledge to the modern research activities will help to discover new drugs much more effective than contemporary synthetic medicines. The present study reviews the traditional therapeutic uses of orchids with its recent advances in pharmacological investigations that would be a useful reference for plant drug researches, especially in orchids.     

Platelet-activating factor (PAF)-antagonists of natural origin

Presently herbal medicines are being used by about 80% of the world population for primary health care as they stood the test of time for their safety, efficacy, cultural acceptability and lesser side effects. The discovery of platelet activating factor antagonists (PAF antagonists) during these decades are going on with different framework, but the researchers led their efficiency in studying in vitro test models. Since it is assumed that PAF play a central role in etiology of many diseases in humans such as asthma, neuronal damage, migraine, cardiac diseases, inflammatory, headache etc. Present days instinctively occurring PAF antagonist exists as a specific grade of therapeutic agents for the humans against these and different diseases either laid hold of immunological or non-immunological types. Ginkgolide, cedrol and many other natural PAF antagonists such as andrographolide, α-bulnesene, cinchonine, piperine, kadsurenone, different Piper species' natural products and marine origin plants extracts or even crude drugs having PAF antagonist properties are being used currently against different inflammatory pathologies. This review is an attempt to summarize the data on PAF and action of natural PAF antagonists on it, which were evaluated by in vivo and in vitro assays.     

木材保护体系的发展

住宅用途的木材防腐剂正逐步走向包括微粒铜在内的新复合防腐剂体系,及无重金属的全有机体系.为了提高这些新防腐剂的性能,一类称为性能增强添加剂已经开发出来,如水分控制稳定剂,表面活性剂和乳化剂,防霉剂和着色剂等;针对人们对于化学防腐剂处理的木材越来越负面的看法,以及监督管理的审查和限制的加强,一些非传统的木材保护体系形成,如阻隔保护体系,化学改性和非化学改性,天然耐久树种木材也出现.笔者在文中对这些问题进行了回顾和讨论.     

Acylated flavonol glycosides from Epimedium elatum, a plant endemic to the Western Himalayas

Herba Epimedii is a well-known Botanical preparation used over long time in traditional Chinese medicine. The extracts and chemical constituents from Epimedium species are aphrodisiac as well as to treat many ailments. Chemical investigation of lonely species growing in Kashmir Himalaya Epimedium elatum was undertaken to evaluate its chemical profile. Two unusual substituted acylated flavonol glycosides named Elatoside A (1) and Elatoside B (2) have been isolated from the ethanolic extract of E. elatum along with 23 previously known ones (3-25). All isolates were evaluated for antimicrobial and PPAR-γ ligand binding activity, and some of them appeared to be modestly active.