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ContextLitsea cubeba(Lour.) Pers. (Lauraceae) has long been used as a folk remedy in Traditional Chinese Medicine (TCM) for the treatment of rheumatic diseases. Previous studies from our laboratory indicated thatL. cubebaextract showed anti-arthritic activity in rats. ObjectiveTo studyL. cubebachemically and biologically and to find the potential constituents responsible for its anti-arthritic effect. Materials and methodsThe compounds were isolated from the root ofL. cubebaby column chromatography which eluted with PE:EtOAc gradient system, and the structures were elucidated by detailed spectroscopic data analysis; the anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide (LPS)-induced RAW 264.7 cells and the TNF-α and NO level were measured by ELISA (commercial kit); The iNOS and COX-2 mRNA expression were measured by RT-PCR and the phosphorylation of IκBα, IKKβ, P38 and Akt were determined by western blots. ResultsA novel 9-fluorenone, 1-ethoxy-3,7-dihydroxy-4,6-dimethoxy-9-fluorenone (1), together with 4 known compounds, namely pinoresinol (2), syringaresinol (3), 9,9′-O-di-(E)-feruloyl-meso-5,5′-dimethoxysecoisolariciresinol (4) and lyoniresinol (5) were isolated from the root ofL. cubebafor the first time. The IC50for NO inhibition on compounds1and4were 56.1 ± 1.2 and 32.8 ± 2.3 μM, respectively. The IC50for TNF-α inhibition were 28.2 ± 0.9 and 15.0 ± 1.0 μM, respectively. Both1and4suppress mRNA expression of iNOS, COX-2 and protein phosphorylation of IκBα, IKKβ in LPS-induced RAW 264.7 cells. Discussion and conclusionCompounds1and4isolated fromL. cubebaexhibited potent anti-inflammatory activity through the NF-κB signal pathway. [ABSTRACT FROM PUBLISHER]

Context: Sinomenium acutum (Thumb.) Rehd. et Wils. (Menispermaceae, SA) has been used as a traditional Chinese medicine in the treatment of various diseases for hundreds of years; it possesses favorable effects against autoimmune diseases, especially rheumatoid arthritis (RA). A great number of investigations have been done on SA in the last decade, but they are usually scattered across various publications. Objective: The purpose of this article is to summarize and review the published scientific information about the chemical constituents, pharmacological effects, pharmacokinetics, and clinic applications of this plant since 2000. Results: The information for 89 cases included in this review was compiled. The SA contains alkaloids, sterols, phospholipids, and some other components. A great deal of pharmacological and clinic research has been done on sinomenine, a main compound from SA, which mainly focuses on the immune system, cardiovascular system, and nervous system. Conclusion: Previous studies strongly support its potential as an effective adaptogenic herbal remedy. There is no doubt that SA is being widely used now and will have extraordinary potential for the future. [ABSTRACT FROM AUTHOR]

Context: Vitex negundo Linn. (Verbenaceae) seeds are pepper substitute and occasionally used as a condiment for edible purposes. The seeds also find use for analgesia, sedation, rheumatism and joint inflammation in folk medicine. Objective: To isolate and characterize bioactive constituents from V. negundo seeds. Materials and methods: The ethanol extract of V. negundo seeds was subjected to repeated column chromatography. Chemical structures were elucidated by detailed spectroscopic analyses on the basis of NMR, IR, and MS data. Several pathogenic fungi isolates were employed to evaluate the antifungal activity of the isolated compound. Results: Chemical investigations of the seed extract afforded a new labdane diterpenoid, named negundol ( 1a + 1b), as an inseparable mixture of two diastereoisomers in a 5:4 ratio. Their structures were identified as ( rel 3 S, 5 S, 8 R, 9 R, 10 S, 13 S, 16 S)-3-acetoxy-9, 13-epoxy-16-hydroxy-labda-15, 16-olide ( 1a), and ( rel 3 S, 5 S, 8 R, 9 R, 10 S, 13 S, 16 R)-3-acetoxy-9, 13-epoxy-16-hydroxy-labda-15, 16-olide ( 1b). Compound 1 was active as an antifungal agent with MIC80 values in the range of 16-64 μg/mL. Discussion and conclusion: The presence of compound 1 in V. negundo is of chemotaxonomic significance, since plants under the genus Vitex are chemically characterized with labdane diterpenoids. Compound 1 exhibited potential antifungal activity and may be considered a lead compound for promising antifungal agent. [ABSTRACT FROM AUTHOR]

Context: Endophytic fungi are microorganisms living within the tissues of host plants, and have proven to be rich sources of biologically active secondary metabolites and therefore have attracted increasing attention in recent years. Objective: To isolate and characterize bioactive constituents from the endophytic fungus cultures of Crocus sativus Linn. (Iridaceae). Materials and methods: Endophytes were isolated from the corm of C. sativus. Endophytic fungus cultures were subjected to repeated column chromatography. Chemical structure was elucidated based on extensive spectroscopic methods and X-ray diffraction analysis. Several pathogenic fungi isolates and tumor cell lines were employed to evaluate the antifungal and cytotoxic activities of the isolated compound. Results: An isolate of Penicillium vinaceum (strain no. X17) was obtained from the corm of C. sativus. Chemical investigations of the endophyte culture broth afforded an unique quinazoline alkaloid (1), identified as (-)-(1R,4R)- 1,4-(2,3)-indolmethane-1-methyl-2,4-dihydro-1H-pyrazino-[2,1-b]-quinazoline-3,6-dione, which showed cytotoxic (IC50 range 40.55–76.83μg/mL) and antifungal (MIC80 range 16–64μg/mL) activities. Discussion and conclusions: Endophytes in C. sativus can be a rich source of novel bioactive compounds, which prompts us to expand the medicinal resource of this valuable plant in another way. Compound 1 exhibited potential cytotoxic and antifungal activities and may be considered a lead compound for promising antifungal and anticariogenic agent. [ABSTRACT FROM AUTHOR]

Context: Ligusticum chuanxiong Hort (LC; Umbelliferae) is an effective medical plant, which has been extensively applied for many years to treat various diseases with other Chinese herbal medicines. Although a considerable amount of scientific research was reported on LC in the last decade, it is currently scattered across various publications. The present review comprises the chemical and pharmacological research on LC in the last decade. Objective: The objective of this review is to bring together most of the scientific research available on LC and evaluate its effects and mechanisms. Methods: The information for 82 cases included in this review was compiled using major databases such as Medline, Elsevier, Springer, Pubmed, and Scholar. Results: The compounds contained in LC can be divided into five kinds, essential oil (EO), alkaloids, phenolic acids, phthalide lactones, and other constituents. A great deal of pharmacological research has been done, which mainly focuses on cardiovascular and cerebrovascular effects, antioxidation, neuroprotection, antifibrosis, antinociception, antiinflammation, and antineoplastic activity. Conclusion: A large number of pharmacological and chemical studies during the last 10 years have demonstrated the vast medicinal potential of LC. It is still very clear that LC is a plant with widespread use now and also with extraordinary potential for the future. The documents strongly support the view that LC has beneficial therapeutic properties and indicates its potential as an effective adaptogenic herbal remedy. [ABSTRACT FROM AUTHOR]

Context: Hypertrophic scarring, a common proliferative disorder of dermal fibroblasts, results from an overproduction of collagen and excessive deposition of extracellular matrix. Although the treatment with surgical excisions or steroid hormones can modify the symptoms, numerous treatment-related complications have also been established. Objective: To investigate the effects of essential oil (EO) from rhizomes of Ligusticum chuanxiong Hort. (Umbelliferae) on hypertrophic scarring in a rabbit ear model. Materials and methods: A rabbit ear model of hypertrophic scarring was established. EO (5, 10, and 20%) was applied once daily to the scars for 22 days. After 28 days of post-wounding, excision of scars was respectively performed for both histological examination and assays of the levels of collagen I, collagen III, matrix metalloproteinase-1 (MMP-1), and transforming growth factor beta 1 (TGF-ββ1). The scar elevation index (SEI) was also determined. Results: After 22 days of treatment with indicated concentrations of EO, hypertrophic scarring was significantly inhibited in the rabbit ears. The levels of TGF-ββ1, collagen I, and collagen III evidently decreased and MMP-1 level markedly increased in the scar tissue. SEI was also significantly reduced. Immunohistochemical findings exhibited significant amelioration of the scar tissue. Discussion and conclusion: EO suppresses hypertrophic scarring in the rabbit ear model and is a probably effective cure for human hypertrophic scarring. [ABSTRACT FROM AUTHOR]

Context: Crocus sativus Linn. (Iridaceae), commonly known as saffron, becomes more and more popular due to its versatile biological and medicinal properties. At present, studies mainly focus on the traditional medicinal part, the saffron stigma, with less attention to the other parts of saffron, such as the perianth, the stamen, and the corm, which are high yield compared to the stigma and also possess various pharmacological effects. Objective: To determine the chemical compositions, antifungal, cytotoxic, and antioxidant activities of the ether fractions from the stamen, perianth, and stigma of saffron. Materials and methods: The chemical constituents of the ether fractions from different parts of saffron were investigated by gas chromatography/mass spectrometry. Several pathogenic fungi isolates and tumor cell lines were employed to evaluate the antifungal and cytotoxic activities of these three ether fractions. 1,1-Diphenyl-2-picrylhydrazyl assay was used to determine the free radical-scavenging activity. Results: The ether fractions composition of the three C. sativus parts are different from each other, but lauric acid, hexadecanoic acid, 4-hydroxydihydro-2(3H)-furanone, and stigmasterol were the common constituents shared by all the three fractions. The stamen ether fraction displayed the strongest antifungal and cytotoxic activities, whereas both of the saffron stamen and perianth ether fractions exhibited significant antioxidant activities. Discussion and conclusion: These findings demonstrate that the saffron stamen and perianth possess significant antifungal, cytotoxic, and antioxidant activities as well as the stigma, though not to the same extent, prompting us to expand the medicinal resource and make best use of this valuable plant. [ABSTRACT FROM AUTHOR]

Context: In folk medicine in China, Desmodium caudatum (Thunb.) DC (Leguminosae) has been used to treat febrile diseases, rheumatic arthritis, and bacillary dysentery; nevertheless, there have been no reports on the analgesic, antipyretic, and anti-inflammatory effects of this plant in animals. Objective: To investigate the analgesic, anti-inflammatory, and antipyretic activities of D. caudatum extract (DCE) in animals. Materials and methods: The analgesic effect of DCE was measured in mice using the acetic acid-induced writhing test and the hot-plate test. The anti-inflammatory activity was assessed using the carrageenan-induced rat paw edema model and the dimethylbenzene-induced mouse inflammation model. The antipyretic effect was estimated using the lipopolysaccharide (LPS)-induced rat fever model. In addition, the acute oral toxicity of DCE was studied. Results: DCE significantly and dose-dependently inhibited the writhing responses in mice, increased reaction time in mice in the hot-plate test, reduced carrageenan-induced paw edema in rats and the dimethylbenzene-induced ear edema in mice, and attenuated LPS-induced fever in rats. Furthermore, no death was observed when mice were orally administered DCE up to 40 g/kg. Discussion and conclusion: DCE possesses evident analgesic, anti-inflammatory, and antipyretic activities, and has a favorable safety, which supports the use of D. caudatum as an analgesic, anti-inflammatory and antipyretic drug in folk medicine. [ABSTRACT FROM AUTHOR]

Context: Hypertrophic scarring following surgical procedures, trauma and especially burns can lead to severe functional and cosmetic impairment, causing a decrease in the quality of life. Although a wide choice of treatments is offered, few therapeutic methods are universally accepted because of their side effects. Objective: The effects of the essential oil (EO) extracted from rhizomes of Ligusticum chuanxiong Hort. (Umbelliferae) in human hypertrophic scar fibroblasts (HSFs) are investigated for the first time. Materials and methods: Chemical composition of hydrodistilled EO obtained from rhizomes of Ligusticum chuanxiong was analyzed by gas chromatography-mass spectrometry (GC-MS). The effects of EO on cell viability, apoptosis rate, mitochondrial membrane potential (MMP), lactate dehydrogenase (LDH), reactive oxygen species (ROS) and caspase-3 in HSFs were investigated. Results: The experimental results showed that EO significantly inhibited cell viability, elicited morphological changes and induced apoptosis in HSFs. EO also evidently increased the loss of MMP, the levels of LDH release and cellular ROS production, and the activity of caspase-3. Discussion and conclusion: EO-induced apoptosis was at least partially carried out via destruction of the intracellular antioxidant system and elicitation of excessive ROS accumulation in HSFs, which impaired mitochondrial membranes and elicited caspase-3 activation. EO could be an effective cure for human hypertrophic scar. [ABSTRACT FROM AUTHOR]

The protective effects of Semen Hoveniae extract (SHE) from Hovenia dulcis Thunb. (Rhamnaceae) on acute alcohol-induced liver injury were investigated in vivo using mice as test models. In the present study, SHE (150, 300, 600 mg/kg/day) was given to mice by intragastric administration for 4 days. Mice were gavaged with 60% ethanol 10 mL/kg after the last dose of extract. Six hours after alcohol administration, liver injury was evaluated by biochemical examination. Lipid peroxidation and the activity of antioxidants were measured by spectrophotometric methods. In mice, administration of SHE significantly decreased the activities of alanine aminotransferase (ALT) and aspartate transaminase (AST) in serum. Administration of SHE also protected against alcohol-induced alcohol dehydrogenase (ADH) elevation in mice. Concurrently, there was an augmentation in the activities of antioxidant enzymes such as superoxide dismutase (SOD), glutathione S-transferase (GST), and glutathione (GSH), and it also facilitated alcohol metabolism. Acute toxicity tests showed that a single dose of oral SHE up to 22 g/kg did not result in any death or toxic side effects in mice during 14 days’ observation. These results demonstrate that SHE could protect against acute alcohol-induced liver injury without any toxic side effects. Therefore, Semen Hoveniae has potential for the development of a clinically useful agent which could protect the liver from alcohol-induced injury. [ABSTRACT FROM AUTHOR]

The antinociceptive activities of the petroleum ether fraction (PEF) from the aqueous ethanol extract of Vitex negundo Linn. (Verbenaceae) seeds have been evaluated in several nociceptive mouse models. Given orally, the PEF (at doses of 12, 24, and 48 mg/kg body weight) produced significant dose-related inhibitions on chemical nociception induced by intraperitoneal acetic acid and sub-plantar formalin injections and on thermal nociception in the hot-plate test. Naloxone (1 mg/kg bw subcutaneously), a non-selected opioid receptor antagonist, notably reversed the analgesic effect caused by the PEF (48 mg/kg bw) when assessed against the first phase of the formalin test, but this effect was less significant for the PEF in the second phase. Our observations suggest that the PEF probably interacted with the opioid system and may be more effective on inflammatory pain. In addition, potent anti-inflammatory activity of the PEF was observed in the xylene-induced ear edema test, which further indicates that the analgesic effects of the PEF may be partially mediated by its anti-inflammatory activity. Further chemical analysis suggests that the analgesic activities of the PEF could be mostly due to the abundance of fatty acids with synergetic effects in the present work. [ABSTRACT FROM AUTHOR]

Context: Veronicastrum axillare (Sieb. et Zucc.) Yamazaki (Scrophulariaceae) embraces varieties of bioactivities such as anti-inflammatory, anti-pyresis and detoxification activity, while little is known of the phytochemical components of this medicinal plant. Objective: To isolate and identify bioactive constituents from the whole herb of V. axillare. Materials and methods: Ethanol extract of the whole herb of V. axillare was subjected to successive column chromatography. Chemical structures of the compounds were elucidated by detailed spectroscopic analyses on the basis of NMR, IR and HR-MS data. Results: A new monoterpenoid, axillacetal A ( 1) and a known analogue, tarumal ( 2), were isolated from the whole herb of V. axillare. The structure of tarumal ( 2) was also revised according to our NMR data. Discussion and conclusion: This is the first report on the isolation and authentication of novel chemical constituents from V. axillare. [ABSTRACT FROM AUTHOR]