Lindera aggregata (Sims) Kosterm: review on phytochemistry and biological activities / Lindera agreggata (Sims) Kosterm: revisión de su fitoquímica y actividades biológicas

The genus Lindera consists of approximately 100 species that are widely distributed in tropical and subtropical areas throughout the world. Most Lindera plants, particularly Lindera aggregata is a well-known traditional Chinese medicine that has important medicinal value and health benefits. Contemporary chemical and pharmacological studies have shown that L. aggregata are a source of structurally diverse molecules having pharmacological potential. In an effort to promote research on L. aggregata and develop therapeutic and pharmacological products, this review describes the structural diversity of its components and pharmacological and biological significance of L. aggregata. This review is based on a literature analysis of scientific journals from electronic sources, such as Science Direct, PubMed, Google Scholar, Scopus and Web of Science. Thus, with the growing interest in traditional medicine and botanical drugs worldwide, L. aggregata will increasingly capture chemists' and pharmacologists' attention because they produce diverse and structurally novel compounds having pharmacological significance.

El género Lindera consta de aproximadamente 100 especies que están ampliamente distribuidas en áreas tropicales y subtropicales en todo el mundo. La mayoría de las plantas de Lindera, particularmente Lindera aggregata, es parte conocida de la medicina tradicional china con un importante valor medicinal y beneficios para la salud. Estudios químicos y farmacológicos contemporáneos han demostrado que L. aggregata es una fuente de moléculas estructuralmente diversas que con potencial farmacológico. En un esfuerzo por promover la investigación sobre L. aggregata y desarrollar productos terapéuticos y farmacológicos, esta revisión describe la diversidad estructural de sus componentes y la importancia farmacológica y biológica de L. aggregata. Esta revisión se basa en un análisis de literatura de revistas científicas de fuentes electrónicas, como Science Direct, PubMed, Google Scholar, Scopus y Web of Science. Por lo tanto, con el creciente interés en la medicina tradicional y las drogas botánicas en todo el mundo, L. aggregata captará cada vez más la atención de los químicos y farmacólogos debido a que producen compuestos diversos y estructuralmente novedosos que tienen importancia farmacológica.

Linderae radix ethanol extract attenuates alcoholic liver injury via attenuating inflammation and regulating gut microbiota in rats

This study aimed to explore the influence of gut microbiota alterations induced by Linderae radix ethanol extract (LREE) on alcoholic liver disease (ALD) in rats and to study the anti-inflammatory effect of LREE on ALD through the lipopolysaccharide (LPS) toll-like receptor 4 (TLR4)-nuclear factor kappa B (NF-κB) pathway. ALD rat models were established by intragastric liquor [50% (v/v) ethanol] administration at 10 mL/kg body weight for 20 days. Rats were divided into six groups: normal group (no treatment), model group (ALD rats), Essentiale group (ALD rats fed with Essentiale, 137 mg/kg), and LREE high/moderate/low dose groups (ALD rats fed with 4, 2, or 1 g LREE/kg). NF-κB and LPS levels were evaluated. Liver pathological changes and intestinal ultrastructure were examined by hematoxylin and eosin staining and transmission electron microscopy. The gut microbiota composition was evaluated by 16S rDNA sequencing. Expression levels of TLR4 and CD68 in liver tissue, and occludin and claudin-1 in intestinal tissue were measured. LREE treatment significantly reduced NF-κB and LPS levels, improved liver pathological changes, and ameliorated intestinal ultrastructure injury. Meanwhile, LREE-fed groups showed a higher abundance of Firmicutes and a lower abundance of Bacteroidetes than the rats in the model group. Administration of LREE suppressed TLR4 overexpression and promoted the expression of occludin and claudin-1 in intestine tissue. Thus, LREE could partly ameliorate microflora dysbiosis, suppress the inflammatory response, and attenuate liver injury in ALD rats. The protective effect of LREE might be related to the LPS-TLR4-NF-κB pathway.

Norisoboldine, a natural aryl hydrocarbon receptor agonist, alleviates TNBS-induced colitis in mice, by inhibiting the activation of NLRP3 inflammasome / 中国天然药物

Although the etiology of inflammatory bowel disease is still uncertain, increasing evidence indicates that the excessive activation of NLRP3 inflammasome plays a major role. Norisoboldine (NOR), an alkaloid isolated from Radix Linderae, has previously been demonstrated to inhibit inflammation and IL-1β production. The present study was to examine the effect of NOR on colitis and the underlying mechanism related to NLRP3 inflammasome activation. Our results showed that NOR alleviated colitis symptom in mice induced by 2, 4, 6-trinitrobenzene sulfonic acid (TNBS). Moreover, it significantly reduced expressions of cleaved IL-1β, NLRP3 and cleaved Caspase-1 but not ASC in colons of mice. In THP-1 cells, NOR suppressed the expressions of NLRP3, cleaved Caspase-1 and cleaved IL-1β but not ASC induced by lipopolysaccharide (LPS) and adenosine triphosphate (ATP). Furthermore, NOR could activate aryl hydrocarbon receptor (AhR) in THP-1 cells, inducing CYP1A1 mRNA expression, and promoting dissociation of AhR/HSP90 complexes, association of AhR and ARNT, AhR nuclear translocation, XRE reporter activity and binding activity of AhR/ARNT/XRE. Both siAhR and α-naphthoflavone (α-NF) markedly diminished the inhibition of NOR on NLRP3 inflammasome activation. In addition, NOR elevated Nrf2 level and reduced ROS level in LPS- and ATP-stimulated THP-1 cells, which was reversed by either siAhR or α-NF treatment. Finally, correlations between activation of AhR and attenuation of colitis, inhibition of NLRP3 inflammasome activation and up-regulation of Nrf2 level in colons were validated in mice with TNBS-induced colitis. Taken together, NOR ameliorated TNBS-induced colitis in mice through inhibiting NLRP3 inflammasome activation via regulating AhR/Nrf2/ROS signaling pathway.

Norisoboldine, a natural aryl hydrocarbon receptor agonist, alleviates TNBS-induced colitis in mice, by inhibiting the activation of NLRP3 inflammasome / 中国天然药物

Although the etiology of inflammatory bowel disease is still uncertain, increasing evidence indicates that the excessive activation of NLRP3 inflammasome plays a major role. Norisoboldine (NOR), an alkaloid isolated from Radix Linderae, has previously been demonstrated to inhibit inflammation and IL-1β production. The present study was to examine the effect of NOR on colitis and the underlying mechanism related to NLRP3 inflammasome activation. Our results showed that NOR alleviated colitis symptom in mice induced by 2, 4, 6-trinitrobenzene sulfonic acid (TNBS). Moreover, it significantly reduced expressions of cleaved IL-1β, NLRP3 and cleaved Caspase-1 but not ASC in colons of mice. In THP-1 cells, NOR suppressed the expressions of NLRP3, cleaved Caspase-1 and cleaved IL-1β but not ASC induced by lipopolysaccharide (LPS) and adenosine triphosphate (ATP). Furthermore, NOR could activate aryl hydrocarbon receptor (AhR) in THP-1 cells, inducing CYP1A1 mRNA expression, and promoting dissociation of AhR/HSP90 complexes, association of AhR and ARNT, AhR nuclear translocation, XRE reporter activity and binding activity of AhR/ARNT/XRE. Both siAhR and α-naphthoflavone (α-NF) markedly diminished the inhibition of NOR on NLRP3 inflammasome activation. In addition, NOR elevated Nrf2 level and reduced ROS level in LPS- and ATP-stimulated THP-1 cells, which was reversed by either siAhR or α-NF treatment. Finally, correlations between activation of AhR and attenuation of colitis, inhibition of NLRP3 inflammasome activation and up-regulation of Nrf2 level in colons were validated in mice with TNBS-induced colitis. Taken together, NOR ameliorated TNBS-induced colitis in mice through inhibiting NLRP3 inflammasome activation via regulating AhR/Nrf2/ROS signaling pathway.

Acaulosproa koreana, a New Species of Arbuscular Mycorrhizal Fungi (Glomeromycota) Associated with Roots of Woody Plants in Korea

A new species of arbuscular mycorrhizal fungi (Glomeromycota), Acaulospora koreana, was isolated from forest soils in South Korea. This novel fungus was collected from the rhizosphere of Lindera obtusiloba and Styrax obassia in forest and propagated with Sorghum bicolor in pot. Morphological characteristics of spores of A. koreana are rarely distinguished from Acaulospora mellea, which is reported as one of the most abundant mycorrhizal species in Korea. However, molecular evidence of rDNA sequence using improved primers for glomeromycotan fungal identification strongly supported that A. koreana is different from A. mellea but also any other species belonging to the genus Acaulospora. This is the first novel glomeromycatan fungus introduced in South Korea, but it suggests that there is a high possibility for discovering new arbuscular mycorrhizal fungi considering the abundance of plant species and advanced phylogenetic analysis technique.

Antiplatelet and Antithrombotic Effects of the Extract of Lindera obtusiloba Leaves

Lindera obtusiloba has been used in traditional herbal medicine for the treatment of blood stasis and inflammation. The leaves of Lindera obtusiloba have been reported to exhibit various physiological activities. However, there is little information available on their antiplatelet and antithrombotic activities. Thus, the present study aimed to evaluate the effect of Lindera obtusiloba leaf extract (LLE) on platelet activities, coagulation and thromboembolism. In a platelet aggregation study, LLE significantly inhibited various agonist-induced platelet aggregations in vitro and ex vivo. Furthermore, LLE significantly inhibited collagen-induced thromboxane A2 (TXA2) production in rat platelets. In addition, oral administration of LLE was protective in a mouse model of pulmonary thromboembolism induced by intravenous injection of a mixture of collagen and epinephrine. Interestingly, LLE did not significantly alter prothrombin time (PT) and activated partial thromboplastin time (aPTT). This study indicates that the antithrombotic effects of LLE might be due to its antiplatelet activities rather than anticoagulation. Taken together, these results suggest that LLE may be a candidate preventive and therapeutic agent in cardiovascular diseases associated with platelet hyperactivity.

Lindera obtusiloba Extends Lifespan of Caenorhabditis elegans

Lindera obtusiloba has been widely used as a traditional medicine for the treatment of lots of diseases, including abdominal pain, bruise, and hepatocirrhosis. Here in this study, we elucidated the lifespan-extending effect of methanolic extract of Lindera obtusiloba (MLO) using Caenorhabditis elegans model system. We found that MLO has potent lifespan extension activities under normal culture condition. Then, we determined the protective effects of MLO on the stress conditions such as osmotic, thermal and oxidative stress. To reveal possible mechanism of MLO-mediated lifespan, we further investigated the effect of MLO on the antioxidant enzyme activities and intracellular ROS levels. Our results demonstrated that superoxide dismutase and catalase activities were significantly up-regulated by MLO treatment, resulted in reduced intracellular ROS levels. In this work, we also tested whether MLO-mediated longevity activity was associated with aging-related factors such as food intake and growth. Our data revealed that both of pharyngeal pumping rate and body length were significantly shifted by MLO treatment, indicating these factors were involved in MLO's lifespan-extension effects. Although MLO induces reduction in food intake, the body movement of MLO-fed aged worms was not decreased, compared to untreated control worms, indicating MLO might extend lifespan without affecting healthspan.

Studies on anti-tumor metastatic constituents from Lindera glauca / 中国中药杂志

<p><b>OBJECTIVE</b>To study the anti-tumor metastatic constituents from Lindera glauca.</p><p><b>METHOD</b>Constituent isolation and purification was carried by repeated column chromatography (silica gel, Toyopearl HW-40 and preparative HPLC). Their structures were elucidated on the basis of spectral data analysis. The anti-tumor metastasis assay was applied to evaluate the isolated compounds of their activities.</p><p><b>RESULT</b>Ten compounds (1 - 10) were isolated and their structures were identified by comparison of their spectral data with literature values as follows: Laurotetanine (1), N-methyllaurotetanine (2), reticuline (3), pallidine (4), N-trans-feruloyltyramine (5), N-cis-feruloyltyramine (6), atheroline (7), norisosocorydine (8), [9,9,9-(2) H3]-(1S*, 3S*, 4S*, 8S*)-p-menthane-3,8-diol (9), [9,9,9-(2) H3 ]-(1S*, 3R*, 4S*, 8S*)-p-Menthane-3,8-diol (10). Compounds 1, 2, 4, 5, 7 and 9 showed positive anti-tumor metastatic activities,and compounds 1, 4, and 5 showed significant anti-tumor metastatic activities.</p><p><b>CONCLUSION</b>Compound 3 was isolated from this plant for the first time. Compounds 9 and 10 were isolated from Lindera genus for the first time. Compounds 1, 4, and 5 showed significant anti-tumor metastatic activities.</p>

Determination of norisoboldine in Radix Lindera by RP-HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a RP-HPLC method for quantitative determination of norisoboldine in Radix Linderae and to provide valuable data for quality control of Radix Linderae.</p><p><b>METHOD</b>The separation was performed on a Phenomenex Gemini C18 column (4.6 mm x 250 mm, 5 microm) at 25 degrees C using a gradient elution of mobile phase A (0.5% formic acid, adjusted pH 2.25 with triethylamine) and mobile phase B (acetonitrile). The detection wavelength was 280 nm.</p><p><b>RESULT</b>The calibration curve showed a good linearity (r = 0.999 9) within test ranges of 0.015-1.509 microg. The average recovery was 99.58% with RSD 1.4%.</p><p><b>CONCLUSION</b>The developed method is simple, accurate and reliable with good repeatability. It is suitable for quality evaluation of Radix Linderae.</p>

Simultaneous determination of three sesquiterpene lactones in Radix Linderae by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To develop an HPLC method for simultaneous determination of three major sesquiterpene lactones in Radix Linderae.</p><p><b>METHOD</b>The chromatographic separation was achieved on a Diamonsil C18 column (4.6 mm x 250 mm, 5 microm) using isocratic elution of acetonitrile-water (containing 0.1% H3 PO4) (45 : 55) at a flow rate of 1.0 mL x min(-1). Detection was carried out using a photodiode array detector at 220 nm.</p><p><b>RESULT</b>The calibration curves were linear in the range of 0.001 8-0.036 0 g x L(-1) for hydroxylinderstrenolide (R2 = 0.999 8), 0.016 2-0.323 2 g x L(-1) for neolinderalactone (R2 = 0.999 9), 0.010 5-0.209 9 g x L(-1) for linderane (R2 = 0.999 9), respectively. The average recoveries were 100.0% for hydroxylinderstrenolide, 98.8% for neolinderalactone and 98.9% for linderane with RSD not more than 3.3%.</p><p><b>CONCLUSION</b>The established method was proved to be simple, sensitive and credible, and can be applied to quality control of Radix Linderae.</p>

Inhibition of the Human Ether-a-go-go-related Gene (HERG) K+ Channels by Lindera erythrocarpa

Lindera erythrocarpa Makino (Lauraceae) is used as a traditional medicine for analgesic, antidote, and antibacterial purposes and shows anti-tumor activity. We studied the effects of Lindera erythrocarpa on the human ether-a-go-go-related gene (HERG) channel, which appears of importance in favoring cancer progression in vivo and determining cardiac action potential duration. Application of MeOH extract of Lindera erythrocarpa showed a dose-dependent decrease in the amplitudes of the outward currents measured at the end of the pulse (I(HERG)) and the tail currents of HERG (I(tail)). When the BuOH fraction and H2O fraction of Lindera erythrocarpa were added to the perfusate, both I(HERG) and I(tail) were suppressed, while the hexane fraction, CHCl3 fraction, and EtOAc fraction did not inhibit either I(HERG) or I(tail). The potential required for half-maximal activation caused by EtOAc fraction, BuOH fraction, and H2O fraction shifted significantly. The BuOH fraction and H2O fraction (100 microgram/mL) decreased gmax by 59.6% and 52.9%, respectively. The H2O fraction- and BuOH fraction-induced blockades of I(tail) progressively decreased with increasing depolarization, showing the voltage-dependent block. Our findings suggest that Lindera erythrocarpa, a traditional medicine, blocks HERG channel, which could contribute to its anticancer and cardiac arrhythmogenic effect.

Simultaneous determination of four alkaloids in Lindera aggregate by high performance liquid chromatography / 中国中药杂志

<p><b>OBJECTIVE</b>To develop an HPLC method for simultaneous determination of four major alkaloids in Lindera aggregate.</p><p><b>METHOD</b>The analysis was carried out on an Agilent ZORBAX SB-C18 column (4.6 mm x 250 mm, 5 microm) with gradient elution using acetonitrile-water (containing 0. 15% diethylamine, adjusted to pH = 3.0 with acetic acid) as mobile phase. Flow rate was 1.0 mL x min(-1) and the detection wavelength was at 289 nm.</p><p><b>RESULT</b>The calibration curves were linear over the range of 0.428-8.560 microg for boldine, 2.122-31.83 microg for norboldine, 0.760-15.20 microg for reticuline and 0.020 4-0.400 8 microg for linderegatine, respectively. The average recoveries were 99.18% for boldine, 101.0% for norboldine, 100.3% for reticuline and 99.17% for linderegatine, respectively. with RSD not more than 3.0%.</p><p><b>CONCLUSION</b>The described method is reliable and convenient and could be used for the quality control of Lindera aggregate.</p>

Influencing factors on dampproof effect of microcapsules and study on mechanism / 中国中药杂志

<p><b>OBJECTIVE</b>The influence of spray drying technology on the damp proof effect of microcapsules and the mechanism were studied.</p><p><b>METHOD</b>The microcapsules prepared with different spray drying parameters have been put in certain surroundings for 12 hours, then the hygroscopic curves were gotten; the mechanism was studied from the following aspects: solvent residue, film's shrink and particle size.</p><p><b>RESULT</b>The damp proof effect enhanced with the increase of inlet air temperature and the decrease of flow rate and air pressure. The properties of the wall, the solvent residue and particle size can influence the damp proof effect of the microcapsules.</p><p><b>CONCLUSION</b>The physical properties of microcapsules are different because of the different spray drying parameters, which lead to different damp proof effect of microcapsules.</p>

Evaluation of antioxidant activity of Radix Linderae and other two Chinese drugs using TLC-bioautography / 药学学报

<p><b>AIM</b>To evaluate the antioxidant capacity and quality of traditional Chinese medicines using TLC-bioautography.</p><p><b>METHODS</b>Two chromatograms of each crude drug sample were obtained, after developing, by spraying with 1,1-diphenyl-2-picrylhydrazyl (DPPH) solution in ethanol and classical stained reagents, separately. The images sprayed with DPPH solution were captured under light after the plates were heated at 40 degrees C for 30 min, and scanned using video scan software to get peak areas of active compounds.</p><p><b>RESULTS</b>Total peak areas of the spots on TLC were calculated to evaluate the antioxidant capacity of the tested crude drugs from different habitats and sources. The results indicated that Radix Linderae cultivated in Tiantai (Zhejiang province), Cortex Magnoliae Officinalis cultivated in Liangshan (Sichuan province), and Fructus Perillae acquired in Shanghai have the highest scavenging properties towards DPPH in their respective TLC-autographic assays. Norisoboldine, magnolol and honokiol, luteolin, apigenin and an unknown compound "U" proved to be the major antioxidant components in the corresponding crude drugs as they contribute the dominating peak areas to the total ones.</p><p><b>CONCLUSION</b>TLC-bioautography can not only be used for screening of the components with antioxidant potency but also for the purpose of quality evaluation of traditional Chinese medicines at the same time, and the method proved to be selective, simple and reproducible.</p>

Investigation on the molecular mechanisms of anti-hepatocarcinoma herbs of traditional Chinese medicine by cell cycle microarray / 中国中药杂志

<p><b>OBJECTIVE</b>To design DNA microarray and investigate the molecular anti-tumor mechanism of herbs of traditional Chinese medicine.</p><p><b>METHOD</b>cDNA microarrays consisting of 56 probes representing 24 human cell cycle genes were constructed, Four anti-hepatocarcinoma herbs including Radix Linderae, Hebra Artemisiae Annuae, Radix Amebiae, Radix Astragli, were chosen. Effects of herbs on SMMC-7721 cell cycle were observed by flow cytometry assay. Effects of herbs on cell cycle gene expression in SMMC-7721 cells were analyzed by comparing hybridization of Dig-Labeled cDNAs from herb-treated cells and cDNAs from untreated cells.</p><p><b>RESULT</b>Expressions of cell cycle geneswere changed in different degrees after herbs treated. Some genes were down-regulated and some genes were up-regulated. The changes in gene expression agreed with the results of flow cytometry assay.</p><p><b>CONCLUSION</b>The results suggest that these herbs may have effects on cell cycle and DNA damage checkpoint genes which may be the mechanism of the herbs, and DNA microarray can be used to investigate the biological function of extracts of traditional Chinese medicine.</p>

Alkaloids from the root of Lindera angustifolia / 药学学报

<p><b>AIM</b>To study the alkaloid constituents of the root of Lindera angustifolia Cheng.</p><p><b>METHODS</b>The constituents were isolated and purified by column chromatography and the structures were characterized by spectral analysis.</p><p><b>RESULTS</b>Seven aporphine alkaloids, laurotetanine (I), N-methyllaurotetanine (II), boldine (III), isoboldine (IV), norboldine (V), N-ethoxycarbonyllaurotetanine (VII) and a quaternary isoquinoline alkaloid, magnocurarine (VI), were isolated and identified. The structure of VII was further identified by semi-synthesis with I as starting material.</p><p><b>CONCLUSION</b>All compounds were obtained from this plant for the first time and compound VII was found as a naturally occurring compound for the first time.</p>

Determination of linderane in root tuber of Lindera aggregata by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To provide scientific basis for quality control of Lindera aggregata.</p><p><b>METHOD</b>HPLC analytical method was established using a Lichrospher C18 column and acetonitrile-water (56:44) as the mobile phase, detected at 235 nm.</p><p><b>RESULT</b>The linear range of linderane is between 0.0642 - 0.5774 microg, the average recovery was 98.4%, RSD1.7% (n = 9).</p><p><b>CONCLUSION</b>Contents of linderane in commercially available and collected samples were from 0.028% to 0.123% and from 0.056% to 0.222% respectively.</p>

Fitomedicina: usos más comunes en Dermatología / Herbal therapy in dermatology

Los suplementos herbales son productos obtenidos de plantas que se utilizan en el tratamiento de diversas enfermedades y condiciones médicas. La práctica de esta medicina natural se ha extendido a la dermatología y a pesar de que en la mayoría de los casos no existen estudios científicos comparativos que certifiquen su eficacia y seguridad, son bien aceptados sus beneficios en diversas patologías como por ejemplo: el ácido glicólico de la caña de azúcar en el acné, el aloe vera en quemaduras y heridas, la caléndula en infecciones, el té verde en el fotoenvejecimiento y el cáncer de piel, entre otras. En el presente trabajo se detallan las hierbas medicinales más usadas, las regulaciones existentes, los aspectos botánicos, históricos y prácticos de su uso en Dermatología