Study on mechanism of hydroxy-a-sanshool on diabetic cardiomyopathy based on proteomics / 中国药理学通报

Aim To explore the mechanism of hydroxy-a-sanshool in the treatment of diabetic cardiomyopathy ( DCM) based on label-free quantitative proteomics detection technique. Methods DCM model was established by high fat diet and intraperitoneal injection of streptozotocin ( STZ) . They were divided into control group ( CON group ) , diabetic cardiomyopathy group (DCM group) and hydroxy-a-sanshool treatment group ( DCM + SAN group) . The cardiac function of mice was evaluated by echocardiography, the myocardial morphology was observed by pathology staining, the protective mechanism of hydroxy-a-sanshool on diabetic cardiomyopathy was speculated by proteomic technique , and the expression level of cAMP/PKA signaling pathway and key proteins were verified by Western blotting. Results Cardiac ultrasound and pathology staining showed that hydroxy-a-sanshool had protective effect on the heart of DCM mice. Label-free quantitative proteomic analysis was carried out between DCM + SAN group and DCM group, and 160 differential pro-teins were identified by proteomics, in which 127 proteins were up-regulated and 33 proteins were down regulated ; GO secondary functional annotations showed the biological process, molecular function and cellular component; KEGG enrichment analysis showed that cAMP signaling pathway was the most abundant; protein interaction network showed that PKA as the central node interacted with many proteins in the cAMP signaling pathway. Western blot showed that the relative expression of с AMP, PKA protein in DCM group was significantly lower than that in CON group ( P < 0. 05 ) , while the relative expression of cAMP, PKA protein in DCM + SAN group was significantly higher than that in DCM group ( P < 0. 05 ) . Conclusions Hydroxy-a-sanshool has protective effect on heart function of mice with diabetes, which plays a role through cAMP signaling pathway.

Research advance on structure and function of amides in Zanthoxylum plants / 中国中药杂志

Zanthoxylum belongs to the Rutaceae family, and there are 81 Zanthoxylum species and 36 varieties in China. Most of the Zanthoxylum plants are used as culinary spice. In recent years, scholars in China and abroad have carried out in-depth research on Zanthoxylum plants, and found that the peculiar numbing sensation of Zanthoxylum plants originates from amides. It is also determined that amides are an important material basis for exerting pharmacological effects, especially in anti-inflammatory analgesia, anesthesia and other aspects. In this paper, 123 amides in 26 Zanthoxylum plants and their pharmacological activity that have been reported were summarized, which provided scientific reference for the clinical application of Zanthoxylum plants and the research and development of new drugs, and also facilitated the sustainable development and utilization of Zanthoxylum plant resources.

Zanthoxylum bungeanum Aqueous Extract Treated Rheumatoid Arthritis by Inhibiting Synovial Cell Proliferation and Inducing Cell Apoptosis / 中国实验方剂学杂志

ObjectiveTo investigate the therapeutic effect of the water extract of Zanthoxylum bungeanum aqueous extract（ZBAE）on rheumatoid arthritis. MethodThe sixty SD rats were divided into normal group， model group ［complete Freund's adjuvant （CFA）， 10 mg·kg-1］， methotrexate（MTX） group （0.25 mg·kg-1）， low -， medium -， and high-dose ZBAE groups （90， 180， 360 mg·kg-1）. The rats in MTX group were given intraperitoneal injection for two weeks， three times a week， and the rats in ZBAE group were administrated for 14 days. The swelling of the ankle joint and body weight were observed， and arthritis scores were also performed. Computed tomography （CT）， hematoxylin-eosin （HE） staining and safranine-O and fast green staining were used to observe the effect of ZBAE on synovial hyperplasia and bone protection. Cell counting kit-8（CCK-8）method was used to detect the proliferation of the RA-FLSs cells treated with ZBAE. According to the results of CCK-8 experiment， the optimal concentration and time of administration were determined， blank group， low -， medium -， and high-dose ZBAE groups （0.08，0.10，0.12 g·L-1） were set up. The cell cycle distribution and apoptosis rate were analyzed by flow cytometry，the migration ability of RA-FLSs cells was examined by scratch test. Western blot was used to detect the effect of ZBAE on phosphatidylinositol 3-kinase （PI3K）， protein kinase B （Akt）， cyclin-dependent kinase 2 （CDK2）， Cyclin A and phosphorylated PI3K， Akt （p-PI3K，p-Akt） protein expression in RA-FLSs cells. ResultCompared with the normal group，joint swelling index and arthritis score were increased in the model group （P<0.05），the bone of the ankle was seriously damaged， and there was obvious synovial hyperplasia. Compared with the model group， the ZBAE group could significantly reduce the joint swelling index （P<0.05）， inhibit synovial hyperplasia and cartilage destruction. In vitro study showed that compared with the blank group， ZBAE could inhibit the migration of RA-FLSs （P<0.05）， promoted cell apoptosis （P<0.05）， and acted on RA-FLSs cells in S phase to inhibit cell proliferation. Moreover， the result of Western blot showed that compared with the blank group， the expression of p-PI3K， p-Akt， CDK2 and Cyclin A proteins were significantly decreased in the high dose group of ZBAE （P<0.05）. ConclusionThese results suggest that ZBAE has a therapeutic effect on rheumatoid arthritis by inhibiting synovial hyperplasia， promoting synovial apoptosis and inhibiting its migration.

Phenylpropanoids from Zanthoxylum species and their pharmacological activities: a review / 中国中药杂志

Phenylpropanoids are one of the major chemical constituents in Zanthoxylum species. They include simple phenylpropanoids, coumarins, and lignans and possess anti-tumor, anti-inflammatory, anti-platelet aggregation, anti-bacterial, anti-viral, insecticidal, and antifeedant activities. This review summarizes the chemical constituents and pharmacological activities from the Zanthoxylum plants in hopes of providing reference for the research and application of phenylpropanoids from this genus.

Genetic diversity and antibacterial activity of endophytic fungi from Zanthoxylum nitidum / 中国中药杂志

In order to reveal the distribution and population characteristics of endophytic fungi from Zanthoxylum nitidum and the antibacterial potential,this study performed molecular identification and analyzed the genetic diversity and antibacterial activity of endophytic fungi from Z. nitidum in Guangxi. Through culture and molecular identification,35 strains,belonging to 15 genera,12 families,10 orders,4 classes,and 2 phyla,were isolated from various tissues of Z. nitidum,of which Colletotrichum and Fusarium were the dominant genera,respectively accounting for 20% of total strains. The diversity of endophytic fungi was significantly different among roots,stems,and leaves,as manifested by the significantly higher Shannon index( H') in stems( 1. 678) than in roots( 0. 882 1) and leaves( 0. 515 4). The antimicrobial activity analysis showed that 14. 28% of endophytic fungi inhibited at least one indicator pathogen. Among them,Fusarium sp. ZN-34 and Fusarium sp. ZN-26 separately demonstrated the strongest inhibitory effect on Escherichia coli and Staphylococcus aureus. In general,Fusarium sp. ZN-26 and Phialemoniopsis plurioloculosa ZN-35 were advantageous in suppressing the two bacteria owing to the broad spectrum and strong efficacy. In summary,Z. nitidum in Guangxi boasts rich endophytic fungi with the majority showing strong antibacterial activity,which can be used as candidates for the extraction and separation of basic antibacterial substances and the development of natural antibacterial agents.

Extract from Zanthoxylum piperitum Induces Apoptosis of AGS Gastric Cancer Cells Through Akt/MDM2/p53 Signaling Pathway / 中国结合医学杂志

OBJECTIVE@#To determine the effect of Zanthoxylum piperitum extracet (ZPE) on apoptosis and analyze anticancer substances in ZPE, changes in proteins related to apoptosis, and pathological changes in tumors in mouse.@*METHODS@#Fifteen 4-week-old female BALB/c nu/nu mice were divided into 3 groups depending on ZPE dose, with 5 in each group. AGS gastric carcinoma cells (1 × 10@*RESULTS@#High performance liquid chromatography (HPLC) analysis showed that ZPE contained organic sulfur compounds such as alliin and S-allylcysteine. MTT assay results revealed that ZPE (10-85 µ g/mL) could effectively inhibit the growth of AGS gastric cancer cells at higher concentrations (P<0.05, P<0.01). The annexin V & dead cell staining assay and cell cycle arrest assay confirmed a dose-dependent increase in the apoptosis rate and G@*CONCLUSION@#ZPE decreases AGS cell proliferation and induces apoptosis by inhibiting Akt and MDM2 expression.

Analgesic and neuromotor effects of two extracts of Zanthoxylum rhoifolium (Rutaceae) in the Swiss albino mouse (Mus musculus) / Efectos analgésicos y neuromotores de dos extractos de Zanthoxylum rhoifolium (Rutaceae) en el ratón albino suizo (Mus musculus)

Background: Colombia has a high diversity of medicinal plants, including Tachuelo (Zanthoxylum rhoifolium), a tree belonging to the family Rutaceae, which has been attributed an analgesic use by communities of the Colombian southwest. Nevertheless, this species has been scarce studied in Colombia. The studies have been limited to the isolation of compounds with antifungal and insecticide activity, using the leaves, branches, and bark of the plant in aqueous, and organic extracts. Neither pharmacological tests have been carried out, nor the analgesic and neuromotor activity have been tested from preparations with this plant's fruits. Objectives: To evaluate the analgesic and neuromotor effect of the aqueous and hexane extract of the fruits of Z. rhoifolium.Methods: As there were no preliminary reports of this study, the first observation was made through Irwin's test. The formalin and the rotarod test were performed to determine the analgesic and motor coordination effects, respectively. Results: All the evaluated treatments demonstrated to generate analgesia, anesthesia, passivity, reduction in the alarm reaction, and have antinociceptive activity in the formalin test; while only the high dose of the nonpolar extract generated a deficit in the motor performance of the rodents in the rotarod test. Conclusions: the antinociceptive effect of the aqueous and hexane extracts of this species' fruits was demonstrated. The hexane extract generated a neuromotor effect, which validates the ethnobotanical reports on Z. rhoifolium fruits.

Antecedentes: Colombia tiene una alta diversidad de plantas medicinales, incluyendo al Ta chuelo (Zanthoxylum rhoifolium), un árbol de la familia Rutaceae al que se le ha atribuido un potencial analgésico debido al uso por parte de las comunidades del Suroccidente Colombiano. Sin embargo, esta especie ha sido poco estudiada en Colombia, limitándose al aislamiento de compuestos con actividad antifúngica e insecticida, empleando las hojas, ramas y corteza de la planta en extractos acuosos y orgánicos; sin embargo, no se han realizado ensayos farmacológicos ni se han probado la actividad analgésica y neuromotora a partir de preparaciones con los frutos de esta planta. Objetivos: Evaluar el efecto analgésico y neuromotor del extracto acuoso y en hexano de los frutos de Z. rhoifolium. Métodos: Al no haber reportes preliminares de este estudio, se realizó la primera observación mediante el test de Irwin. Para determinar el efecto analgésico y neuromotor se realizó el test de formalina y el test de rotarod, respectivamente. Resultados: Todos los tratamientos evaluados demostraron generar analgesia, anestesia, pasividad, reducción en la reacción de alarma, tener actividad antinociceptiva en el test de formalina, mientras que solo la dosis alta del extracto apolar generó un déficit en el rendimiento motor de los roedores en el test de rotarod. Conclusiones: Se demostró el efecto antinociceptivo del extracto acuoso y en hexano de los frutos de esta especie y el efecto neuromotor generado por el extracto en hexano, validando los reportes etnobotánicos sobre los frutos de Z. rhoifolium.

Sickling Cells Inhibition and Radical Scavenging Activities of Zanthoxylum leprieurii’s (GUILL) Bark Extracts: Comparative Study

Aims:In traditional medicine, several plant species from Rutaceae’s family have been used to treat sickle cell anemia. However, more studies are needed to corroborate the antisickling activity of Zanthoxylumleprieuriispecies. The objective of this paper was to evaluate the sickling cell inhibition and radical scavenging activities of hydroethanolic and aqueous extracts of Zanthoxylum leprieurii’s bark, a plant species used in the management of sickle cell anemia in eastern Côte d’Ivoire.Methods:Hydroethanolic and aqueous extracts of the stem bark of Zanthoxylum leprieuriiwere prepared. Qualitative and quantitative phytochemical tests were carried out. In addition, diphenyl 1 2 picrylhydrazyl (DPPH) was used to determine the antioxidant potential of these two extracts. The antisickling activity of two extracts was determined by the Emmel method.Resultsand Discussion: Zanthoxylum leprieurii’s barkextracts have demonstrated antioxidant property. The IC50value of the hydroethanolic extract (0.308±0.06) was lower than that of the decocted (0.434 ±0.06). At 10mg/mL, the sickling cell inhibition of DZL was 81% ±2.66 while EZL was 89% ±0.44. The presence of alkaloids, sterols, Polyterpenes and phenolic compounds in both extracts could explain the sickling inhibition activity of these extracts. All the extracts revealed an antioxidant and antisickling activities higher than the standard.Conclusion: The hydroethanolic extract (EZL) demonstrated a higher antisickling activity and exhibited a better free radical scavenging activity.The use of Zanthoxylum leprieurii’s bark in the traditional management of sickle cell anemia is justified

Evaluación genotóxica de las moléculas con efectos tripanocida y leishmanicida cantin-6-ona y 5-metoxicantin-6-ona en células de médula ósea de ratones / Genotoxic evaluation of the molecules with trypanocidal and leishmanicidal effects, canthin-6-one and 5-methoxycanthin-6-one in mouse bone marrow cells

La tripanosomiasis americana y la leishmaniasis son problemas de salud pública relevantes en Iberoamérica. Las drogas utilizadas actualmente para el tratamiento de estas enfermedades poseen efectos colaterales tóxicos severos. Varios grupos de investigación están abocados a la búsqueda de productos naturales y sintéticos para encontrar nuevos agentes terapéuticos efectivos que no presenten reacciones colaterales adversas. En la evaluación de compuestos de la especie vegetal Zanthoxylum chiloperone (Rutaceae), se demostró que compuestos aislados del extracto presentaban actividad leishmanicida, tripanocida y antifúngica in vivo. Teniendo como antecedentes estos resultados, en el presente estudio se evaluaron los efectos genotóxico y citotóxico del cantín-6-ona y del 5-metoxicantin-6-ona, moléculas aisladas de la planta, en células de médula ósea de animales tratados. El estudio de los efectos genotóxicos se hizo a través del ensayo de modificaciones en la frecuencia de micronúcleos y el efecto citotóxico por modificaciones en la relación entre eritrocitos policromáticos y eritrocitos normocromáticos. Se realizaron 2 ensayos independientes y en cada ensayo los animales fueron divididos en tres grupos de tratamiento: GRUPO I: control negativo que recibió 200 uL de agua y 2.1% de DMSO, vía oral, GRUPO II: compuesto a ser evaluado (canthin-6-ona o 5-methoxicantin-6-ona) con 2.1% de DMSO, y GRUPO III: control positivo que recibió ciclofosfamida 50mg/kg/peso del animal, vía intraperitoneal. El análisis estadístico mostró que ambos compuestos no presentaron efectos genotóxicos ni citotóxicos. Estos resultados permiten proponer a estas moléculas como candidatas a ser sometidas a estudios más detallados como potenciales fármacos contra estas dos enfermedades

American trypanosomiasis and leishmaniasis are relevant public health problems in Latin America. The drugs currently used to treat these diseases have severe toxic side effects. Several research groups are dedicated to the search of natural and synthetic products to find new effective therapeutic agents that do not present adverse collateral reactions. In the evaluation of compounds of the plant species Zanthoxylum chiloperone (Rutaceae), it was shown that isolated compounds of the extract had leishmanicidal, trypanocidal and antifungal in vivo activities. Based on these results, the genotoxic and cytotoxic effects of canthin-6-one and 5-methoxycanthin-6-one, molecules isolated from the plant, on bone marrow cells of treated mice were evaluated in the present study. The study of genotoxic effects was made through the test of modifications in the frequency of micronuclei and the cytotoxic effects by modifications in the relationship between polychromatic erythrocytes and normochromic erythrocytes. Two independent assays were performed and in each assay the animals were divided into three treatment groups: GROUP I: negative control that received 200 µL of water and 2.1% of DMSO, orally, GROUP II: compound to be evaluated (canthin-6 -one or 5-methoxycanthin-6-one) with 2.1% DMSO, and GROUP III: positive control that received cyclophosphamide 50mg /kg animal weight, intraperitoneal. Statistical analysis showed that both compounds had neither genotoxic nor cytotoxic effects. These results allow these molecules to be proposed as candidates to be subjected to more detailed studies as potential drugs against these two diseases

Chemical Constituents from Stems of Zanthoxylum bungeanum / 中国实验方剂学杂志

Objective::To isolate and identify the chemical constituents from the 95%, 75%ethanol extracts of the stems of Zanthoxylum bungeanum. Method::The 25 kg stems of Z. bungeanum were extracted with 95%, 75%ethanol for three times, and the combined filtrates were concentrated under vacuum to get the extracts. The 95%extracts were then extracted by petroleum ether, dichloromethane, ethyl acetate and n-butanol successively to obtain corresponding fractions. Such fractions and 75%extracts were isolated and purified by silicagel, Sephadex LH-20, ODS, preparation HPLC and recrystallization to obtain compounds. Their structures were identified by mass spectroscopy (MS), and nuclear magnetic resonance (NMR). Result::Sixteen compounds were isolated from the stems of Z. bungeanum and identified as dictamnine(1), decarine(2), zanthobungeanine(3), pseudocolumbamine(4), skimmianine(5), norchelerythrine(6), osthenol(7), dimethylfraxetin(8), 3, 4, 5-trimethoxycinnamylalcohol(9), asarinin(10), yangambin(11), syringaresinol(12), ashantin(13), bis(2-ethylhexyl) benzene-1, 2-dicarboxylate(14), 24-propylcholesterol(15), and sucrose(16). Conclusion::Compounds pseudocolumbamine(4), 3, 4, 5-trimethoxycinnamylalcohol(9), and 24-propylcholesterol(15)were isolated from the genus of Zanthoxylum for the first time and compounds dictamnine(1), osthenol(7), dimethylfraxetin(8), asarinin(10), yangambin(11), syringaresinol(12), ashantin(13), and bis(2-ethylhexyl) benzene-1, 2-dicarboxylate(14)were isolated from this plant for the first time.

Study on Inhibitory Effect of Volatile Oils in 16 Plants on Aspergillus flavus of Platycladi Semen / 中国实验方剂学杂志

Objective::To select volatile oils from 16 species of plants (Cymbopogon citratus, Pelargonium graveolens, Pinus tabulieformis, Litsea cubeba, Mentha haplocalyx, Zingiber officinale, Syzygium aromaticum, Curcuma longa, Zanthoxylum bungeanum, Cinnamomum cassia, Ocimum basilicum, Rosmarinus officinalis, Zanthoxylum schinifolium, Zanthoxylum armatum, Illicium verum, Myristica fragrans) that have good inhibitory effect on the growth of Aspergillus flavus. Method::Aspergillus flavus was isolated from the surface of Platycladi Semen medicinal materials by plate culture method. The volatile oils of 16 plants were extracted by steam distillation. The colony diameter of Aspergillus flavus was determined by fumigation of filter paper, and the effect of volatile oils on the growth of Aspergillus flavus was systematically studied. Result::Aspergillus flavus was successfully isolated from Platycladi Semen by means of morphological, microscopic and DNA barcoding identification methods, the bacteriostatic rates of the above 16 kinds of volatile oils against Aspergillus flavus were 2.93%, 0.05%, 0.37%, 76.07%, 0.34%, 0.15%, 50.05%, 8.51%, 1.43%, 58.20%, 0.07%, 2.60%, 8.73%, 100.00%, 52.62%, 0.07%, respectively. Conclusion::The volatile oils of 16 plants all have different degrees of antibacterial activities for Aspergillus flavus, and volatile oils of Zanthoxylum armatum, Litsea cubeba and Cinnamomum cassia have good inhibitory effect. This study can provide a theoretical basis for the prevention and control of Aspergillus flavus in the growth and storage of Platycladi Semen, and provide a basis for further research on plant volatile oil as bacteriostatic agents in the storage process of traditional Chinese medicine.

Chemical Constituents of Pericarps of Zanthoxylum bungeanum / 中国实验方剂学杂志

<b>Objective::To study the chemical constituents of pericarps of <italic>Zanthoxylum bungeanum</italic>. <b>Method::The dried pericarps of <italic>Z</italic>. <italic>bungeanum</italic> were smashed, and then extracted and concentrated in 95%ethanol to obtain the total extract. The total extract was loaded on a silica gel CC, eluted with different polar solvents in sequence, and then concentrated to obtain corresponding parts. The methylene chloride fraction and the <italic>n</italic>-butanol fraction were separated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, ODS column chromatography, semi-preparative HPLC, etc. And their structures were identified based on physicochemical properties and various spectroscopic methods. <b>Result::Fourteen compounds were isolated from the dichloromethane fraction and the n-butanol fraction of the <italic>Z</italic>. <italic>bungeanum</italic> and identified as(1<italic>S</italic>, 3<italic>S</italic>)-1-methyl-1, 2, 3, 4-tetrahydro-<italic>β</italic>-carboline-3-carboxylic acid(<bold>1</bold>), (3<italic>S</italic>)-1, 2, 3, 4-tetrahydro-<italic>β</italic>-carboline-3-carboxylic acid(<bold>2</bold>), apigenin-7, 4′-dimethyl ether(<bold>3</bold>), genkwanin(<bold>4</bold>), lcariside F₂(<bold>5</bold>), breyniaionoside A(<bold>6</bold>), 3-methoxyphenethyl alcohol-4-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopynanoside(<bold>7</bold>), 1-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopyranosyloxy-3-methoxy-5-hydroxybenzene(<bold>8</bold>), orcinol-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>9</bold>), syringin(<bold>10</bold>), 4-[(3<italic>S</italic>)-3-hydroxybutyl]-2-methoxyphenyl-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>11</bold>), (+ )-lyoniresinol-3a-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>12</bold>), 2-methylpropanyl-6-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-apiofuranosyl-<italic>β</italic>-<italic>D</italic>-glucopyranoside(<bold>13</bold>)and(<italic>E</italic>)-6-hydroxy-2, 6-dimethylocta-2, 7-dienoic acid(<bold>14</bold>). <b>Conclusion::All compounds were isolated from <italic>Z</italic>. <italic>bungeanum</italic> for the first time, and compounds <bold>1-4, 12</bold> and <bold>14</bold> were isolated from this genus for the first time.

Transcriptome and quality evaluation of Sichuan Dao-di herbs Zanthoxylum bungeanum / 中国中药杂志

"Huajiao" is dried ripe fruit peel of Zanthoxylum bungeanum or Z. schinifolium, is konwn as geoherbs, especially the "Dahongpao" cultivated in Hanyuan, Maoxian and Jiulong of Sichuan province. However, the genetic basis of Dao-di "Huajiao" is virtually unknown. The transcriptome of the fruit and leaf from Sichuan(Hanyuan, Jiulong, Lixian, Maoxian), Gansu(Wudu) province and Shaanxi(Fengxian) province was sequenced. Trinity de novo assembling resulted in a total of 177 616 unigenes. Through the KEGG, NR, SwissProt, Trembl, KOG/COG, GO, Pfam database comparision 106 644 annotated Unigene finally, 4 574 deferentially expressed genes were found in fruit between Sichuan and other provinces, including 3 740 up-regulated genes and 834 down-regulated genes. Among the up-regulated genes, 27 up-regulated genes were raleted to terpenoids, and 8 up-regulated genes were related to isoquinoline alkaloid bio-synthesis. Furthermore, it was also showed remarkable differences in groups which enrichment ratio of the diffe-rent expressed gene compared. The different expressed genes were annotated by the KEGG database into plant-pathogen interaction, plant hormone signal transduction and phenylpropanoid biosynthesis in fruit and leaf, but isoflavonoid bio-synthesis and betaine bio-synthesis were significantly different in fruit and leaf. The study laid a certain reference basis for comparison of quality and different expressed gene of Z. bungeanum from different groups.

Anti-oxidant and Anti-microbial Activities of Silver Nanoparticles of Essential Oil Extracts from Leaves of Zanthoxylum ovalifolium

Aim: The present study was aimed to synthesis and characterization of silver nanoparticles (AgNPs) using Zanthoxylum ovalifolium leaf essential oil extracts and to screen the anti-oxidant and antimicrobial potential of the same. Place and Duration of Study: The studies were carried out at Department of Botany, AVK College for Women, Hassan and Department of Biochemistry, Aurora’s Degree & PG College, Hyderabad from July 2017 to June 2018 Methodology: The essential oil from leaves of Zanthoxylum ovalifolium was obtained by hydrodistillation and analyzed by GC and GC-MS. Synthesis of silver nanoparticles of essential oil extract was carried out and characterized by using UV-VIS spectroscopy and transmission electron microscopy (TEM). The total phenolic and flavonoid contents were estimated in all the extracts. Furthermore, all the extracts were evaluated for anti-microbial activity against two gram-positive and two gram-negative bacteria and four pathogenic fungi using agar disc diffusion technique. Subsequently the minimum inhibitory concentration (MIC) was also determined. Results: The major compounds identified were Limonene, isofenchol, Geijerene, isothujanol, Borneol, dihydrocarveol, isobornyl acetate, pregeijerene, b-elemene, trans-caryophyllene and Germacrene D. The TEM analysis of nanoparticles synthesized showed a size of 8 to 14 nm with a lmax of 450nm. All the extracts were evaluated for in vitro anti-oxidant activity where the AgNP of essential oil extract showed maximum activity of 89.61% and 84.92% respectively for both DPPH free radical scavenging and Hydrogen peroxide free radical scavenging assays at a concentration of 100µg/ml. Among all the bacteria tested, B. subtilis was most susceptible at 100µg/ml with zone of inhibition of 22.5mm. While among all the fungi tested, A. niger inhibited more effectively by the AgNP of essential oil extract at 100µg/ml with a zone of inhibition of 16.2mm. Conclusion: The results obtained were remarkable suggesting that AgNP of essential oil extract possess excellent anti-oxidant and anti-microbial activity and can be an alternative bio-friendly source for various pharmaceutical industries.

Vasorelaxant activity and acute toxicity of the ethanolic extract of Zanthoxylum rhoifolium Lam leaves

The study evaluated the vasorelaxant effect induced by the ethanolic extract of the leaves of Zanthoxylum rhoifolium Lam (EEtOH-Zr/leaves). Wistar rats were treated with the leaf extract containing a single dose of 2,000 mg / kg, v.o. After 14 days, the animals were anesthetized for blood collection and subsequent analysis of the biochemical parameters; they were then euthanized (sodium pentobarbital-100 mg/kg, i.p.) for the removal and morphological analysis of the heart, lung, liver and kidney. The vasorelaxation activity the and vascular reactivity of EEtOH-Zr/leaves were evaluated on artery mesenteric rings isolated from rats. The extract showed no signs of toxicity and no significant difference in the values of the biochemical parameters between the control group and the group of treated animals. In the evaluation of pharmacological activity in the smooth muscle, the EEtOH-Zr/leaves caused vasorelaxant effect on the tonic contraction induced by phenylephrine in mesenteric artery preparations in the presence (pD2=2.17±0.05 µg/mL; Emax=99.8±5.2%) and absence (pD2=2.14±0.05 µg/mL; Emax=95.3±6.4%) of the vascular endothelium. Oral administration of EEtOH-Zr/leaves reduced the contraction induced by the cumulative addition of PHE. It is concluded that the EEtOH-Zr/leaves promote vasorelaxation and reduce vascular reactivity of adrenergic alpha-1 agonist in the mesenteric artery. The results did not show toxic effects of the extract.

Targets prediction and mechanism of Zanthoxylum nitidum in intervention of inflammation based on network pharmacology / 中草药

Objective: To construct the “active components-inflammatory target-anti-inflammatory pathway” network of Zanthoxylum nitidum intervened in inflammation, and predict the target of Z. nitidum intervened in inflammation and its anti-inflammatory mechanism. Methods: Using domestic and foreign literatures, TCMSP database, Pharmmapper server, oral availability (OB), and pharmacodynamics (DL) as the limiting conditions, the components of Z. nitidum were screened and the relative targets were predicted and collected. OMIM database was used to screen inflammation-related genes and protein targets; The STRING database was used to construct the interactive network between inflammatory targets; The network file of “active ingredient-predictive target-inflammatory target” was obtained by PPI analysis and imported into Cytoscape 3.5.1 software to construct the network of “active ingredient- inflammatory target”, so as to obtain the targets directly related to the anti-inflammatory effects of Z. nitidum. DAVID database was used to enrich the KEGG pathway of the selected targets, and then ClueGO plug-in was used to analyze the biological function of the target involved. Finally, the “active component-inflammatory target-anti-inflammatory pathway” network was constructed by combining the above relationships. Results: Twenty-three active ingredients were screened, and nine core anti-inflammatory targets were identified as COX-2, iNOS, PPARG, COX1, MAPK-14, JUN, NR3C1 and so on; The most critical pathways included TNF TRLs signaling pathways. Conclusion: It is preliminarily revealed that the anti-inflammatory effect of Z. nitidum is achieved through the interaction of multiple components and multiple targets, regulating the joint intervention of multiple pathways. However, the key targets and specific regulatory mechanisms need to be explored and verified by further experimental studies.

Studies on chemical constituents and bioactivities of alkaloids from zanthoxylum schinifolium / 中草药

Objective: To study the chemical structure and bioactivity of the alkaloids from Zanthoxylum schinifolium. Methods The alkaloids were isolated and purified by silica gel, Sephadex LH-20 column chromatography, recrystallization, and semi-preparetive HPLC. Their structures were elucidated by physical and spectroscopic analysis. The cytotoxic activity of these compounds were tested by MTS. Results Nine alkaloids were obtained and identified as dictamnine (1), skimmianine (2), schinifoline (3), 6-methoxy-furanoquinolone (4), (+)-(S)-isoplatydesmine (5), (+)-(S)-araliopsine (6), (−)-(S)-ribalinine (7), (−)-(S)-edulinine (8), and (−)-(S)-6-acetonyldihydrochelerythrine (9). Conclusion Compound 4 is a new natural product and compounds 5—9 are isolated from this plant for the first time. Compound 9 has potential cytotoxicity towards HL-60, SMMC-7721, and A549.

A new coumarin isolated from root barks of Zanthoxylum schinifolium / 中草药

Objective: To study the anti-inflammatory components from the root barks of Zanthoxylum schinifolium. Methods: The compounds were isolated and purified by silica gel, MCI, Sephadex LH-20 column chromatographies, and semi-preparative HPLC, and their structures were elucidated by physical and spectroscopic analysis. The anti-inf1ammatory activity was evaluated by the levels of NO in LPS-induced RAW264.7 tested by Griess reagent. Results: Four coumarins, namely zantholin A (1), 7-methoxycoumarin (2), isoscopoletin (3), and esculetin (4), were isolated from the root barks of Z. schinifolium. Compounds 1-4 exhibited anti-inflammatory activities on inhibition of lipopolysaccharide (LPS)-induced NO production in RAW 264.7 macrophages with IC50 values of (0.21 ± 0.03), (0.92 ± 0.16), (0.15 ± 0.02), and (0.26 ± 0.04) μmol/L, respectively. Conclusion: Compound 1 is a new compound, a rare terpenylated coumarin named zantholin A, and compounds 3 is obtained from this plant for the first time. All compounds exhibited anti-inflammatory activities.

Effect and mechanism of essential oil from Zanthoxylum bungeanum in microemulsion gel preparation on percutaneous delivery of complex components / 中国中药杂志

This study aimed to investigate the transdermal enhancing effect of essential oil from Zanthoxylum bungeanum(Z. bungeanum oil) in microemulsion gel(ZO-ME-gel) on permeation of different components,and reveal the transdermal enhancing mechanism of ZO-ME-gel. A series of components with different log P values were selected as model drugs and encapsulated in ZO-ME-gel to simplify and characterize the complex components of traditional Chinese medicine. The transdermal behavior of the model drugs was further examined using the improved Franz diffusion cell method. Then attenuated total reflection Fourier transform infrared spectroscopy(ATR-FTIR),differential scanning calorimetry(DSC) studies and hematoxylin-eosin(HE) staining were used to investigate the effects of Z. bungeanum oil and ZO-ME-gel on keratin,intercellular lipids and microstructure of the stratum corneum(SC). The results showed that Z. bungeanum oil and ZO-ME-gel had a good transdermal enhancing effect on both hydrophilic and lipophilic drugs,and the best effect was achieved when log P value was-0. 5. The transdermal enhancing mechanism of Z. bungeanum oil and ZO-ME-gel was related to affecting the order of the SC lipids,changing lipid fluidity and protein conformation,and disrupting the integrity of the SC structure. 5% Z. bungeanum oil had greater transdermal enhancing effect and destruction of SC structure than ZO-ME-gel. These results suggested that Z. bungeanum oil loaded in microemulsion gel still had a good transdermal enhancing effect although the effect was not as great as Z. bungeanum oil itself,in addition,ZO-ME-gel was less irritating to the skin and safer to use,which had a guiding role in the development and clinical application of Z. bungeanum oil-containing traditional Chinese medicine topical preparations.

Chemical Constituents from Stems of Zanthoxylum bungeanum / 中国实验方剂学杂志

Objective:To isolate and identify the chemical constituents from 95%ethanol extracts from stems of Zanthoxylum bungeanum. Method:The stems (25 kg) were extracted with 95%ethanol under reflux for three times and then filtrated,and the combined filtrates were concentrated under vacuum to get the extracts. After suspension with water,the extracts were extracted with petroleum ether,dichloromethane,ethyl acetate and n-butanol successively,and five corresponding parts were obtained. The parts of petroleum ether,dichloromethane,ethyl acetate were separated in a similar way to get pure compounds. By the method the subjects were first chromatographed on silica gel column respectively,then the selected sub-fractions were further separated by Sephadex LH-20, and finally purified on preparation HPLC to get the monomer compound. The n-butanol part was first treated with macroporous resin D101,and then the sub-fractions were further purified by almost the same method as mentioned above. The structures of these compounds were determined by spectrum technology as IR,MS,1H-NMR,13 C-NMR. Result:Ten compounds were isolated from Z. bungeanum stems and identified as follows:(+)-magnoflorine(1),(-)-marmesin(2),(-)-columbianetin(3),(-)-decursinol(4),lupeol(5),α-amyrin(6),β-amyrin(7),δ-amyrin(8),quercetin(9),rutin(10). Among them, 1 was alkaloid, 2,3,4 were coumarin, 5,6,7,8 were triterpenoid, 9,10 were flavonoids. Conclusion:Compounds 1-8 were isolated from this plant for the first time.