Exploring the potential of omics technologies in medicinal plant research: a review in Colombia / Explorando el potencial de las tecnologías ómicas en la investigación de plantas medicinales: una revisión en Colombia

This review presents advances in the implementation of high - throughput se quencing and its application to the knowledge of medicinal plants. We conducted a bibliographic search of papers published in PubMed, Science Direct, Google Scholar, Scopus, and Web of Science databases and analyzed the obtained data using VOSviewer (versi on 1.6.19). Given that medicinal plants are a source of specialized metabolites with immense therapeutic values and important pharmacological properties, plant researchers around the world have turned their attention toward them and have begun to examine t hem widely. Recent advances in sequencing technologies have reduced cost and time demands and accelerated medicinal plant research. Such research leverages full genome sequencing, as well as RNA (ribonucleic acid) sequencing and the analysis of the transcr iptome, to identify molecular markers of species and functional genes that control key biological traits, as well as to understand the biosynthetic pathways of bioactive metabolites and regulatory mechanisms of environmental responses. As such, the omics ( e.g., transcriptomics, metabolomics, proteomics, and genomics, among others) have been widely applied within the study of medicinal plants, although their usage in Colombia is still few and, in some areas, scarce. (185)

El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria se evaluaron para determinar su actividad antiproliferativa in vitro contra 10 líneas ce lulares tumorales humanas [leucemia (K - 562), mama (MCF - 7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR - RES), melanoma (UACC - 62), pulmón (NCI - H460), próstata (PC - 3), colon (HT29), ovario (OVCAR - 3), glioma (U251) y riñón (786 - 0)]. CE presentó actividad antiproliferativa débil a moderada (log GI 50 medio 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent - pimara - 8 (14), ácido 15 - dien - 19 - oico y ent - 8(14),15 - pimaradien - 3 ß - ol], presentaron activid ad moderada a potente para la mayoría de las líneas celulares, con un log GI 50 medio de 0.62 y 0.59, respectivamente. Los resultados mostraron una acción antiproliferativa in vitro prometedora de las muestras obtenidas de A. arenaria , con los mejores resul tados para NCI/ADR - RES, HT29 y OVCAR - 3, y valores de TGI que van desde 5.95 a 28.71 µg.mL - 1, demostrando que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos

Adaptation and validation of the Bengali version of the Chronic Urticaria Quality of Life Questionnaire (CU-Q2oL)

Background: Chronic urticaria exerts a profound impact on quality of life. Recent guidelines recommend its evaluation in all chronic urticaria patients. Currently, the Chronic Urticaria Quality of Life Questionnaire (CU-Q2oL) is the only validated tool to assess chronic urticaria-specific quality of life. Objective: To validate and adapt the CU-Q2oL to the Bengali language for its widespread use. Methods: The CU-Q2oL questionnaire was translated into Bengali. Its internal consistency and reliability were tested by asking 42 chronic urticaria patients to complete this version. They completed the validated Bengali Dermatology Life Quality Index and Urticaria Control test questionnaires, and their scores were correlated with CU-Q2oL score to assess the validity of our Bengali version. Results: The mean CU-Q2oL score of our patients (mean age 38.41 ± 13.4 years, male: female 29:13) was 48.8 ± 16.5. Domain 4 (sleep problems) was worst affected, followed by domain 1 (pruritus), while domain 2 (swelling) was least affected. We detected an excellent overall internal consistency (Cronbach’s alpha = 0.93) of our version and nearly complete agreement (intra-class correlation coefficient = 0.91) between the test-retest scores. We found a significant positive correlation between the overall CU-Q2oL and Dermatology Life Quality Index scores (rs = 0.53, P = 0.0002), thus implying the validity of our version. Additionally, we noted a significant negative correlation between the overall CU-Q2oL and Urticaria Control test scores (rs = -0.48, P = 0.0007), suggestive of a more severe impairment of quality of life with poorer disease control. Limitations: Small sample size, observational design and bias in test-retest reliability analysis due to the use of rescue therapy in-between assessment sessions were important limitations of our study. Conclusion: The Bengali version of CU-Q2oL questio

Terpine-4-ol on inhibiting vascular smooth muscle cell calcification by improving mitochondrial dynamics / 药学学报

The aim of this study was to investigate the role and mechanism of terpinen-4-ol (T4O) on high glucose (HG) -induced calcification in vascular smooth muscle cell (VSMC). To investigate the role of T4O on HG-induced calcium deposition, osteogenic phenotypic transformation and mitochondrial dynamics in VSMC, Mdivi-1, a mitochondrial dynamin-related protein 1 (Drp-1) inhibitor, was used to analyze the correlation between mitochondrial dynamics and VSMC calcification and the role of T4O. Alizarin red S staining was used to observe calcium salt deposition and flow cytometry to detect intracellular Ca2+ content; Western blot and immunofluorescence were used to detect the expression of phenotypic switching-related markers α-smooth muscle actin (α-SMA), bone morphogenetic protein 2 (BMP2) and Runt related transcription factor 2 (Runx2), and mitochondrial dynamics-related markers mitofusin 1 (MFN1), mitofusin 2 (MFN2) and Drp-1. The results showed that low and high doses of T4O could inhibit HG-induced down-regulation of α-SMA, MFN1 and MFN2 expression levels, and up-regulation of BMP2, Runx2 and Drp-1 expression levels, reduce intracellular Ca2+ content and calcium salt deposition, and effectively inhibit HG-induced VSMC calcification and mitochondrial dynamics disorders. The T4O group, Mdivi-1 group and T4O+Mdivi-1 group were able to up-regulate the expression levels of HG-induced α-SMA, MFN1 and MFN2, down-regulate the protein expression levels of BMP2, Runx2 and Drp-1, and inhibit calcium salt deposition, and there was no significant difference between the above indexes in the T4O and T4O+Mdivi-1 groups. The above findings suggest that T4O can inhibit the expression level of Drp-1, regulate the disturbance of mitochondrial dynamics, and suppress HG-induced VSMC calcification.

The protective effect of terpinen-4-ol on inflammatory injury of VSMCs induced by high glucose through improving autophagic flux disorder / 中国药理学通报

Aim To investigate the effect of terpinen-4-ol (T40) on inflammatory injury of vascular smooth muscle cells (VSMCs) induced by high glucose based on the improvement of autophagic flow disorder and involved molecular signals. Methods The scratch test was used to analyze the migration ability of VSMCs, the levels of IL-1β and IL-6 in cell culture supernatant were measured by ELISA, the expression levels of inflammation-related proteins NF-κb p65, p-NF-κb p65, IL-1β, IL-18 and autophagy-related proteins p62, LC3-HYLC3-I, Beclinl, p-Beclinl were de-tected by Western blot. Results T40 inhibited migration of VSMCs induced by high glucose, reduced the secretion and release of pro-inflammatory factors IL-1β and IL-6, inhibited the expression of p-NF-κb p65/ NF-κb p65, IL-1β, IL-18, downregulated the expression of p62, LC3-TJ/LC3- I and p-Beclinl at same time. After interfering the autophagic flux of VSMCs with autophagy inhibitor chloroquine (CQ) , T40 pre-treatment significantly inhibited the protein expression levels of the above inflammatory factors and autophagy-related signals which mediated by CQ. Conclusion T40 inhibits the inflammatory injury of VSMCs induced by high glucose through improving the autophagic flow disorder.

Progress on Pharmacological Effect of Terpinen-4-ol： A Review / 中国实验方剂学杂志

Terpine-4-ol is abundant in nature. As a cyclic monoterpenoid compound， terpine-4-ol is distributed in a variety of natural plants. It is the main component and the key active substance in many traditional Chinese essential oils， such as Melaleuca alba essential oil and coral ginger essential oil. Terpine-4-ol has anti-microbial， anti-tumor， insecticidal， anti-inflammatory， and other effects. It can treat cancer， as well as oral and cardiovascular diseases with great safety. In terms of antibacterial activity， terpine-4-ol can destroy bacterial cell walls， improve membrane permeability， and regulate bacterial migration， reproduction， and other related genes to inhibit bacterial activity. In terms of antifungal activity， terpine-4-ol can bind with ergosterol in fungal cell walls to cause fungal death. In terms of insecticidal activity， terpine-4-ol can inhibit Na+ and K+-ATPase activity and cause the death of the insect. In terms of anticancer activity， terpine-4-ol can regulate the expression of apoptosis-related proteins in cancer cells， so as to control the apoptosis of cancer cells. In this paper， the pharmacological activity and action mechanism of terpine-4-ol were reviewed to provide a reference for further research and utilization of terpine-4-ol.

Terpinen-4-ol inhibits proliferation of VSMCs exposed to high glucose via regulating KLF4/NF-κB signaling pathway / 中国中药杂志

This study aimed to observe the effect of terpinen-4-ol(T4O) on the proliferation of vascular smooth muscle cells(VSMCs) exposed to high glucose(HG) and reveal the mechanism via the Krüppel-like factor 4(KLF4)/nuclear factor kappaB(NF-κB) signaling pathway. The VSMCs were first incubated with T4O for 2 h and then cultured with HG for 48 h to establish the model of inflammatory injury. The proliferation, cell cycle, and migration rate of VSMCs were examined by MTT method, flow cytometry, and wound healing assay, respectively. The content of inflammatory cytokines including interleukin(IL)-6 and tumor necrosis factor-alpha(TNF-α) in the supernatant of VSMCs was measured by enzyme-linked immunosorbent assay(ELISA). Western blot was employed to determine the protein levels of proliferating cell nuclear antigen(PCNA), Cyclin D1, KLF4, NF-κB p-p65/NF-κB p65, IL-1β, and IL-18. The KLF4 expression in VSMCs was silenced by the siRNA technology, and then the effects of T4O on the cell cycle and protein expression of the HG-induced VSMCs were observed. The results showed that different doses of T4O inhibited the HG-induced proliferation and migration of VSMCs, increased the percentage of cells in G_1 phase, and decreased the percentage of cells in S phase, and down-regulated the protein levels of PCNA and Cyclin D1. In addition, T4O reduced the HG-induced secretion and release of the inflammatory cytokines IL-6 and TNF-α and down-regulated the expression of KLF4, NF-κB p-p65/NF-κB p65, IL-1β, and IL-18. Compared with si-NC+HG, siKLF4+HG increased the percentage of cells in G_1 phase, decreased the percentage of cells in S phase, down-regulated the expression of PCNA, Cyclin D1, and KLF4, and inhibited the activation of NF-κB signaling pathway. Notably, the combination of silencing KLF4 with T4O treatment further promoted the changes in the above indicators. The results indicate that T4O may inhibit the HG-induced proliferation and migration of VSMCs by down-regulating the level of KLF4 and inhibiting the activation of NF-κB signaling pathway.

Tea tree oil, a vibrant source of neuroprotection via neuroinflammation inhibition: a critical insight into repurposing Melaleuca alternifolia by unfolding its characteristics / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Over the past few decades, complementary and alternative treatments have become increasingly popular worldwide. The purported therapeutic characteristics of natural products have come under increased scrutiny both in vitro and in vivo as part of efforts to legitimize their usage. One such product is tea tree oil (TTO), a volatile essential oil primarily obtained from the native Australian plant, Melaleuca alternifolia, which has diverse traditional and industrial applications such as topical preparations for the treatment of skin infections. Its anti-inflammatory-linked immunomodulatory actions have also been reported. This systematic review focuses on the anti-inflammatory effects of TTO and its main components that have shown strong immunomodulatory potential. An extensive literature search was performed electronically for data curation on worldwide accepted scientific databases, such as Web of Science, Google Scholar, PubMed, ScienceDirect, Scopus, and esteemed publishers such as Elsevier, Springer, Frontiers, and Taylor & Francis. Considering that the majority of pharmacological studies were conducted on crude oils only, the extracted data were critically analyzed to gain further insight into the prospects of TTO being used as a neuroprotective agent by drug formulation or dietary supplement. In addition, the active constituents contributing to the activity of TTO have not been well justified, and the core mechanisms need to be unveiled especially for anti-inflammatory and immunomodulatory effects leading to neuroprotection. Therefore, this review attempts to correlate the anti-inflammatory and immunomodulatory activity of TTO with its neuroprotective mechanisms.

Plantas medicinales utilizadas en la región de Teziutlán, Puebla, México / Medicinal plants used in the region of Teziutlán, Puebla, México

The objective of this work was to collect information on the curative use of plants in the municipality of Teziutlán, Puebla through semi-structured interviews. Thus, 78 plants used for medicinal purposes were identified, of which 40 are native to Mexico and 38 introduced; The value of use (UV) of each one and the Informant's Consensus Factor (FCI) of 10 categories of diseases were calculated. The five most frequently used plants are Ruta chalepensis L., Rosmarinus officinalis, Arnica montana, Loeselia mexicana (Lam.) Brandegee and Sambucus cerulea var., Neomexicana, which underwent a chemical and pharmacological review. On the other hand, the most frequent preparations are infusion and decoction, using mainly leaves (49.34%) and flowers (19.51%). It is concluded that the inhabitants of Teziutlán have a fairly homogeneous ethnomedical knowledge, setting the standard for research on its pharmacological properties.

El objetivo del presente trabajo fue recopilar información sobre el uso curativo de las plantas del municipio de Teziutlán, Puebla por medio de entrevistas semiestructuradas. Así, se identificaron 78 plantas utilizadas con fines medicinales, de las cuales 40 son propias de México y 38 introducidas; se calculó el valor de uso (UV) de cada una y el Factor de Consenso del Informante (FCI) de 10 categorías de padecimientos. Las cinco plantas utilizadas con mayor frecuencia son Ruta chalepensis L., Rosmarinus officinalis, Arnica montana, Loeselia mexicana (Lam.) Brandegee y Sambucus cerulea var., neomexicana, a las que se les hizo una revisión química y farmacológica. Por otro lado, las preparaciones más frecuentes son infusión y decocción, utilizando principalmente hojas (49.34 %) y flores (19.51 %). Se concluye que los habitantes de Teziutlán cuentan con un conocimiento etnomédico bastante homogéneo, dando la pauta para investigaciones sobre sus propiedades farmacológicas.

Chemical compositions, larvicidal and antimicrobial activities of Zingiber castaneum (Škorničk. & Q.B. Nguyễn) and Zingiber nitens (M.F. Newman) essential oils

Abstract In this paper, the chemical constituents, larvicidal and antimicrobial activities of hydrodistilled essential oils from Zingiber castaneum Škorničk. & Q.B. Nguyễn and Zingiber nitens M.F. Newman were reported. The main constituents of Z. castaneum leaf were bicyclogermacrene (24.8%), germacrene D (12.9%), cis-β-elemene (11.2%) and β-pinene (10.3%), while sabinene (22.9%) and camphene (21.2%) were the significant compounds in the rhizome. However, the dominant compounds in the leaf of Z. nitens includes β-pinene (45.8%) and α-pinene (10.7%). Terpinen-4-ol (77.9%) was the most abundant compound of the rhizome. Z. castaneum rhizome oil displayed larvicidal activity against Aedes aegypti and Culex quinquefasciatus with LC50 values of 121.43 and 88.86 µg/mL, respectively, at 24 h. The leaf oil exhibited activity with LC50 values of 39.30 µg/mL and 84.97 µg/mL, respectively. Also, the leaf and rhizome oils of Z. nitens displayed greater larvicidal action towards Ae. aegypti with LC50 values of 17.58 µg/mL and 29.60 µg/mL, respectively. Only the rhizome oil displayed toxicity against Cx. quinquefasciatus with LC50 value of 64.18 µg/mL. All the studied essential oils inhibited the growth of Pseudomonas aeruginosa ATCC25923 with minimum inhibitory concentration (MIC) value of 50.0 µg/mL. This paper provides information on the larvicidal and antimicrobial potentials of Z. castaneum and Z. nitens essential oils.

Processing evolution and modern research progress of Euryale ferox / 中国药房

Euryale f erox is the dry and mature seed kernel of Euryale ferox Salisb.，the effect of raw E. ferox is mainly to astringe spontaneous emission or leukorrhea ，while the effect of fried E. ferox is mainly to tonify the spleen and stomach. Therefore ， processing has an important impact on the effect of E. ferox . The author summarizes the processing evolution ，chemical composition ， pharmacological action and quality control of E. ferox by consulting past materia medica monographs and related research papers. The results show that the processing methods of E. ferox in the past include cleansing ，medicinal juice ，frying and steaming ；modern processing methods mainly continue to use cleansing and frying ，among which frying can be divided into stir-frying and bran-frying. E. ferox mainly contains polyphenols ，flavonoids，sterols and other components ，with antioxidant ，antibacterial，hypoglycemic and other pharmacological effects. At present ，scholars have established a variety of fingerprints to control the quality of E. ferox . Naringin，total amino acids and other components may be the differential components that affect the quality of E. ferox ，while the contents of heavy metals and sulfur dioxide are important indicators that affect the safety of E. ferox ，and α-tocopherol and gallic acid may be the quality markers of E. ferox . Later ，according to the basic properties of raw and processed products of E. ferox ， pharmaceutical analysis methods can be used to comprehensively investigate the differences and change rules of chemical components in E. ferox before and after processing. The pharmacodynamic effects of E. ferox before and after processing can be evaluated by in vivo and in vitro models，so as to provide references for the inheritance of processing technology ，the formulation of processing standards and clinical application of E. ferox .

Terpinen-4-ol inhibits proliferation, migration and invasion and promotes apoptosis of glioma U87 and U251 cells / 中国药理学通报

Aim To investigate the effect of T40 on malignant biological behavior of glioma U87 and U251 cells and its mechanism. Methods U87 and U251 cells were treated with T40 at different concentrations (0,1,2 and 4 p,mol • L"1). Changes of cell proliferation, clonal formation, apoptosis, migration and invasion in each group were detected by CCK-8, cloning plate, flow cytometry, scratch and transwell experi-ments. Bioinformatics was used to explore T40 targets and analyze the relationship between targets and glioma progression. The protein expression levels of PTPN1, PTPN2, Bcl-2, Bax, pro-caspase-3 , cleaved caspase- 3, MMP-2 and MMP-9 in each group were detected by Western blot. Results T40 significantly inhibited U87 and U251 proliferation, clone formation, migration and invasion and promoted apoptosis ( P < 0. 05 ) ; T40 had 37 targets, among which the expression levels of PTPN1 and PTPN2 were negatively correlated with the overall survival rate of glioma patients; T40 signifi cantly reduced the expression of PTPN1, PTPN2, Bcl- 2, MMP-2 and MMP-9 in U87 and U251 cells, and increased the expression of Bax and cleaved caspase-3 (P < 0. 05). Conclusions T40 inhibits the proliferation , migration and invasion of glioma U87 and U251 cells and promotes their apoptosis, and its mechanism may be related to the reduction of PTPN1 and PTPN2 expression.

Construction of yeast cell factories for production of azadirachtin precursor tirucalla-7,24-dien-3β-ol / 中国中药杂志

Azadirachtin, as a botanical insecticide, is a highly oxidized limonoid triterpenoid existing in the seeds of Azadirachta indica. However, due to the low content in the seeds, the production of azadirachtin by seed extraction has low yield. Chemical synthesis of azadirachtin is characterized by complex process and low yield. Synthetic biology provides an alternative for the supply of azadirach-tin. In this study, two oxidosqualene cyclases AiOSC1 and MaOSC1 respectively derived from A. indica and Melia azedarach were identified in yeast. A yeast strain producing tirucalla-7,24-dien-3β-ol was constructed by integration of AiOSC1, Arabidopsis thaliana-derived squalene synthase gene(AtAQS2), and Saccharomyces cerevisiae-derived truncated 3-hydroxy-3-methyl-glutaryl coenzyme A reductase gene(PgtHMGR) into the delta site of yeast. Then, the function of MaCYP71BQ5 was successfully verified in yeast after this gene was introduced into the constructed yeast strain. This study not only laid a foundation for the biosynthesis of tirucalla-7,24-dien-3β-ol, but also provided a chassis cell for the functional identification of cytochrome oxidases(CYP450 s) in azadirachtin biosynthesis pathway.

Ethnobotany of Plectranthus neochilus Schltr (Meprobamate) in Cuba / Estudio etnobotánico de Plectranthus neochilus Schltr (Meprobamato) en Cuba

Chloroform extract (CE) and fractions obtained from Aldama arenaria roots were evaluated for their in vitro antiproliferative activity against 10 human tumor cell lines [leukemia (K-562), breast (MCF-7), ovary expressing a multidrug-resistant phenotype (NCI/ADR-RES), melanoma (UACC-62), lung (NCI-H460), prostate (PC-3), colon (HT29), ovary (OVCAR-3), glioma (U251), and kidney (786-0)]. CE presented weak to moderate antiproliferative activity (mean log GI50 1.07), whereas fractions 3 and 4, enriched with pimaranetype diterpenes [ent-pimara-8(14),15-dien-19-oic acid and ent-8(14),15-pimaradien-3ß-ol], presented moderate to potent activity for most cell lines, with mean log GI50 of 0.62 and 0.59, respectively. The results showed promising in vitro antiproliferative action of the samples obtained from A. arenaria, with the best results for NCI/ADR-RES, HT29, and OVCAR-3, and TGI values ranging from 5.95 to 28.71 µg.ml -1, demonstrating that compounds of this class may be potential prototypes for the discovery of new therapeutic agents.

El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria fueron evaluadas por su actividad antiproliferativa in vitro contra 10 líneas celulares tumorales humanas [leucemia (K-562), mama (MCF-7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR-RES), melanoma (UACC-62), pulmón (NCI-H460), próstata (PC-3), colon (HT29), ovario (OVCAR-3), glioma (U251) y riñón (786-0)]. CE presentó actividad antiproliferativa débil a moderada (log GI50 promedio de 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent-pimara-8 (14), ácido 15-dien-19-oico y ent-8 (14), 15-pimaradien-3ß-ol], presentaron actividad moderada a potente para la mayoría de las líneas celulares, con un log GI50 promedio de 0.62 y 0.59, respectivamente. Los resultados mostraron una prometedora acción antiproliferativa in vitro de las muestras obtenidas de A. arenaria, con los mejores resultados para NCI/ADR-RES, HT29 y OVCAR-3, y valores de TGI que van desde 5.95 a 28.71 µg.ml -1, lo que demuestra que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos.

Lead Molecule Identification From Vitex Trifolia Linn For Helminthiasis Using In Vitro And In Silico Methods

Objective: The study was an attempt to discover a lead molecule to treat helminthiasis using Vitex trifolia. Linn (V. folia Linn) through sterile effect, in vitro and in silico evaluation. Methods: The antibacterial activity was done by Kirby-Bauer disc diffusion method in three different concentrations of extract and in vitro anthelmintic activity was carried out by petri dish and organ bath method. Further, the in silico docking studies were carried out by 11 phytoconstituents against phosphoethanolamine methyltransferase (4FGZ) using Auto Dock 4.2, it was working based on the principle of Lamarckian genetic algorithm. In docking studies, three important parameters such as binding energy, inhibition constant and intermolecular energy are determined. Results: The extracts showed an antibacterial effect in three different concentrations. At 16 mcg/disc a significant effect was observed when compared to blank and ciprofloxacin 5 mcg/disc. The anthelmintic activity in the petri dish method, means paralyzing time of Pheretimaposthuma with the dose of 25, 50 and 100 mg/ml were 13.78, 5.79 and 4.57 min respectively and Piperazine citrate (10 mg/ml) showed paralysis in 21.58 min. In the organ bath method, the time for paralysis of the worm was recorded on a slow-moving Sherrington rotating drum and the study report showed that paralyzing time was decreased at increasing concentrations of the extract. The results of in silico studies exhibited a binding energy of-10.25kcal/mol, inhibitory constant (Ki) 30.91nM, intermolecular energy,-10.84kcal/mol for abietatriene-3-ol which is lesser than the standard ligand phosphoethanolamine (-6.03kcal/mol, 38.29µM,-7.82kcal/mol) respectively. Conclusion: The study reports conclude that the active constituents in V. folia Linn having better anthelmintic activity, thus the active constituents may be optimized and make way to a new moiety for the treatment of helminthiasis.

Study on chemical constituents of Gendarussa vulgaris / 中草药

Objective: To study the chemical constituents of aerial part of Gendarussa vulgaris. Methods: The compounds were separated and purified by silica gel column chromatography, ODS and Sephadex LH-20 chromatography and semi-preparative HPLC. Base on HR-ESI-MS, NMR, and other spectral data, their structures were identified. Results: A total of 17 compounds were isolated from the EtOAc fraction of 95% ethanol extract and identified as 24-norchol-5-en-3β-ol (1), dihydrobetulic acid (2), betulinic acid (3), 3-hydroxy-30-nor-20-oxo-28-lupanoic acid (4), 6-hydroxy-7,8-dimethoxycoumarin (5), 6,7-dimethoxycoumarin (6), 5,6,7- trimethoxycoumarin (7), 6,7,8-trimethoxycoumarin (8), syringaresinol-4-O-β-D-glucopyranoside (9), 4-O-caffeoylquinic acid methyl ester (10), N-trans-feruloyl tyramine (11), N-(2-hydroxy-3-phenylpropyl) acetamide (12), 3-O-caffeoylquinic acid methyl ester (13), 3,5-O-dicaffeoylquinic acid methyl ester (14), p-E-coumarin quinic acid methyl ester (15), 3,4,5-O-tricaffeoyl quinic acid methyl ester (16) and 1'S*,4'R*-8-(4'-hydroxy-2',6',6'-trimethylcyclohex-2-enyl)-6-methyloct-3E,5E,7E-trien-2-one (17). Conclusion: Compounds 1 and 2 are new natural products. All Compounds are isolated from this plant for the first time except compound 6. Besides, all compounds are screened for anti-inflammatory activity and compounds 2, 3, 11, 13, and 17 have NO release inhibiting activities on LPS-induced RAW 264.7 macrophage cells with IC50 values of (30.91 ± 0.50), (44.66 ± 0.56), (17.67 ± 0.57), (28.45 ± 0.67) and (20.79 ± 0.24) μmol/L, respectively.

Chemical constituents from stems and leaves of Aphanamixis sinensis and their antibacterial activities / 中草药

Objective: To study the chemical constituents of stems and leaves from Aphanamixis sinensis and evaluate their antibacterial activities. Methods: The compounds were isolated and purified by various column chromatography techniques, such as silica gel, ODS, Sephadex LH-20, and MCI, and their structures were identified by physiochemical properties and spectroscopic data. Moreover, antimicrobial activities against Staphylococcus aureus ATCC 25923, Escherichia coli CICC 10003, and Salmonella enterica UK-1 8956 of compounds 1-13 were evaluated by filter paper method. Results: Fifteen compounds were isolated from A. polystachya which were elucidated as (23E)-25-methoxycycloart-23-en-3β-ol (1), 25-hydroxy-cycloart-23-en-3-one (2), 23 (Z)-9,19-cycloart-23-ene-3β,25-diol (3), 23 (E)-cycloart-23-en-3β,25-diol (4), ent-labd-8 (17), 13E-dien-15-ol (5), vulgaro (6), ambroxdiok (7), α-cadinol (8), 1 (10)-en-oxo-7α-isopropanoleremophilane (9), (5R,7R,10S)-isopterocarpolone (10), 1S,4S,5S,10R- 4,10-guaianediol (11), (4R,5R,7S,9S,10S)-(-)-eudesma-11 (13)-en-4,9-diol (12), phytol (13), ergosterol endoperoxide (14) and 7α-hydroxysitosterol (15). Conclusion: All isolates were obtained from this plant for the first time, and compounds 2, 5, 7-10, and 12-15 were isolated from the genus Aphanamixis for the first time. Compound 5 showed obvious activity against S. aureus ATCC 25923 with the MIC value of 5 μg/mL.

Chemical constituents from ethyl acetate extracts of Pholidota articulata / 中草药

Objective: To study the chemical constituents of ethyl acetate extract from the whole herb of Pholidota articulata. Methods: Silica gel and Sephadex LH-20 gel column chromatographic techniques were used to separate and purify the chemical constituents. Their structures were elucidated based on NMR spectroscopic and reported data. Results: A total of 17 compounds were isolated from 78% ethyl acetate extracts of P. articulata and identified as flavidin (1), flaccidin (2), imbricatin (3), coelonin (4), lusianthridin (5), hircinol (6), gigantol (7), batatasin III (8), 5,3'-dihydroxy-3-methoxybibenzyl (9), cirrhopetalidin (10), β-sitosterol (11), stigmasterol (12), glut-5-en-3-ol (13), laurostearic acid (14), 4, 4'-dihydroxydiphenylmethane (15), 3-methoxy-benzaldehyde (16), and trans-cinnamic acid (17). Conclusion: Compounds 3-17 are isolated from this plant for the first time. In addition, compounds 9, 10, 13, and 16 are found in the genus Pholidota for the first time.

Chemical constituents from pericarpium of Metaplexis japonica / 中草药

Objective: To study the chemical constituents from the pericarpium of Metaplexis japonica. Methods: The petroleum ether, dichloromethane and ethyl acetate fractions of 95% ethanol extract from M. japonica were isolated and purified by silica gel, Sephadex LH-20, MPLC and preparative HPLC, etc. The structures of the obtained compounds were identified by physicochemical properties and spectral data. Results: Ten compounds were isolated and identified as (15β,21α)-dihydroxypregna-17,20-trimethylene oxide-4,6-dien-3-one (1), 25-hydroperoxycyc-loart-23-en-3β-ol (2), α-amyrin (3), scoparone (4), aleuritin (5), syringaresinol (6), pergularin-3-O-β-D-oleanodropyranose (7), (20β)-21-dihydroxypregna-4,6-dien-3-one (8), blumenol A (9) and 4-pregnen-20,21- diol-3-one (10). Conclusion: Compound 1 is a new C21 steroidal compound named metajapogenin F, compounds 2 and 10 are isolated from the genus Metaplexis for the first time, and compound 8 is isolated from this plant for the first time.

Interactions between Terpinen-4-ol and Nystatin on biofilm of Candida albicans and Candida tropicalis

Abstract The aim of this study was to evaluate the antifungal activity of Terpinen-4-ol associated with nystatin, on single and mixed species biofilms formed by Candida albicans and Candida tropicalis, as well as the effect of terpinen-4-ol on adhesion in oral cells and the enzymatic activity. The minimum inhibitory concentrations and minimum fungicide concentrations of terpinen-4-ol and nystatin on Candida albicans and Candida tropicalis were determined using the microdilution broth method, along with their synergistic activity ("checkerboard" method). Single and mixed species biofilms were prepared using the static microtiter plate model and quantified by colony forming units (CFU/mL). The effect of Terpinen-4-ol in adhesion of Candida albicans and Candida tropicalis in coculture with oral keratinocytes (NOK Si) was evaluated, as well as the enzymatic activity by measuring the size of the precipitation zone, after the growth agar to phospholipase, protease and hemolysin. Terpinen-4-ol (4.53 mg mL-1) and nystatin (0.008 mg mL-1) were able to inhibit biofilms growth, and a synergistic antifungal effect was showed with the drug association, reducing the inhibitory concentration of nystatin up to 8 times in single biofilm of Candida albicans, and 2 times in mixed species biofilm. A small decrease in the adhesion of Candida tropicalis in NOK Si cells was showed after treatment with terpinen-4-ol, and nystatin had a greater effect for both species. For enzymatic activity, the drugs showed no action. The effect potentiated by the combination of terpinen-4-ol and nystatin and the reduction of adhesion provide evidence of its potential as an anti-fungal agent.

Resumo O objetivo desse estudo foi avaliar a atividade antifúngica do Terpinen4-ol associado à nistatina em biofilmes simples e misto, formados por Candida albicans e Candida tropicalis, bem como o efeito do terpinen-4-ol na adesão em células orais e atividade enzimática. As concentrações inibitórias mínimas e as concentrações fungicidas mínimas do terpinen-4-ol e da nistatina em Candida albicans e Candida tropicalis foram determinadas pelo método de microdiluição em caldo, juntamente com a atividade sinérgica (método do tabuleiro de "xadrez"). Biofilmes simples e misto foram preparados usando o modelo de placa de microtitulação estática e quantificados por unidades formadoras de colônias (CFU/mL). O efeito do Terpinen-4-ol na adesão de Candida albicans e Candida tropicalis em co-cultura com queratinócitos orais (NOK Si) foi avaliado, bem como a atividade enzimática, medindo o tamanho da zona de precipitação, após o crescimento em ágar fosfolipase, protease e hemolisina. O terpinen-4-ol (4.53 mg mL-1) e a nistatina (0,008 mg mL-1) conseguiram inibir o crescimento de biofilmes e um efeito antifúngico sinérgico foi demonstrado com a associação de fármaco, reduzindo a concentração inibidora de nistatina até 8 vezes em biofilme simpes de Candida albicans e 2 vezes em biofilme misto. Uma pequena diminuição na adesão de Candida tropicalis em células NOK Si foi mostrada após o tratamento com terpinen-4-ol e a nistatina teve um efeito maior para ambas as espécies. Para a atividade enzimática, as drogas não apresentaram ação. O efeito potencializado pela combinação de terpinen-4-ol e nistatina e a redução de adesão evidenciam seu potencial como agente anti-fúngico.

Identification and evaluation of (3Z, 6Z, 8E)-dodeca-3, 6, 8-trien-1-ol as the trail following pheromone on Microcerotermes exiguous (Isoptera:Termitidae) / Identificación y evaluación de (3Z, 6Z ,8E)-dodeca-3, 6, 8-trien-1-ol como feromona de camino de Microcerotermes exiguus (Isoptera:Termitidae)

Abstract Trail-following pheromone is one of the most important semiochemical in termites. This pheromone is responsible for the recruitment of individuals from the colony to perform different tasks. The aim of this work was to isolate and identify the trail-following pheromone of Microcerotermes exiguus (Isoptera: Termitidae), a typical termite from the Neotropic, that is considered pest in some crops. Subterranean nest of M. exiguus were collected with a shovel in Caracas, Venezuela in 2010. Different chemical micro-reactions combined with chromatographic analysis of solvent extracts, as well as solid phase microextraction analyses (SPME) were applied to termite sternal glands; besides, some behavioral biossays were undertaken. A peak in the chromatograms from extracts (retention index: 1 483), presented a fragmentation pattern with m/z ions: 41; 55; 67; 79; 91; 105; 119; 135; 142; 180, this result alongside behavioral assays allowed us to conclude that (3Z,6Z,8E)-dodeca-3, 6, 8-trien-1-ol (DTOH) acts as the main component of the trail following pheromone. The estimated optimum concentration for termite recruitment and orientation was around 1 pg/cm, being statistically comparable to the value on trails marked with whole body extracts at concentration of 1 worker/cm. The period of time that this compound takes to recruit other colony members is 13.67 ± 5.76 s and lasts up to two hours. Both analytical and behavioral results provided better understanding on the chemical communication of M. exiguus. This information could be used for the future development of newer pest control methods. Rev. Biol. Trop. 66(1): 303-311. Epub 2018 March 01.

Resumen La feromona de camino es uno de los semioquímicos más importantes en las termitas. Esta feromona es responsable del reclutamiento de individuos de la colonia para realizar diversas tareas. El objetivo de este trabajo fue aislar e identificar la feromona de camino de Microcerotermes exiguus (Isoptera: Termitidae), que es una termita típica del Neotrópico, considerada como plaga en algunos cultivos. Nidos subterráneos de M. exiguus fueron recolectados en Caracas, Venezuela en el 2010. Se realizaron diferentes micro-reacciones químicas combinadas con el análisis cromatográfico de los extractos en solventes, así como el de la microextracción en fase sólida (SPME) de las glándulas esternales de las termitas; además de algunos bioensayos de comportamiento. Un pico en los cromatogramas de los extractos (índice de retención:1 483), presentó un patrón de fragmentación con los iones m/z: 41; 55; 67; 79; 91; 105; 119; 135; 142; 180, este resultado junto con los ensayos comportamentales, nos permitieron concluir que el (3Z,6Z,8E)-dodeca-3, 6, 8-trien-1-ol (DTOH) es el compuesto principal de la feromona de camino. La concentración óptima estimada para el reclutamiento y la orientación se encuentra alrededor de 1 pg/cm, siendo estadísticamente comparable al valor en los caminos trazados con extractos de cuerpo entero de 1 obrera /cm. El tiempo que toma este compuesto para reclutar a otros miembros de la colonia es de aproximadamente 13.67 ± 5.76 s y se mantiene hasta por dos horas. Los resultados analíticos y de comportamiento proporcionan una mejor comprensión de la comunicación química de M. exiguus, y dicha información podría ser utilizada para el desarrollo de nuevos métodos de control de plagas.