UHPLC-MS characterisation of principal triterpene glycosides and biological activities of different solvent extracts of Allochrusa gypsophiloides (Caryophyllaceae).

A crude methanol extract of the roots of Allochrusa gypsophiloides (syn. Acanthophyllum gypsophiloides) (collected from the Tashkent region of Uzbekistan) was chemically characterised by UHPLC-ESI-QTOF-MS/MS analysis. The results indicate the presence of six major bisdesmosidic saponins derived from gypsogenin, gypsogenic and quillaic acids, including five compounds reported for the first time for this species. The chloroform, methanol and water extracts of A. gypsophiloides showed weak antioxidant and anthelmintic activities. Among the tested extracts, the water extract exhibited the highest level of cytotoxicity in CCRF-CEM and CEM/ADR5000 cell lines with IC50 values of 23.6 and 31.9 µg/mL, respectively.

Lycorine suppresses the malignancy of breast carcinoma by modulating epithelial mesenchymal transition and ß-catenin signaling.

Lycorine, an isoquinoline alkaloid can exhibit significant anti-cancer effects. The present study was conducted to illustrate the underlying mechanisms of action of lycorine on breast carcinoma under in vitro and in vivo settings Tandem Mass Tag assay and Kyoto Encyclopedia of Genes and Genomes analysis revealed that 20 signaling pathways were closely related to tumorigenesis, especially Wnt signaling pathway and tight junctions. The results demonstrated that lycorine evidently inhibited the proliferation of MDA-MB-231 and MCF-7 cells with IC50 values of 1.84 ± 0.21 µM and 7.76 ± 1.16 µM, respectively. It also blocked cell cycle in G2/M phase, caused a decrease in mitochondrial membrane potential, and induced apoptosis pathways through regulating caspase-3, caspase-8, caspase-9, and PARP expression. Moreover, lycorine effectively repressed the ß-catenin signaling and reversed epithelial-mesenchymal transition (EMT) process. Furthermore, 4T1/Luc homograft tumor model was used to further demonstrate that lycorine significantly inhibited the growth and metastasis of breast tumor. These findings highlight the significance of lycorine as potential anti-neoplastic agent to combat breast cancer.

Berberine inhibits breast carcinoma proliferation and metastasis under hypoxic microenvironment involving gut microbiota and endogenous metabolites.

A potential role of berberine, a benzyl isoquinoline alkaloid, in cancer therapy is apparent. Its underlying mechanisms of berberine against breast carcinoma under hypoxia have not been elucidated. We focused on the doubt how berberine restrains breast carcinoma under hypoxia in vitro and in vivo. A molecular analysis of the microbiome via 16 S rDNA gene sequencing of DNA from mouse faeces confirmed that the abundances and diversity of gut microbiota were significantly altered in 4T1/Luc mice with higher survival rate following berberine treatment. A metabolome analysis liquid chromatography-mass spectrometer/mass spectrometer (LC-MS/MS) revealed that berberine regulated various endogenous metabolites, especially L-palmitoylcarnitine. Furthermore, the cytotoxicity of berberine was investigated in MDA-MB-231, MCF-7, and 4T1 cells. In vitro to simulate under hypoxic environment, MTT assay showed that berberine inhibited the proliferation of MDA-MB-231, MCF-7, and 4T1 cells with IC50 values of 4.14 ± 0.35 µM, 26.53 ± 3.12 µM and 11.62 ± 1.44 µM, respectively. Wound healing and trans-well invasion studies revealed that berberine inhibited the invasion and migration of breast cancer cells. RT-qPCR analysis shed light that berberine reduced the expression of hypoxia-inducible factor-1α (HIF-1α) gene. Immunofluorescence and western blot demonstrated that berberine decreased the expression of E-cadherin and HIF-1α protein. Taken together, these results provide evidence that berberine efficiently suppresses breast carcinoma growth and metastasis in a hypoxic microenvironment, highlighting the potential of berberine as a promising anti-neoplastic agent to combat breast carcinoma.

Biological characteristics of Edgeworthia tomentosa (Thunb.) Nakai flowers and antimicrobial properties of their essential oils.

Edgeworthia tomentosa (Thunb.) Nakai belongs to Thymelaeaceae family, its alabastrum is used as the traditional Chinese medicine 'Buddleja Officinalis Maxim'. The present study was to elucidate the ultrastructure characteristics of the flower, the phytochemical composition of the aroma essential oils (EOs) and the relevant antimicrobial properties. There were exclusive characters of calyx, ovule, anther and pollen grain of the flowers under scanning electron microscopy. A total of 40 phytochemical components representing 98% of the EOs were successfully identified: monoterpenes and sesquiterpenes were the dominant terpenoids according to Kovats retention index and MS database. EOs exhibited a broad spectrum antimicrobial activity against Gram-positive and Gram-negative bacteria, the best bacteriostatic effect was against Diplococcus pneumonia with MIC and MBC values ranging between 7.8 and 62.5 and 26.0-71.0 µg/mL, respectively. These results demonstrate that the surface microscopic morphological characteristics of Edgeworthia chrysantha Lindl. flowers, are full-scale chemical composition and antimicrobial properties of the EOs.

Lycorine possesses notable anticancer potentials in on-small cell lung carcinoma cells via blocking Wnt/ß-catenin signaling and epithelial-mesenchymal transition (EMT).

Lycorine, an natural isoquinoline alkaloid has reportedly that possesses multi-anticancer activity. However, to date, the anticancer feature of lycorine in non-small cell lung carcinoma (NSCLC) has still not fully been spelled out. The present study mainly focused on the molecular mechanism of lycorine against NSCLC in vitro and vivo. The results showed that lycorine evidently inhibited proliferation of A549 and H460 with IC50 values were 10.83 ± 1.14 µM and 12.35 ± 1.13 µM, while caused slight cytotoxicity in normal pulmonary epithelial Beas-2B cells, and arrested cell cycle in G0/G1 phase. Hoechst DNA-binding staining showed that typical characteristics of nuclear morphology apoptosis, AnnexinV-FITC/PI staining revealed the early-period apoptosis and the dissipation of mitochondrial membrane potential (Δψm) were also captured after lycorine treatment. Moreover, lycorine effectively repressed the Wnt/ß-catenin signaling and reversed epithelial-mesenchymal transition (EMT). In addition, lycorine also intervened the caspase-mediated mitochondrial apoptosis pathway. Furthermore, A549/Luc tumor xenograft model was also corroborated that lycorine significantly suppressed the growth and metastasis of the lung tumor. These data highlight the significance of lycorine as potential anti-neoplastic agents to combat NSCLC.

The Essential Oil Compositions of Ocimum basilicum from Three Different Regions: Nepal, Tajikistan, and Yemen.

The aerial parts of Ocimum basilicum L. were collected from four different geographical locations, Sindhuli and Biratnagar (Nepal), Chormaghzak village (Tajikistan), and Sana'a (Yemen). The essential oils were obtained by hydrodistillation and analyzed by gas chromatography/mass spectrometry. A cluster analysis of 179 essential oil compositions revealed six major chemotypes: Linalool, eugenol, estragole, methyl eugenol, 1,8-cineole, and geraniol. All four of the basil oils in this study were of the linalool-rich variety. Some of the basil oils were screened for bioactivity including antimicrobial, cytotoxicity in human cancer cells, brine shrimp lethality, nematicidal, larvicidal, insecticidal, and antioxidant. The basil oils in this study were not notably antibacterial, cytotoxic, antioxidant, nor nematicidal, but were active in the brine shrimp lethality test, and did show larvicidal and insecticidal activities.

Chemical Composition of the Essential Oils of Some Central Asian Nepeta Species (Lamiaceae) by GLC-MS.

The chemical composition of the essential oils obtained from aerial parts of Nepeta alatavica Lipsky, N. nuda L, and N. olgae Regel (Lamiaceae), growing wild in Central Asia (Tajikistan and Uzbekistan), were analyzed by GLC and GLC-MS. The main constituents of the essential oil from N. nuda were 1,8-cineole (24.6%), 4a-α,7-ß,7a-α-nepetalactone (21.0%), germacrene D (13.5%), and ß-caryophyllene (12.7%), whereas those of N. alatavica were thymol (48.5%) verbenone (7.7%), and carvacrol (7.5%). In the essential oil of N. olgae the most abundant compounds were acetylcyclohexene (31.5%), 4-tridecyne (13.2%), 2-methyl cyclopentanone (6.8%) and 1,8-cineole (6.0%). The potential antioxidant activity of these essential oils was studied by using DPPH, ABTS and FRAP assays. The essential oil of N. alatavica showed the highest in vitro free radical scavenging activity, probably due to its high thymol and carvacrol content.

Radical scavenging and antioxidant activities of essential oil components--an experimental and computational investigation.

The antioxidant activities of eighteen different essential oil components have been determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay, the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) radical cation assay, and the ferric reducing antioxidant power (FRAP) assay. The phenolic compounds, carvacrol, thymol, and eugenol, showed the best antioxidant activities, while camphor, menthol, and menthone were the least active. The structural and electronic properties of the essential oil components were assessed using density functional theory (DFT) at the B3LYP/6-311++G** level. Correlations between calculated electronic properties and antioxidant activities were generally poor, but bond-dissociation energies (BDEs) seem to correlate with DPPH radical-scavenging activities, and the ferric reducing antioxidant power (FRAP) assay correlated with vertical ionization potentials calculated at the Hartree-Fock/6-311++G** level.

Aromatic Medicinal Plants from Tajikistan (Central Asia).

Tajikistan is a small country located in Central Asia. The mostly mountainous terrain with a continental, subtropical, and semiarid climate, is characterized by diverse flora. Many people in Tajikistan rely on medicinal plants as their traditional form of medicine to prevent and cure health disorders. Aromatic medicinal plants, in particular, have played an important role for the local people. In this review, we present a summary of the uses of 18 aromatic medicinal plants from Tajikistan and their compositions of secondary metabolites.

Composition of essential oil from Tagetes minuta and its cytotoxic, antioxidant and antimicrobial activities.

The essential oil from the leaves of Tagetes minuta L., growing wild in Yemen, was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry. A total of 28 compounds were identified representing 74.2% of total oil composition. Major components of the essential oil were (Z)-ocimenone (15.9%), (E)-ocimenone (34.8%), (Z)-beta-ocimene (8.3%), limonene (2.3%), (Z)-tagetone (1.8%), dihydrotagetone (1.4%) and an unidentified dimethylvinylketone derivative (20.6%). The oil showed moderate cytotoxic activity against MCF-7 breast tumor cells, with an IC50 of 54.7 +/- 6.2 microg/mL. In the DPPH radical scavenging assay, T. minuta oil showed potent antiradical activity with an IC50 value of 36 microg/mL. Antimicrobial activity was also investigated on several microorganisms, and the essential oil exhibited high activity against methicillin-resistant Staphylococcus aureus (MRSA) with an inhibition zone of 23 mm. It also exhibited remarkable antifungal activity against Candida albicans with an inhibition zone of 26 mm.

Chemical composition and biological activity of essential oil from Pulicaria undulata from Yemen.

The chemical composition of the essential oil obtained from the leaves of Pulicaria undulata Gamal Ed Din (syn P. orientalis sensu Schwartz and P. jaubertii Gamal Ed Din) was analyzed by GC-MS. Major compounds of P. undulata oil were the oxygenated monoterpenenes, carvotanacetone (91.4%) and 2,5-dimethoxy-p-cymene (2.6.%). The antimicrobial activity of the essential oil was evaluated against six microorganisms, Escherichia coli Pseudomonas aeruginosa, Staphylococcus aureus, methicillin-resistant S. aureus, Bacillus subtilis, and Candida albicans, using disc diffusion and broth microdilution methods. The oil showed the strongest bactericidal activity against Staphylococcus aureus and methicillin-resistant S. aureus, as well as Candida albicans. The essential oil showed moderate cytotoxic activity against MCF-7 breast tumor cells, with an IC50 of 64.6 +/- 13.7 microg/mL. Bioautographic assays were used to evaluate the acetylcholinesterase inhibitory effect as well as antifungal activity of the oil against Cladosporium cucumerinum.

Chemical diversity of Ziziphora clinopodioides: composition of the essential oil of Z. clinopodioides from Tajikistan.

The chemical composition of the essential oils of Ziziphora clinopodioides Lam. from the aerial flowering parts, collected during two different years, were obtained by hydrodistillation and analyzed by gas chromatography - mass spectrometry. Forty-five components representing 100% and 94.7% of the total oil were identified. The main constituents of the essential oils were pulegone (72.8 and 35.0%), neomenthol (6.5 and 23.1%), menthone (6.2 and 13.3%), p-menth-3-en-8-ol (1.7 and 3.5%), piperitenone (2.6 and 1.1%) and piperitone (0.7 and 1.2%). A cluster analysis was carried out on the essential oil compositions of Z. clinopodioides.

The essential oil of Artemisia scoparia from tajikistan is dominated by phenyldiacetylenes.

The essential oil from the aerial parts of Artemisia scoparia was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry. A total of 32 compounds were identified representing 98.0% of the total oil composition. A. scoparia oil was dominated by the diacetylenes 1-phenyl-2,4-pentadiyne (34.2%) and capillene (4.9%). Other major components were beta-pinene (21.3%), methyl eugenol (5.5%), alpha-pinene (5.4%), myrcene (5.2%), limonene (5.0%), and (E)-beta-ocimene (3.8%). The oil was tested for in-vitro cytotoxic activity against MCF-7 cells, but was inactive.

Composition of the essential oil of Origanum tyttanthum from Tajikistan.

Origanum tyttanthum Gontsch. was collected from two different sites in south-central Tajikistan. The essential oils were obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry. A total of 52 compounds were identified representing 99.0-100% of total oil compositions. The major components of Origanum tyttanthum Gontsch. oil were carvacrol (34.3-59.2%), thymol (10.8-46.4%), p-cymene (0.7-7.3%), beta-thujone (1.9-4.1%), piperitenone oxide (0.1-3.8%), gamma-terpinene (0.3-3.5%), cis-piperitone epoxide (0.8-3.3%), carvacrol acetate (0.4-2.4%), menthone (0.6-2.1%) and borneol (1.0-2.3%).