Phenothiazine-based fluorescent probes for the detection of hydrazine in environment and living cells.

As an important chemical raw material, hydrazine brings convenience to people's lives and provides opportunities for human development. However, the misuse or leakage of hydrazine has brought pollution to the environment, including water, soil and living organisms. At the same time, hydrazine poses a potential threat to human health as a carcinogen. Despite the enormous challenges, it is crucial to develop an effective method to detect hydrazine in environmental samples. In this work, we have synthesized a series of probes based on phenothiazine fluorophore by the introduction of different substituents and developed a novel probe for the detection of hydrazine. The probe is capable of detecting hydrazine in aqueous solutions with high sensitivity and selectivity, and can be easily fabricated into paper test strips for use in in situ samples. In addition, the probe is effective in detecting hydrazine in water, soil, cells, and zebrafish, providing an excellent tool for detecting hydrazine in the environment.

Aptamer-functionalized two-photon SiO2@GQDs hybrid-based signal amplification strategy for targeted cancer imaging.

Targeted imaging is playing an increasingly important role in the early detection and precise diagnosis of cancer. This need has motivated research into sensory nanomaterials that can be constructed into imaging agents to serve as biosensors. Graphene quantum dots (GQDs) as a valuable nanoprobe show great potential for use in two-photon biological imaging. However, most as-prepared GQDs exhibit a low two-photon absorption cross-section, narrow spectral coverage, and "one-to-one" signal conversion mode, which greatly hamper their wide application in sensitive early-stage cancer detection. Herein, a versatile strategy has been employed to fabricate an aptamer Sgc8c-functionalized hybrid as a proof-of-concept of the signal amplification strategy for targeted cancer imaging. In this study, GQDs with two-photon imaging performance, and silica nanoparticles (SiO2 NPs) as nanocarriers to provide amplified recognition events by high loading of GQD signal tags, were adopted to construct a two-photon hybrid-based signal amplification strategy. Thus, the obtained hybrid (denoted SiO2@GQDs) enabled extremely strong fluorescence with a quantum yield up to 0.49, excellent photostability and biocompatibility, and enhanced bright two-photon fluorescence up to 2.7 times that of bare GQDs (excitation at 760 nm; emission at 512 nm). Moreover, further modification with aptamer Sgc8c showed little disruption to the structure of the SiO2@GQDs-hybrid and the corresponding two-photon emission. Hence, SiO2@GQDs-Sgc8c showed specific responses to target cells. Moreover, it could be used as a signal-amplifying two-photon nanoprobe for targeted cancer imaging with high specificity and great efficiency, which exhibits a distinct green fluorescence compared to that of GQDs-Sgc8c or SiO2@GQDs. This signal amplification strategy holds great potential for the accurate early diagnosis of tumors and offers new tools for the detection a wide variety of analytes in clinical application.

Open-Air Dual-Diamination of Aromatic Aldehydes: Direct Synthesis of Azolo-Fused 1,3,5-Triazines Facilitated by Ammonium Iodide.

A new and practical protocol for the synthesis of medicinally privileged azolo[1,3,5]triazines by simply heating under air has been presented. The in situ generated N-azolo amidines from commercially available aromatic aldehydes and 3-aminoazoles with ammonium iodide undergo the second diamination to accomplish the [3 + 1 + 1 + 1] heteroannulation reaction. This convenient process is appreciated by high efficiency, broad substrate scope, gram-scale synthesis, and operational simplicity under reagent-free conditions.

Triterpenoids with α-glucosidase inhibitory activity from Artemisia argyi.

Two new nordammarane-type triterpenoids, 3ß-acetoxy-20-oxo-21-nordammaran-23-carboxylic acid methyl ester (1) and 3ß-acetoxy-17ß-dammaranic acid (2), along with two known cycloartane-type triterpenoids (3-4), were isolated from the petroleum ether-soluble extract of Artemisia argyi. Their structures were elucidated based on 1D and 2D NMR spectroscopic data analysis. All compounds were evaluated for their α-glucosidase inhibitory activity in vitro. Compounds 1-4 exhibited significant inhibitory effects on α-glucosidase with IC50 values ranging from 38.34 ± 0.23 to 105.54 ± 0.33 µM.

Sesquiterpenoids from Artemisia argyi and their COXs inhibitory activities.

Four new sesquiterpene lactones, named artemargyinolides A-D (1-4), and seven known sesquiterpenoids (5-11) were isolated from Artemisia argyi. Their structures were elucidated based on the extensive analysis of spectroscopic data. The absolute configuration of 1 was assigned by X-ray crystallographic analysis. Compound 1 is an unprecedented sesquiterpene dimer-monoterpene lactone. The cyclooxygenases (COX-1 and COX-2) inhibitory activities of all isolated compounds were evaluated. Compounds 1, 2, 4, and 6-11 showed inhibitory activity against COX-2 with IC50 values ranging from 35.78 ±â€¯0.39 to 256.07 ±â€¯0.38 µM. However, compounds 7, 9, and 10 exhibited weak inhibitory activity against COX-1 with IC50 values of 465.70 ±â€¯1.53, 281.43 ±â€¯3.56, and 490.45 ±â€¯6.07 µM, respectively. Other compounds are inactive against COX-1. Therefore, compounds 1, 2, 4, 6, 8, and 11 displayed selective COX-2 inhibitory activity.

Phthalide dimers from Angelica sinensis and their COX-2 inhibition activity.

Four new dimeric phthalides, angesinenolides C-F (1-4), along with three known ones, were isolated from the roots of Angelica sinensis. Their structures were determined by means of HRMS and NMR experiments. The structures of compounds 1 and 3 were confirmed using X-ray crystallographic data. All isolated compounds were tested for activities on the inhibition of COX-2 enzyme in vitro. Compounds 1-6 exhibited inhibitory activity against COX-2 with IC50 values ranging from 29.32 ±â€¯0.07 to 137.91 ±â€¯0.24 µM.

Two new flavonoids from Artemisia argyi with their anticoagulation activities.

A new flavone glycoside, eupatilin 7-O-ß-d-glucopyranoside (1) and a new flavone, 5,6,2',4'-tetrahydroxy-7,5'-dimethoxyflavone (2), were isolated from Artemisia argyi. Their structures were unambiguously elucidated by extensive spectroscopic analysis. Both flavonoids were evaluated for in vitro anticoagulation activities. Compound 1 significantly extended thrombin time. Compound 2 had obvious effect in increasing prothrombin time.

Phthalide Derivatives with Anticoagulation Activities from Angelica sinensis.

Two new phthalide derivatives, angesinenolides A and B (1 and 2), were isolated from the roots of Angelica sinensis. Their structures were elucidated using HRMS, NMR, and X-ray crystallographic data. Compound 1 is the first example of a phthalide trimer presumably formed through two [2+2] cycloaddition reactions. Compound 2 is a unique dimeric phthalide with a peroxy bridge between C-3a and C-6. Both phthalides were evaluated for in vitro anticoagulation activities. Compound 1 reduced the level of fibrinogen (FIB). Compound 2 significantly extended thrombin time and activated partial thromboplastin time, as well as markedly reduced the content of FIB.

[Research progress of structures and pharmacological activities of phthalides from Angelica sinensis].

Angelica sinensis(Umbelliferae)is a worldwide-known medicinal plant and also a famous traditional Chinese medicinal herb. It is recorded to possess the efficacy of enriching the blood and invigorating the circulation of blood of the individual.Danggui was extensively applied to the treatment of gynecological disorders. Modern researches indicate that phthalides are main chemical components related to the bioactivities of A.sinensis, such as anti-tumor, analgesic and neuroprotective effect.The advances in studies on the structures and pharmacological activities of phthalides from A.sinensis are reviewed to provide references for further researches and utilization of their medicinal value.

Geranyl flavonoids from Robinia pseudoacacia.

A new geranyl flavonol, robipseudin A (1), and a known geranyl flavone, kuwanon S (2), were isolated from the leaves of Robinia pseudoacacia. The structure of the new compound was determined by spectroscopic methods. Compounds 1 and 2 showed moderate antioxidant activities in the DPPH radical scavenging assay.

Japonicasins A and B, two new isoprenylated flavanones from Sophora japonica.

Two new flavanones with a C15 isoprenoid group, japonicasins A and B (1 and 2), were isolated from the leaves of Sophora japonica. This is the first report on the presence of the (2E,7E)-6-isopropyl-3,9-dimethyldeca-2,7,9-trien-1-yl group (C15 isoprenoid group) in isoprenylated flavonoids. Their structures were determined by spectroscopic methods, including UV, IR, 1D and 2D NMR, HRESIMS, and CD experiments. In addition, the antioxidant activities of compounds 1 and 2 were determined through DPPH radical scavenging assays. They exhibited potential antioxidant activities, with IC50 values of 35.1±0.8 µM and 88.7±1.1 µM for compounds 1 and 2, respectively.

[Influence of different processing methods on Angelica sinensis polysaccharides from same origin].

OBJECTIVE: To study the influences of different processing methods on the content of Angelica sinensis polysaccharides (APS) from the same origin. METHOD: The contents of neutral polysaccharides and acidic polysaccharides in various samples of A. sinensis were determined by phenol-sulfuric acid and carbazole-sulfuric acid method, respectively. The proliferation ability of lymphocyte was detected by MTT method after the cells were cultured with different concentrations of APS from two samples processed by different methods. RESULT: The different processing methods had different effects on the contents of polysaccharide. The maximum content of APS (26.03%) was found in the sample processed by microwave drying medium-fired, but the minimum content of APS (2.25%) was found in the sample processed by vacuum drying at 50 TC. Furthermore, the APS (high concentration group, P < 0.01) processed by microwave drying medium-fired could both accelerate proliferation of spleen lymphocytes directly and increase proliferation of T cells of mice induced by Con A. However, the APS processed by far-infrared drying did not show conspicuous immune enhancement activity. CONCLUSION: Different processing methods have different effects on the contents of APS and the proliferation ability of lymphocytes.

[Traditional experiences and modern cognition on primary processing of traditional Chinese medicinal materials].

Primary processing is important links and closely related to the quality of traditional Chinese medicinal materials. The methods and technologies system of traditional primary processing were derived from the long-term practices and experiences, which is distinctive, colorful and diverse, and scientific, it is not only to cleaning of remove the non-officinal parts, drying for termination the physiological status of organisms, but also to retain the most active substances, decrease the toxic components, and promote the transformation among chemical ingredients through primary processing. So the traditional primary processing endowed with characters, quality, specifications and properties of traditional Chinese medicine, and embodied some important science truth. This paper analyzed the traditional experiences and modern cognition on primary processing of TCM materials based on the changes of chemical compositions and explored the scientific truth. These data may be providing foundation and support for process of normalization and standardization of primary processing of TCM materials.