5(S)-5-Carboxystrictosidine from the Root of Mappianthus iodoides Ameliorates H2O2-induced Apoptosis in H9c2 Cardiomyocytes via PI3K/AKT and ERK Pathways.

5(S)-5-carboxystrictosidine (5-CS) is a compound found in the root of Mappianthus iodoides, a traditional Chinese medicine used for the treatment of coronary artery disease. The aim of the present study was to investigate the protective effect of 5-CS against oxidative stress-induced apoptosis in H9c2 cardiomyocytes and the underlying mechanisms. 5-CS pretreatment significantly protected against H2O2-induced cell death, LDH leakage, and malondialdehyde (MDA) production, which are indicators for oxidative stress injury. 5-CS also enhanced the activity of SOD and CAT. In addition, 5-CS pretreatment significantly inhibited H2O2-induced apoptosis, as determined by flow cytometer, suppressed the activity of caspase-3 and caspase-9, and attenuated the activation of cleaved caspase-3 and caspase-9. 5-CS also increased Akt and ERK activation altered by H2O2 using Western blot analysis. The PI3K-specific inhibitor LY294002 abolished 5-CS-induced Akt activation. The ERK-specific inhibitor PD98059 abolished 5-CS-induced ERK activation. Both LY294002 and PD98059 attenuated the protective effect of 5-CS on H9c2 cardiomyocytes against H2O2-induced apoptosis and cell death. Taken together, these results demonstrate that 5-CS prevents H2O2-induced oxidative stress injury in H9c2 cells by enhancing the activity of the endogenous antioxidant enzymes, inhibiting apoptosis, and modulating PI3K/Akt and ERK signaling pathways.

Three new cassane-type diterpenoids from Caesalpinia sinensis.

Three new cassane-type diterpenoids, namely, (4S)-6ß,12α,19-trihydroxy-cass-13(15)-en-16,12-olide (1), cass-13(15)-en-​16,12-olide (2), and 12α-hydroxy-cass-13(15)-en-16,12-olide (3), were isolated from the seeds of Caesalpinia sinensis. The structures of 1-3 were established by extensive spectroscopic analysis, and their absolute configurations were assigned by electronic circular dichroism (ECD) calculations. The inhibitory activities against PTP1B of the isolated compounds were evaluated. The results showed that compound 2 possessed PTP1B inhibitory activity with an IC50 value of 217.45 ± 36.4 µM.

[Processing evolution,chemical components and pharmacological effects of Bufonis Venenum].

Bufonis Venenum,the dried secretion of Bufo bufo gargarizans or B. melanostictus,is toxic and hard with the efficacy of removing toxicity for detumescence and relieving pain. The processing of Bufonis Venenum dates back to the Song dynasty. In addition to the wine-processing,milk-processing and talcum powder-processing,there were some other kinds of processing methods in ancient times,such as baking,calcining,water-soaking and vinegar-processing. Modern studies have shown that the Bufonis Venenum has the main chemical components of bufadienolides,indole alkaloids sterols,and other compounds. It has the pharmacological effects of antitumor,cardiac,antibacterial,and analgesic activities,local anesthesia,and so on. This paper reviews the processing evolution,chemical components and pharmacological effects of Bufonis Venenum,providing references for its special processing and modern research as well as the theoretical basis for the research on its processing mechanism and quality control.

[Research advances in chemical constituents and pharmacological activities of Pueraria genus].

Kudzu plants in the subfamily sphenoideae of Leguminosae are commonly used herbs in China, Japan, Korea, India and Thailand, with a long history of medicinal use. They are recorded in Chinese Pharmacopoeia, Japanese Pharmacopeia, Korea Pharmacopeia, Ayurveda Pharmacopoeia of India and Flora of Thailand. There are 15-20 species of Pueraria in the world, including 7 species and 2 varieties in China. At present, there are 6 species with medicinal value, such as Pueraria lobata and P. thomsonii. The main chemical components of the genus are isoflavones, flavonoids, terpenes, steroids, coumarins, puerarin glycosides and benzopyrans. A total of 240 compounds have been isolated and identified from this genus, and their pharmacological effects mainly include improvement of the cardiovascular system, antioxidant, hypoglycemic, antipyretic, anti-inflammatory, anti-alcoholic and estrogen-like effects. In this study, chemical constituents and pharmacological activities of Pueraria at home and abroad were systematically summarized, in order to provide references for the material basis, quality control and further development of Pueraria genus.

Three new diterpenes from Dysoxylum lukii and their NO production inhibitory activity.

Three new diterpenes were isolated from the stems of Dysoxylum lukii Merr and characterized on the basis of spectral data. Neoclerod-13Z-ene-3α, 4ß, 15-triol (3) exhibited the inhibition of lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophages with an IC50 value of 25.49 µM.[Formula: see text].

[Study on neoflavonoids from heartwood of Dalbergia latifolia].

Dalbergiae Odoriferae Lignum is derived from heartwood of Dalbergia odorifera,which is national Ⅱ level of rare and endangered protective plants in China. Its resources are scarce and its price is high. In order to find substitutes of D. odorifera,the chemical constituents of 70% ethanol extract of heartwood of D. catifolia were systematically studied by using silica gel,Sephadex LH-20 column chromatography,and semi-preparative HPLC. Sixteen neoflavanoids were isolated and identified as eight dalbergiphenols( 1-8),three dalbergiones( 9-11),two dalbergins( 12,13),two benzophenones( 14,15) and one other type neoflavanoids( 16) based on spectroscopic data analyses and/or comparing the spectroscopic data with those in literature. Among them,compounds 3,7 and 11 were isolated from the genus Dalbergia for the first time,and compounds 2,4-6,8,14 and 15 were isolated from the D. latifolia for the first time. Ten neoflavonoids were both discovered from D. latifolia and D. odorifera.

[Neoflavonoids and their pharmacological activities in Dalbergia genus].

Neoflavonoids are a kind of characteristic components in the Dalbergia genus. Based on the previous researches, 59 neoflavonoids have been obtained from the Dalbergia genus. According to their molecular skeleton, the neoflavonoids can be divided intodalbergiphenols, dalbergiones, dalbergins, benzophenones and other types. Modern research shows that neoflavonoids displayed a variety of pharmacological activities, such as anti-osteoporosis, anti-inflammatory, antitumor, anti-androgen, anti-allergic, antioxidation etc. This paper reviewed neoflavonoids and their pharmacological functions, which could provide the valuable reference for comprehensive utilization and new drug development in the Dalbergia genus.

Novel stilbenes from Artocarpus nanchuanensis.

Four new stilbene derivatives, hypargystilbenes B-E (1-4), together with seven known compounds (5-11), were isolated from the stems of Artocarpus nanchuanensis S.S. Chang. Their structures were elucidated on the basis of spectral data. Hypargystilbene B, hypargystilbene D, and hypargystilbene E exhibited protein tyrosine phosphatase 1B inhibitory effects with corresponding IC50 values of 3.23, 37.31, and 2.53 nM.

[Lignans from Stem Bark of Styrax perkinsiae].

OBJECTIVE: To study the chemical constituents in the stem bark of Styrax perkinsiae. METHODS: The chemical constituents were separated and purified by chromatographic methods after solvent extraction and identified by spectroscopic analyses. RESULTS: Ten lignans were isolated from the stem bark of Styrax perkinsiae and identified as following: pinoresinol 4-O-ß-D-glucopyranoside (1), matairesinoside (2), styraxlignolide B (3), 3- (ß-D-glucopyranosyloxymethyl)-2-(4-hydroxy-3-methoxyphenyl)-5-(3-hydroxypropyl )-7-methoxy-(2R , 3S) -dihydrobenzofuran (4), burselignan (5), (+) -neo-olivil (6), threo-1-(4-hydroxy-3-methoxyphenyl )-2-[ 4-(3-hydroxypropyl)-2-methoxyphenoxy]-1, 3-propanediol (7), erythro-1-(4-hydroxy-3-methoxyphenyl )-2-[ 4-(3-hydroxypropyl )-2-methoxyphenoxy ] -1 ,3-propanediol (8), isolariciresinol(9) and (+) -lariciresinol (10). CONCLUSION: Compounds 5 - 10 are isolated from the plants of Styrax genus for the first time.

[Chemical Constituents from Periplaneta americana].

OBJECTIVE: To study the chemical constituents in Periplaneta americana. METHODS: The chemical constituents were separated and purified by chromatographic methods after solvent extraction and identified by spectroscopic analyses. RESULTS: Ten compounds were isolated from Periplaneta americana and identified as following: 8-hydroxy-3,4-dihydroquinolin-2 (1H)-one (1), cyclo-( L-Phe-L-Pro) (2), cyclo-(Pro-Ile) (3), cyclo-(L-Pro-D-Leu) (4), brevianamide F (5), cyclo-(Ile-Ala) (6), cyclo-( L-Val-L-Pro) (7), cyclo-(L-Pro-L-Tyr) (8), cyclo-(Trp-Val)-dipeptide (9), and (-)-(1S, 3S)-1-methyl-1,2,3,4-tetrahydro-ß-carboline-3-carboxylic acid (10). CONCLUSION: Compounds 2 - 9 are isolated from Periplaneta americana for the first time.

[Chemical Constituents from Dalbergia cochinchinensis].

OBJECTIVE: To investigate the chemical constituents from the heartwood of Dalbergia cochinchinensis. METHODS: Isolate and purify compounds by various column chromatographic methods. Spectral analysis were taken to identify the structures. RESULTS: Elev- en compounds were isolated and identified as dibutyl terephthalate (1), medicarpin (2), pterostilbene (3), 6-hydroxy-2-(2-hydroxy-4- methoxyphenyl)-benzofuran (4), pterocarpol (5), butyl isobutyl phthalate (6), pterolinus B (7), methyl 4-hydroxybenzoate (8), ethyl 4- hydroxybenzoate (9),2-(2'-methoxy-4'-hydroxy)-aryl-3-methyl-6-hydroxy-benzofuran (10) and 6α-hydroxycyclonerolidol (11). CONCLUSION: Compounds 1 and 6~10 are isolated from Dalbergia genus for the first time, and compounds 2, 4 and 11 are isolated from this plant for the first time.

Two new norcassane-type diterpenoids from Mezonevron sinense Hemsl.

Two new norcassane-type diterpenoids, named 6ß-hydroxy-bisnorcass-13-en-12-one (1) and 6ß-hydroxy-bisnorcassan-12-one (2), were isolated from the seeds of Mezonevron sinense Hemsl. The structures of compounds 1-2 were determined by extensive spectroscopic analysis. Two compounds exhibited immunosuppressive activity with the IC50 values of 19.35 ± 0.87 µM and 18.69 ± 0.88 µM in the ConA induced T cell model and 65.04 ± 0.83 µM and 48.06 ± 0.76 µM in LPS induced B cell model, respectively.

Three new caryophyllene-type sesquiterpenoid glycosides from Biebersteinia heterostemon maxim.

Three new caryophyllene-type sesquiterpenoid glycosides were isolated from Biebersteinia heterostemon. Their structures were elucidated by comprehensive analysis of NMR and MS spectroscopic data. All the isolated compounds were evaluated for MCF-7/TAM cytotoxic activity. The results indicated that compound 1 was found to exhibit the weak cytotoxicity against MCF-7/TAM with the IC50 value of 106.4 ± 0.04 µM.

A new lignan from Pandanus tectorius.

A new lignan, named (8S, 8'S)-2,2',3,3'-tetramethoxy-4'-hydroxy-epoxylignan-4-O-ß-D-glucoside (1), together with eight known compounds (2-9), was isolated from the leaves of P. tectorius. Their structures were elucidated on the basis of spectral characteristics and comparison with the data of literatures. Besides, the absolute configuration of 1 was established by using ECD calculations. The cytotoxicity of 1 in vitro against three selected tumor cell lines (A549, HeLa and MCF-7) was evaluated by MTT assay. The results showed that compound 1 exhibited moderate cytotoxicity against HeLa cell with IC50 value of 19.30 ± 4.46 µM.

Serratene triterpenoids from Lycopodium cernuum L. as α-glucosidase inhibitors: Identification, structure-activity relationship and molecular docking studies.

Phytochemical investigation of Lycopodium cernuum L. afforded seven undescribed serratene triterpenoids named 3ß, 21ß-dihydroxyserra-14-en-24-oic acid-3ß-(5'-hydroxybenzoate) (1), 3ß, 21ß, 24-trihydroxyserrat-14-en-3ß-(5'-hydroxyl benzoate) (2), 3ß, 14α, 15α, 21ß-tetrahydroxyserratane-24-methyl ester (3), 3ß, 14α, 21ß-trihydroxyserratane-15α-(4'-methoxy-5'-hydroxybenzoate)-24-methyl ester (4), 3ß, 14α, 21ß-trihydroxyserratane-15α-(4'-methoxy-5'-hydroxybenzoate) (5), 3ß-hydroxy-21ß-acetate-16-oxoserrat-14-en-24-oic acid (6), 3ß, 21ß-dihydroxy-16α, 29-epoxyserrat-14-en-24-methyl ester (7), together with eleven known compounds (8-18), whose chemical structures were elucidated through spectroscopic analysis of HRESIMS, 1D NMR, 2D NMR and comparison between the literature. All compounds were evaluated for their α-glucosidase inhibitory activity for the first time. The results showed that compounds 1, 2, 4, 5, 6, 10, 13, 15, and 16 were among the most potent α-glucosidase inhibitors, with IC50 values ranging from 23.22 ± 0.64 to 50.65 ± 0.82 µM. Structure-activity relationship (SAR) studies indicated that the combined properties of the 5-hydroxybenzoate moiety at C-3, ß-OH at C-21, COOH- at C-24, and Δ14,15 groups enabled an increase in the α-glucosidase inhibitory effect. In addition, molecular docking studies showed that the potential inhibitors mainly interact with key amino acid residues in the active site of α-glucosidase through hydrogen bonds and hydrophobic forces.

Protective effects of 5(S)-5-carboxystrictosidine on myocardial ischemia-reperfusion injury through activation of mitochondrial KATP channels.

5(S)-5-carboxystrictosidine (5-CS) is a compound found in Mappianthus iodoides Hand.-Mazz., root, a traditional Chinese medicine used for the treatment of coronary artery disease. In this study, we investigated whether 5-CS protects heart against I/R injury. Sprague-Dawley rats were treated with 5-CS intraperitoneally for 7 days before the experiment. Hearts were perfused for 20 min global ischemia and 180 min reperfusion. 5-CS significantly inhibited an increase in the post-ischemic left ventricular end-diastolic pressure (LVEDP) and improved the post-ischemic left ventricular developed pressure (LVDP), dP/dt maximum and dP/dt minimum rates of pressure change, and coronary flow as compared with sham group. Pretreatment with 5-hydroxydecanoic acid (5-HD), an inhibitor of mitochondrial KATP channel, for 10 min before ischemia attenuated the improvement of LVEDP, LVDP, dP/dt maximum and dP/dt minimum rates of pressure change, and coronary flow induced by 5-CS. 5-CS markedly decreased the infarct size and attenuated the increased lactate dehydrogenase (LDH) level in effluent during reperfusion. Pretreatment with 5-HD also blocked these protective effects of 5-CS. 5-CS increased Mn-SOD, catalase, and HO-1 levels decreased by I/R injury and pretreatment of 5-HD blocked the 5-CS effects. Increases in Bax, cleaved caspase-3 and cytochrome c levels, caspase-3 and caspase-9 activity, and decrease in Bcl-2 level by I/R injury were attenuated by 5-CS treatment and pretreatment of 5-HD blocked its effects. These results suggest that the protective effects of 5-CS against myocardial I/R injury may be partly related to activating antioxidant enzymes and suppressing apoptosis through opening mitochondrial KATP channels.

[Study on the flavonoids from Mosla chinensis 'jiangxiangru'].

OBJECTIVE: To study the chemical constituents of Mosla chinensis 'jiangxiangru'. METHODS: The chemical components were isolated and purified by silica gel and Sephadex LH-20 column chromatography. The chemical structures were elucidated on the basis of physic chemical properties and spectral data. RESULTS: Five compounds have been isolated from Mosla chinensis 'jiangxiangru'. On the basis of spectral analysis and physicochemical properties, the compounds were identified as negletein (I), luteolin (II), quercetin (III), chrysoeriol (IV) and apigenin (V). CONCLUSION: Compounds I-V are obtained from the genus for the first time.

Near Real-Time Wildfire Progression Monitoring with Sentinel-1 SAR Time Series and Deep Learning.

In recent years, the world witnessed many devastating wildfires that resulted in destructive human and environmental impacts across the globe. Emergency response and rapid response for mitigation calls for effective approaches for near real-time wildfire monitoring. Capable of penetrating clouds and smoke, and imaging day and night, Synthetic Aperture Radar (SAR) can play a critical role in wildfire monitoring. In this communication, we investigated and demonstrated the potential of Sentinel-1 SAR time series with a deep learning framework for near real-time wildfire progression monitoring. The deep learning framework, based on a Convolutional Neural Network (CNN), is developed to detect burnt areas automatically using every new SAR image acquired during the wildfires and by exploiting all available pre-fire SAR time series to characterize the temporal backscatter variations. The results show that Sentinel-1 SAR backscatter can detect wildfires and capture their temporal progression as demonstrated for three large and impactful wildfires: the 2017 Elephant Hill Fire in British Columbia, Canada, the 2018 Camp Fire in California, USA, and the 2019 Chuckegg Creek Fire in northern Alberta, Canada. Compared to the traditional log-ratio operator, CNN-based deep learning framework can better distinguish burnt areas with higher accuracy. These findings demonstrate that spaceborne SAR time series with deep learning can play a significant role for near real-time wildfire monitoring when the data becomes available at daily and hourly intervals with the launches of RADARSAT Constellation Missions in 2019, and SAR CubeSat constellations.

A Deep Convolutional Coupling Network for Change Detection Based on Heterogeneous Optical and Radar Images.

We propose an unsupervised deep convolutional coupling network for change detection based on two heterogeneous images acquired by optical sensors and radars on different dates. Most existing change detection methods are based on homogeneous images. Due to the complementary properties of optical and radar sensors, there is an increasing interest in change detection based on heterogeneous images. The proposed network is symmetric with each side consisting of one convolutional layer and several coupling layers. The two input images connected with the two sides of the network, respectively, are transformed into a feature space where their feature representations become more consistent. In this feature space, the different map is calculated, which then leads to the ultimate detection map by applying a thresholding algorithm. The network parameters are learned by optimizing a coupling function. The learning process is unsupervised, which is different from most existing change detection methods based on heterogeneous images. Experimental results on both homogenous and heterogeneous images demonstrate the promising performance of the proposed network compared with several existing approaches.

A new diaryl 1, 2-diketone from the heartwood of Dalbergia latifolia.

A new diaryl 1,2-diketone, named 1-(2,5-dihydroxy-4-methoxyphenyl)-2-phenylethane-1,2-dione (1), along with eight known compounds (2-9), were isolated from the heartwood of Dalbergia latifolia. They were identified on the basis of spectral data. Compounds 1-7 were obtained from the Dalbergia genus for the first time. Compounds 8 and 9 were firstly isolated from the plant. Compound 1 exhibited inactive against Staphylococcus aureus ATCC 6538 and Escherichia coli ATCC 21530 with the minimum inhibitory concentrations of 10.0 and 10.0 mg/mL, respectively.