The updated weeping forsythia genome reveals the genomic basis for the evolution and the forsythin and forsythoside A biosynthesis

Weeping forsythia (Forsythia suspensa,Oleaceae) is a deciduous broad-leaved tree species distributed in the warm temperate zone of China.However,the species still lacks a chromosome-level genome.In this study,the former draft genome (Accession No.WIPI00000000) of weeping forsythia was assembled into 14 chromosomes with a 712.9 Mb genome size.Weeping forsythia underwent a and b whole-genome duplication events.After the divergence between weeping forsythia and Olea europaea,1 453 gene families had a significant expansion,and 1 146 gene families had a significant contraction.The enrichment pathways and ontologies of expanded genes suggested that the tillering,photosynthesis and growth capacity of weeping forsythia were enhanced after the divergence of weeping forsythia and O.europaea.The contracted genes suggested that the resistance of weeping forsythia to cold and drought was weakened.The last glacial period led to a significant decline in the effective population size of weeping forsythia.Forty-six candidate genes were identified for the synthesis of the forsythin and forsythoside A by genomic and transcriptomic data.In this study,we improved the previous draft genome of weeping forsythia.Our genome will provide genomic resources for the subsequent evolution and breeding research of weeping forsythia.

Forsythosides as Essential Components of Forsythia-based Traditional Chinese Medicines Used to Treat Inflammatory Diseases and COVID-19

The dried fruits of the plant Forsythia suspensa(Forsythia Fructus: Lianqiao in Chinese) are used in many herbal preparations to treat various diseases or the associated symptoms. Forsythia extracts contain phenylethanoid glycosides(Ph Gs) such as the forsythosides(Fst A-to-P). The leading products, Fst-A,-B and-F(arenarioside), can be found also in >90 other plants inventoried here. The pharmacological properties of Fst are reviewed, with emphasis on their anticancer, antiviral, and antibacterial activities, which essentially derive from their anti-inflammatory and antioxidant effects. Fst-B functions as a potential binder of the repressor protein Kelch-like ECH-association protein 1(Keap 1), thus promoting the nuclear translocation of the transcription factor Nuclear factor erythroid 2-related factor 2(Nrf2) implicated in the subsequent activation of the production of antioxidant enzymes and repression of the oxidative stress. The regulation of the Nrf2/Heme oxygenase-1 pathway is the central piece of the multifaceted mechanism of action of Fst-A/B. Their prominent antioxidant and anti-inflammatory effects support the use of these compounds in different inflammation-related diseases and conditions, from sepsis to neuroprotection and many other pathologies discussed here. In addition, these properties contribute to the antiviral action of the compounds. Fst-A/B displays activities against the influenza A virus and different Fst-containing traditional Chinese medicinal(TCMs) have revealed beneficial effects to combat the current COVID-19 pandemic. The mechanisms whereby Fst-A/B could inhibit viral multiplication are discussed. Ph Gs likely contribute to the anti-COVID-19 activities reported with several TCM such as Shuang-Huang-Lian oral liquid, Lianhua-Qingwen capsules, and others. This review highlights the pharmacological profile of Fst and illustrates health benefits associated with the use of Forsythia Fructus.

紫珠的水溶性成分(英文)

目的:研究中药紫珠的水溶性成分。方法:运用多种色谱技术进行分离纯化,运用光谱技术鉴定化合物结构。结果:从紫珠的水溶性提取物中分离到4个苯丙素苷类化合物,分别鉴定为连翘苷(forsythoside B,1),arenarioside(2),类叶升麻苷(acteoside,3)和异类叶升麻苷(isoacteoside,4)。结论:这4个化合物都是首次从该植物中分离得到。

Forsythiaside A Induced IFN-α and Up-regulated the Correlated Factors in JAK-STAT Signaling Pathway in vitro

[Objective] This study was to investigate the effect of forsythiaside A added in chick embryo kidney cells (CEKs), on the changes in expression of interferon α(IFN-α) and mRNA expression level of correlated factors in JAK-STAT pathway. [Methods] Three levels of forsythiaside (100, 200, 400 μg/ml) were adopted to treat the experimental materials, then the expression levels of IFN-α and correlated factors in JAK-STAT pathway were detected by real-time RT-PCR at the transcriptional level (mRNA) and by Western blot at the translation level(IFN-α protein). [Result] Compared with the control group (untreated group), Application of forsythiaside A not only significantly increased the expression of IFN-α in treated CEKs (P<0.05) , but also up-regulated the expression of STAT1, JAK1, IFNAR1, IFNAR2, IRF1 and IRF7, the correlated factors in JAK-STAT pathway. [Conclusion] Forsythiaside A induced the expression of IFN-α in CEKs, and can positively regulate the JAK-STAT signaling pathway significantly.

连翘中苯乙醇甙类化合物

从连翘果实中分离了三种苯乙醇甙类化合物，calceolarioside A(1),plantainoside A(2)和forsythoside A(3），用光谱方法鉴定了它们的结构。1和2系首次从本属植物中分离得到，通过^1H－^1H COSY和^13C-^1H COSY对3的氢信号与碳信号进行正确归属，补充文献的不足，3能显著促进Con A诱导的淋巴细胞转化，提示其具有增强免疫作用，该活性未见报导。

Phenylethanoid Glycosides from Forsythia suspensa Vahl

从连翘果实中分离了三种苯乙醇甙类化合物，ｃａｌｃｅｏｌａｒｉｏｓｉｄｅＡ（１），ｐｌａｎｔａｉｎｏｓｉｄｅＡ（２）和ｆｏｒｓｙｔｈｏｓｉｄｅＡ（３），用光谱方法鉴定了它们的结构。１和２系首次从本属植物中分离得到。通过１Ｈ１ＨＣＯＳＹ和１３Ｃ１ＨＣＯＳＹ对３的氢信号与碳信号进行正确归属，补充文献的不足。３能显著促进ＣｏｎＡ诱导的淋巴细胞转化，提示其具有增强免疫作用，该活性未见报导。

Study on the Optimum Picking Time of Callicarpa kwangtungensis

[Objective] This study was conducted to compare total contents of poliumoside and forsythoside B from Callicarpa kwangtungensis Chun in Qiandongnan Miao and Dong Autonomous Prefecture collected in different seasons, which could provide reference for its deep development and utilization. [Methods] Poliumoside and forsythoside B were measured according to the pharmacopoeia standard in the middle of each month in 2014, and the yield of C. kwangtungensis was simultaneously evaluated. All these results provided data reference for the determination of suitable picking time for C. kwangtungensis. [Results] The results showed the content of poliumoside and forsythoside B in C. kwangtungensis was the highest in November, and the content of the medicinal material in August was over eight times higher than the pharmacopoeia standard, besides at this month the yield was the highest during the year. Comprehensively, mid October is the optimum picking time for C. kwangtungensis in Taijiang. [Conclusion] Dynamic variations of content of poliumoside and forsythoside B in and yield of C. kwangtungensis were investigated, which would significantly benefit production of C. kwangtungensis in Qiandongnan Miao and Dong Autonomous Prefecture.

Inhibition of intracellular proton-sensitive Ca^(2+)-permeable TRPV3 channels protects against ischemic brain injury

Ischemic brain stroke is pathologically characterized by tissue acidosis, sustained calcium entry and progressive cell death. Previous studies focusing on antagonizing N-methyl-D-aspartate(NMDA) receptors have failed to translate any clinical benefits, suggesting a non-NMDA mechanism involved in the sustained injury after stroke. Here, we report that inhibition of intracellular proton-sensitive Ca^(2+)-permeable transient receptor potential vanilloid 3(TRPV3) channel protects against cerebral ischemia/reperfusion(I/R) injury. TRPV3 expression is upregulated in mice subjected to cerebral I/R injury. Silencing of TRPV3 reduces intrinsic neuronal excitability, excitatory synaptic transmissions, and also attenuates cerebral I/R injury in mouse model of transient middle cerebral artery occlusion(tMCAO). Conversely, overexpressing or re-expressing TRPV3 increases neuronal excitability, excitatory synaptic transmissions and aggravates cerebral I/R injury. Furthermore, specific inhibition of TRPV3 by natural forsythoside B decreases neural excitability and attenuates cerebral I/R injury. Taken together, our findings for the first time reveal a causative role of neuronal TRPV3 channel in progressive cell death after stroke, and blocking overactive TRPV3 channel may provide therapeutic potential for ischemic brain injury.

Simultaneous Determination of Eight Active Components in Liuwei Wuling Tablet Using HPLC

Objective To develop an effective method for simultaneous determination of eight major components in Liuwei Wuling Tablet（LWT）. Methods Reversed phase HPLC method was used with variously improved conditions. Results Salidroside, forsythoside A, specnuezhenide, phillyrin, schisandrol A, schizandrol A, schizandrin A, and schizandrin B in LWT were successfully separated on a Kromasil 100-5-C_（18） reverse phase column（250 mm × 4.6 mm, 5 μm） using acetonitrile -0.1% phosphoric acid（gradient elution） as mobile phase. The detection wavelength was 275 nm with flow rate of 1.0 mL/min, and the column temperature was maintained at 35 ℃. The recovery rate of the method was within the range of 95.13%-104.56% and the precision（RSD） was less than 3% for all eight analytes. All the compounds showed good linearities（r^2〉0.9980） in a relatively wide concentration range. Conclusion Simultaneous quantification of the multiple components by HPLC would be a better strategy for the quality evaluation of LWT.