Bioactive phenazines from an earwig-associated Streptomyces sp. Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Hao HAN, Zhi-Kai GUO, Bo ZHANG, Mei ZHANG, Jing SHI, Wei LI, Rui-Hua JIAO, Ren-Xiang TAN, Hui-Ming GE Abstract Three new phenazine-type compounds, named phenazines SA—SC (1—3), together with four new natural products (4—7), were isolated from the fermentation broth of an earwig-associated Streptomyces sp. NA04227. The structures of these compounds were determined by extensive analyses of NMR, high resolution mass spectroscopic data, as well as single-crystal X-ray diffraction measurement. Sequencing and analysis of the genome data allowed us to identify the gene cluster (spz) and propose a biosynthetic pathway for these phenazine-type compounds. Additionally, compounds 1—5 exhibited moderate inhibitory activity against acetylcholinesterase (AChE), and compound 3 showed antimicrobial activities against Micrococcus luteus.

Withaminimas A—F, six withanolides with potential anti-inflammatory activity from Physalis minima Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Shan-Shan WEI, Cai-Yun GAO, Rui-Jun LI, Ling-Yi KONG, Jun LUO Abstract Withaminimas A—F (1—6), six new withaphysalin-type withanolides were isolated from the aerial parts of Physalis minima L.. The structures of these compounds were elucidated through a variety of spectroscopic techniques including HR-MS, NMR, and ECD. Compound 1 belongs to rare 18-norwithanolides, and 2—3 were 13/14-secowithanolides. According to the traditional usage of P. minima, inhibitory effects on nitric oxide (NO) production in lipopolysaccaride-activated RAW264.7 macrophages were evaluated, and compounds 1—4 exhibited significant inhibitory effects with IC50 values among 3.91—18.46 μmol·L−1.

Cardamine komarovii flower extract reduces lipopolysaccharide-induced acute lung injury by inhibiting MyD88/TRIF signaling pathways Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Qi CHEN, Ke-Xin ZHANG, Tai-Yuan LI, Xuan-Mei PIAO, Mei-Lan LIAN, Ren-Bo AN, Jun JIANG Abstract In the present study, we investigated anti-inflammatory effect of Cardamine komarovii flower (CKF) on lipopolysaccharide (LPS)-induced acute lung injury (ALI). We determined the effect of CKF methanolic extracts on LPS-induced pro-inflammatory mediators NO and prostaglandin E2 (PGE2), production of pro-inflammatory cytokines (IL-1β, TNF-α, and IL-6), and related protein expression levels of MyD88/TRIF signaling pathways in peritoneal macrophages (PMs). Nuclear translocation of NF-κB-p65 was analyzed by immunofluorescence. For the in vivo experiments, an ALI model was established to detect the number of inflammatory cells and inflammatory factors (IL-1β, TNF-α, and IL-6) in bronchoalveolar lavage fluid (BALF) of mice. The pathological damage in lung tissues was evaluated through H&E staining. Our results showed that CKF can decrease the production of inflammatory mediators, such as NO and PGE2, by inhibiting their synthesis-related enzymes iNOS and COX-2 in LPS-induced PMs. In addition, CKF can downregulate the mRNA levels of IL-1β, TNF-α, and IL-6 to inhibit the production of inflammatory factors. Mechanism studies indicated that CKF possesses a fine anti-inflammatory effect by regulating MyD88/TRIF dependent signaling pathways. Immunocytochemistry staining showed that the CKF extract attenuates the LPS-induced translocation of NF-kB p65 subunit in the nucleus from the cytoplasm. In vivo experiments revealed that the number of inflammatory cells and IL-1β in BALF of mice decrease after CKF treatment. Histopathological observation of lung tissues showed that CKF can remarkably improve alveolar clearance and infiltration of interstitial and alveolar cells after LPS stimulation. In conclusion, our results suggest that CKF inhibits LPS-induced inflammatory response by inhibiting the MyD88/TRIF signaling pathways, thereby protecting mice from LPS-induced ALI.

Vitellaria paradoxa nutshells from seven sub-Saharan countries as potential herbal medicines for treating diabetes based on chemical compositions, HPLC fingerprints and bioactivity evaluation Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Da LI, Jian-Qi XIAO, Wen-Yuan LIU, Chao-Feng ZHANG, Toshihiro AKIHISA, Masahiko ABE, Eliot-T. MASTERS, Wei-Wei ZHAI, Feng FENG, Jie ZHANG Abstract The aim of the study was to determine the feasibility of the Vitellaria paradoxa nutshell as a new medicinal resource for treating diabetes. A total of forty-one compounds were identified by HPLC-DAD-Q-TOF-MS and phytochemical methods in V. paradoxanutshell methanol extract. Based on HPLC fingerprints, four characteristic constituents were quantified and the origin of twenty-eight V. paradoxa nutshells from seven sub-Saharan countries was compared, which were classified into three groups with chemometric method. Twenty-eight samples contained high total phenolic content, and exhibited moderate-higher antioxidant activity and strong α-glucosidase inhibitory activity. Furthermore, all fractions and isolated compounds were evaluated for their antioxidant and α-glucosidase inhibitory activities, and α-glucosidase inhibitory action mechanism of four characteristic constituents including protocatechuic acid, 3, 5, 7-trihydroxycoumarin, (2R, 3R)-(+)-taxifolin and quercetin was investigated via molecular docking method, which were all stabilized by hydrogen bonds with α-glucosidase. The study provided an effective approach to waste utilization of V. paradoxa nutshell, which would help to resolve waste environmental pollution and provide a basis for developing potential herbal resource for treating diabetes.

Cimicifuga heracleifolia is therapeutically similar to black cohosh in relieving menopausal symptoms: evidence from pharmacological and metabolomics studies Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Lan-Yun MIAO, Thi Thanh Huyen CHU, Ping LI, Yan JIANG, Hui-Jun LI Abstract In the market of botanical dietary supplements, Cimicifuga heracleifolia (CH) has always been considered as an adulterated species of Cimicifuga racemosa (CR), a conventional American herb with promising benefits to counteract troubles arising from the menopause. However, the detailed comparison of their therapeutic effects is lacking. In present study, the pharmacological and metabolomics studies were comparatively conducted between CH and CR in ovariectomized (OVX) female rats. Specifically, estrogen-like, anti-hyperlipidemia and anti-osteoporosis effects were evaluated through measuring serum biochemical parameters, histopathological examination and micro computed tomography (Micro-CT) scanning. At the same time, a gas chromatography-mass spectrometry (GC-MS)-based serum metabolomics method was employed to profile the metabolite compositional changes. As a result, both CR and CH displayed anti-osteoporosis and anti-hyperlipemia on menopause syndrome. Meanwhile, their potentials in improving the OVX-induced metabolic disorders were discovered. In conclusion, these results demonstrated that CH is therapeutically similar to CR in relieving menopausal symptoms and CH could be considered as a promising alternative to CR instead of an adulterant in the market of botanical dietary supplements.

Pretreatment of Populus tomentiglandulosa protects hippocampal CA1 pyramidal neurons from ischemia-reperfusion injury in gerbils viaincreasing SODs expressions and maintaining BDNF and IGF-I expressions Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Tae-Kyeong Lee, Joon Ha Park, Ji Hyeon Ahn, Hyunjung Kim, Minah Song, Jae-Chul Lee, Jong Dai Kim, Yong Hwan Jeon, Jung Hoon Choi, Choong Hyun Lee, In Koo Hwang, Bing-Chun YAN, Moo-Ho Won, Il Jun Kang Abstract To examine the effects of Populus tomentiglandulosa (PT) extract on the expressions of antioxidant enzymes and neurotrophic factors in the cornu ammonis 1 (CA1) region of the hippocampus at 5 min after inducing transient global cerebral ischemia (TGCI) in gerbils, TGCI was induced by occlusion of common carotid arteries for 5 min. Before ischemic surgery, 200 mg·kg−1 PT extract was orally administrated once daily for 7 d. We performed neuronal nuclear antigen immunohistochemistry and Fluoro-Jade B staining. Furthermore, we determined in situ production of superoxide anion radical, expression levels of SOD1 and SOD2 as antioxidant enzymes and brain-derived neurotrophic factor (BDNF) and insulin-like growth factor I (IGF-I) as neurotrophic factors. Pretreatment with 200 mg·kg−1 PT extract prevented neuronal death (loss). Furthermore, pretreatment with 200 mg·kg−1 PT extract significantly inhibited the production of superoxide anion radical, increased expressions of SODs and maintained expressions of BDNF and IGF-I. Such increased expressions of SODs were maintained in the neurons after IRI. In summary, pretreated PT extract can significantly increase levels of SODs and protect the neurons against TGCI, suggesting that PT can be a useful natural agent to protect against TGCI.

3′-Methoxydaidzein exerts analgesic activity by inhibiting voltage-gated sodium channels Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Run-Jia XU, Shuo-Han FEI, Lin-Yan CHEN, Gan WANG, Ming LIU, Wen-Sheng ZHANG, Xiu-Wen YAN, Ren LAI, Chuan-Bin SHEN Abstract Isoflavones are widely consumed by people around the world in the form of soy products, dietary supplements and drugs. Many isoflavones or related crude extracts have been reported to exert pain-relief activities, but the mechanism remains unclear. Voltage-gated sodium channels (VGSCs) play important roles in excitability of pain sensing neurons and many of them are important nociceptors. Here, we report that several isoflavones including 3′-methoxydaidzein (3MOD), genistein (GEN) and daidzein (DAI) show abilities to block VGSCs and thus to attenuate chemicals and heat induced acute pain or chronic constriction injury (CCI) induced pain hypersensitivity in mice. Especially, 3MOD shows strong analgesic potential without inducing addiction through inhibiting subtypes NaV1.7, NaV1.8 and NaV1.3 with the IC50 of 181 ± 14, 397 ± 26, and 505 ± 46 nmol·L−1, respectively, providing a promising compound or parent structure for the treatment of pain pathologies. This study reveals a pain-alleviating mechanism of dietary isoflavones and may provide a convenient avenue to alleviate pain.

The mechanisms of traditional Chinese medicine underlying the prevention and treatment of atherosclerosis Publication date: June 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 6 Author(s): Ting-Ting LI, Zhi-Bin WANG, Yang LI, Feng CAO, Bing-You YANG, Hai-Xue KUANG Abstract Atherosclerosis (AS) is a chronic inflammatory disease associated with high morbidity and mortality. The incidence of AS is increasing in the last decades. So development of safe and effective therapeutics for treating AS has become prominently important. Although there are numerous chemical drugs available for treating AS, some drugs are not effective and some have serious side effects. Traditional Chinese medicine (TCM) has a long history for the prevention and treatment of AS due to its less side effects and superior efficacy. This paper describes the effectiveness and underlying mechanisms for prevention and treatment of AS by TCM or its active components. Some TCM, e.g. XuemaiNing, Tongxinluo and Salvia miltiorrhiza have been reported to have cardio-protective effect. Some active components of TCM, e.g. saikosaponin-A, kuwanon G, luteolin and β-elemene have been isolated from various TCM and demonstrated to have beneficial effects on prevention and treatment of AS.

Six new monacolin analogs from red yeast rice Publication date: 20 May 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 5 Author(s): Bing-Yu LIU, Fei XU, Jian BAI, Dao-Jiang YAN, Le ZHANG, Dan ZHANG, You-Cai HU Abstract Six novel monacolin analogs, monacolins V1–V6 (1–6), together with seven known ones (7–13), were isolated from the ethyl acetate extract of red yeast rice. Their structures and absolute configurations were determined by spectroscopic methods, especially 2D NMR (1H-1HCOSY, HSQC, HMBC, and NOESY/ROESY) and CD spectroscopic analyses as well as chemical derivation. Monacolins V2 (2) and V3 (3) represent the first examples of monacolins with 3-hydroxybutyrate substitute. The anti-inflammatory inhibitory activities against the lipopolysaccharide (LPS) induced NO production in BV-2 cells as well as antioxidant activities against rat liver microsomal lipid peroxidation were evaluated.

Dalestones A and B, two anti-inflammatory cyclopentenones from Daldinia eschscholzii with an edited strong promoter for the global regulator LaeA-like gene Publication date: 20 May 2019 Source: Chinese Journal of Natural Medicines, Volume 17, Issue 5 Author(s): Zhen-Zhen ZHOU, Hong-Jie ZHU, Cheng-Long YANG, Yan-Jun LIU, Nan JIANG, Yong-Sheng XIAO, Li-Yun SHI, Rui-Hua JIAO, Hui-Ming GE, Ren-Xiang TAN Abstract Replacement of the native promoter of theglobal regulator LaeA-like gene of Daldinia eschscholzii by a strong gpdA promoter led to the generation of two novel cyclopentenone metabolites, named dalestones A and B, whose structures were assigned by a combination of spectroscopic analysis, modified Mosher’s reaction, and electronic circular dichroism (ECD). Dalestones A and B inhibit the gene expression of TNF-α and IL-6 in LPS-induced RAW264.7 macrophages.