BRITISH JOURNAL OF PHARMACOLOGY
·
2025
·
IF 7.7
Huan Li,Chang Chen,Xinzhu Chen,Jiale Liu,Chen Luo,Huilin Chen,Xiaoyu Geng,Zheng Pan
Background and Purpose We previously showed that the iridoid glycoside extract of Lamiophlomis rotata (IGLR) induces M2 macrophage polarisation to accelerate wound healing. The potentially active compounds (quality markers) in IGLR that accelerate wound healing have not been elucidated; we here identified quality markers that accelerate wound healing. Experimental Approach After IGLR gavage of dorsal excisional wound mice and normal mice for 7 days, the tissues were analysed using the matrix-assisted laser desorption/ionisation (MALDI) mass spectrometry imaging (MSI) method and were further validated by liquid chromatography/mass spectrometry (LC/MS) coupled with multivariate analyses to identify quality markers. Key Results Using the MSI assay, Shanzhiside methyl ester (SM), 8- O -acetylshanzhiside methyl ester (ASM) and Phlorigidoside C (PhC) were identified as the quality markers in IGLR and overlapped with endogenous metabolites (lactate, citrate and itaconate) in the same class by UMAP manifold analysis. Additionally, the results were also confirmed by UPLC-Q/TOF-MS coupled with multivariate analyses of the skin tissues in normal and wound groups. MSI data from the livers and kidneys revealed that the accumulation of SM, ASM and PhC in the livers significantly increased in the model group, and the ion intensity of their glucuronide conjugates in the kidneys was decreased compared to the normal group. These results suggested that bioavailability of these compounds was improved in the wound group. Conclusions and Implications The overall data demonstrated that SM, ASM and PhC were selectively increased in new granulation tissues, and are most likely the quality markers that accelerate wound healing. Graphical
研究领域:
药理学
·
分子生物学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 5
·2459-2468
·
IF 2.936
Dan Zhang,Yun-ling Gao,Sheng Jiang,Yiwen Chen,Yi Zhang,Zheng Pan
Lamiophlomis rotata (L. rotata) is a Tibetan medicinal herb used for centuries that contains iridoid glycosides (IGs), which are pharmacologically active ingredients and can be used for quality control. The IG profiles of the underground and aerial parts of the plant were determined by UPLC-TOF-MS to evaluate the similarity and variability of the different herbal parts listed in the Chinese Pharmacopoeia. Twenty-six IGs were detected in the total ion current (TIC) profile of L. rotata, and twenty-two of these were identified by comparing the retention times and mass spectra of the compounds to those of authentic standards. Among these compounds, five IGs with the same molecular formula (C17H26O11) were identified for the first time by mass spectrometry based on their different hydroxyl group-substituted positions. The aerial part has a similar chemical profile to that of the roots. The difference between the two parts was determined by multivariate statistical analysis of the UPLC-TOF-MS data of 24 specimens. Sesamoside was explored as the most characteristic marker to distinguish the two parts of L. rotata. To further estimate the distinction between the two parts, the content of total IGs and the antioxidant capacity were investigated in samples from different locations. The aerial parts showed a high content of total IGs and high antioxidant capacity, although not higher than those of the roots. The results also suggest the dosage should be increased when the aerial parts are used as crude medicinal materials instead of the underground parts.
研究领域:
药用植物学
·
中药化学
·
质量控制
✓ 已验证
产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2026
·
IF 5.9
Xiaoli Yi,Siwei Xiong,Wenbi Tuo,Jun Zhao,Peng Guo,Qin Yang,Weidong Zhang,Yunzhi Tian,Yingying Du,Yanqing Shu,Jiehao Jia,Pengcheng Li,Yongjun Zhu,Chen Zhang,Yan Qu
Wounds are susceptible to persistent infections and chronic inflammation, which can significantly impeding the healing process. Lamiophlomis rotata (Benth.) Kudo (LR), a traditional Tibetan medicine, is known for its efficacy in treating injuries, contusions, and skin ulcers. Existing LR-related formulations such as capsules and patches are primarily used for pain relief and cannot provide an optimal environment for infected wounds, thereby limiting their healing potential. In this study, we successfully extracted an extract of LR and confirmed its strong antibacterial activity, supporting its use in infected wound management. A gel matrix was developed using carbomer 940 (CP940) as the base, along with glycerol, 1,2-propanediol, and other excipients. The LR was incorporated into this matrix to obtain Lamiophlomis rotata (Benth.) Kudo gel (LR Gel). Rheological experiments characterized the adhesion and mechanical strength of LR Gel, confirming that it possesses sufficient adhesive force and mechanical strength to tightly adhere to and protect the wound site. Animal experiments showed that LR Gel effectively modulates immune activity and significantly promotes healing in a rat model of infectious full-thickness skin defects. These findings indicate that the LR Gel can prevent wound infection and secondary damage, offering a safe and efficient treatment for infected wounds with promising clinical application.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Natural Product Communications
·
2026
·
IF 1.5
Yue Wu,Guo-long Dong,Qi-lin Li,Jiang-hong Ran,Qian-yin Pan,Li Li
Objectives/BackgroundSensitive scalp (SSc) is a skin condition characterized by various unpleasant reactions. Plant extracts, particularly Lamiophlomis rotata (Benth.) Kudo (L. rotata), are used for their natural antioxidant, antibacterial and anti-inflammatory properties in the treatment of sensitive scalp.MethodsWe extracted the active ingredient in L. rotata and used it to improve SSc. We recruited 30 volunteers with SSc using a 10Q questionnaire. The volunteers were asked to apply a 0.5% extract of L. rotata to their affected scalps on a regular basis. The volunteers’ scalp microbiome was analyzed by high-throughput sequencing, and non-invasive physiological indices were assessed.ResultsAfter two weeks (tw2) of treatment, epidermal water loss (TEWL), temperature and pH decreased significantly, while scalp moisture (CM) and sebum (SM) levels remained stable. Furthermore, analysis of the scalp microbiome revealed a decrease in the ratio of Malassezia restricta to Malassezia globosa from 14.57 to 3.65, and an increase in the ratio of Cutibacterium acnes to Staphylococcus capitis from 0.93 to 1.82.ConclusionL. rotata extracts were found to be effective in repairing the scalp barrier and modulating the microbiota, thereby alleviating symptoms such as itching, burning, tightness and redness associated with bacterial and fungal activity.
✓ 已验证
DOI
高影响因子
Chinese Medicine
·
2024
·Vol. 19
·期 1
·1-19
·
IF 5.3
Geng Xiaoyu,Wang Ying,Li Huan,Song Liang,Luo Chen,Gu Xiaojie,Zhong Haixin,Chen Huilin,Chen Xinzhu,Wang Jianwei,Pan Zheng
Background Lamiophlomis rotata (Benth.) Kudo ( L. rotata ), the oral Traditional Tibetan herbal medicine, is adopted for treating knife and gun wounds for a long time. As previously demonstrated, total iridoid glycoside extract of L. rotata (IGLR) induced polarization of M2 macrophage to speed up wound healing. In diabetic wounds, high levels inflammatory and chemotactic factors are usually related to high reactive oxygen species (ROS) levels. As a ROS target gene, nuclear factor erythroid 2-related factor 2 (NRF2), influences the differentiation of monocytes to M1/M2 macrophages. Fortunately, iridoid glycosides are naturally occurring active compounds that can be used as the oxygen radical scavenger. Nevertheless, the influence of IGLR in diabetic wound healing and its associated mechanism is largely unclear. Materials and methods With macrophages and dermal fibroblasts in vitro, as well as a thickness excision model of db/db mouse in vivo, the role of IGLR in diabetic wound
healing and the probable mechanism of the action were investigated. Results Our results showed that IGLR suppressed oxidative distress and inflammation partly through the NRF2/cyclooxygenase2 (COX2) signaling pathway in vitro . The intercellular communication between macrophages and dermal fibroblasts was investigated by the conditioned medium (CM) of IGLR treatment cells. The CM increased the transcription and translation of collagen I (COL1A1) and alpha smooth muscle actin (α-SMA) within fibroblasts. With diabetic wound mice, the data demonstrated IGLR activated the NRF2/KEAP1 signaling and the downstream targets of the pathway, inhibited COX2/PEG2 signaling and decreased the interaction inflammatory targets of the axis, like interleukin-1beta (IL-1β), interleukin 6 (IL-6), apoptosis-associated speck-like protein (ASC), cysteinyl aspartate specific proteinase1 (caspase1) and NOD-like receptor-containing protein 3 (NLRP3).In addition, the deposition of COL1A1, and the level of α-SMA, and Transforming growth factor-β1 (TGF-β1) obviously elevated, whereas that of pro-inflammatory factors reduced in the diabetic wound tissue with IGLR treatment. Conclusion IGLR suppressed oxidative distress and inflammation mainly through NRF2/COX2 axis, thus promoting paracrine and accelerating wound healing in diabetes mice. Graphical Abstract
研究领域:
药理学
·
分子生物学
·
传统医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Jianhao Xie,Juan Su,Wanqi Zhou,Simin Cai,Wenfeng Liao,Jianing Zong,Junfeng Peng,Huanhuan Qu,Fei He,Kan Ding
Pancreatic ductal adenocarcinoma (PDAC) is a highly malignant cancer with limited treatment options. Recent pharmacological studies suggested that Lamiophlomis rotata might contain components with antitumor activities. In this study, we aimed to investigate the potential of polysaccharides as active components in Lamiophlomis rotata . Our findings suggest that a polysaccharide, LRP01B, from Lamiophlomis rotata induces PDAC cells apoptosis by causing mitochondrial dysfunction and oxidative stress in vitro and in vivo . LRP01B is a homogeneous polysaccharide with a molecular weight of 15.9 kDa, composed of galactose, glucose, xylose, arabinose, rhamnose, and galacturonic acid in a molar ratio of 0.7: 0.3: 0.1: 1.1: 1.0: 4.3. The backbone of LRP01B mainly consists of 1,4-linked α-Gal p A, 1,2-linked α-Rha p , and 1,3-linked α-Gal p A, with existence of arabinose and xylose on the side chain. In vivo experiments demonstrate that LRP01B significantly inhibits pancreatic tumor growth in a patient-derived xenograft nude mouse model. Mechanism studies uncover that LRP01B induces apoptosis of PDAC cells through mitochondrial dysfunction and oxidative stress by recruiting TNF-related apoptosis-inducing ligand (TRAIL) to TRAIL-R1, which leads to the binding of LRP01B to both TRAIL and TRAIL-R1. Our results demonstrate that LRP01B is a dual-targeting polysaccharide with anti-PDAC activity and may be a promising anti-PDAC drug candidate.
研究领域:
癌症生物学
·
药理学
·
生物化学
·
分子生物学
·
药物化学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2023
·
IF 5.4
Lei Lei,Guoguo Wan,Xiaoyu Geng,Jianguo Sun,Yi Zhang,Jianwei Wang,Congwen Yang,Zheng Pan
Ethnopharmacological relevance Lamiophlomis rotata (Benth.) Kudo ( L . rotata ), a Tibetan medicinal plant , is used to treat “yellow-water diseases”, such as skin disease, jaundice and rheumatism . Our previous study showed that the iridoid glycoside extract of L. rotata (IGLR) is the major constituent of skin wound healing. However, the role of IGLR in the biological process of trauma repair and the probable mechanism of the action remain largely unknown. Aim of the study To investigate the role of IGLR in the biological process of trauma repair and the probable mechanism of the action. Materials and methods The role of IGLR in wound healing was investigated by overall skin wound in mice with Hematoxylin and Eosin (H&E) and Masson trichrome staining. The anti-inflammatory, angiogenesis-promoting and fibril formation effects of IGLR were visualized in wound skin tissue by immunofluorescence staining, and the proinflammatory factors and growth factors were assayed by real-time polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay (ELISA). Macrophages, dermal fibroblasts, and endothelial cells were cultured to measure the direct/indirect interaction effects of IGLR on the proliferation and migration of cells, and flow cytometry was employed to assess the role of IGLR on macrophage phenotype. Network pharmacology combined with Western blot experiments were conducted to explore possible mechanisms of the actions. Results IGLR increased the expression of CD206 (M2 markers) through the RAS/p38 MAPK/NF-κB signaling pathway during wound injury in vivo and in vitro . IGLR suppressed the inflammatory cytokines iNOS, IL-1β and TNF-α in the early stage of wound healing . During the proliferation step of wound repair, IGLR promoted angiogenesis and fibril formation by increasing the expression of VEGF, CD31, TGF-β and α-SMA in wound tissue, and similar results were verified by RT-PCR and ELISA. In a paracrine mechanism, the extract promoted the proliferation of dermal fibroblasts, and endothelial cells were founded by the conditioned medium (CM). Conclusion IGLR induced M2 macrophage polarization in the early stage of wound healing; in turn, IGLR played a key role in the transition from inflammation to cell proliferation during the biological process of wound healing.
研究领域:
药理学
·
免疫学
·
伤口愈合
·
植物科学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2023
·
IF 5.4
Hupo Zhan,Ruixin Chen,Mei Zhong,Guowei Wang,Guihua Jiang,Xingbao Tao,Min Chen,Yunbin Jiang
Ethnopharmacological relevance Lamiophlomis rotata (Benth.) Kudo (LR, Lamiaceae) is a traditional Tibetan medicinal material in China. Tibetan medicine classic and research report suggested that LR could be used to cure rheumatoid arthritis (RA). However, the anti-RA active ingredients and pharmacological mechanisms of LR have not been elucidated. Aim of the study To explore the mechanisms and key active ingredients of total flavonoids from LR (TFLR) against RA. Materials and methods First, the mechanisms of TFLR against RA were investigated on collagen-induced arthritis (CIA) rat model by analyzing paw appearance, paw swelling, arthritis score, spleen index, thymus index, inflammatory cytokine (TNF-α, IL-1β, IL-6 and IL-17) levels in serum, histopathology of ankle joint and synovium from knee joint (hematoxylin-eosin, safranin O-fast green and DAB-TUNEL staining), and apoptosis-related protein (PI3K, Akt1, p-Akt, Bad, p-Bad, Bcl-xL and Bcl-2) levels in the synovium of ankle joints (Western blot). Then, the crucially active ingredients of TFLR against RA were explored by network pharmacology , ingredient analysis, in vitro metabolism and TNF-α-induced human RA synovial fibroblast MH7A proliferation assays. Network pharmacology was applied to predict the key active ingredients of TFLR against RA. The ingredient analysis and in vitro metabolism of TFLR were performed on HPLC, and MH7A proliferation assay were applied to evaluate the predicted results of network pharmacology. Results TFLR shown excellently anti-RA effect by reducing paw swelling, arthritis score, spleen index, thymus index and inflammatory cytokine (IL-1β, IL-6 and IL-17) levels, and improving the histopathological changes of ankle joint and synovium from knee joint in CIA rats. Results of Western blot indicated that TFLR reversed the changes of PI3K, p-Akt, p-Bad, Bcl-xL and Bcl-2 levels in the ankle joint synovium of CIA rats. Results of network pharmacology exhibited that luteolin was identified as the pivotal active ingredient of TFLR against RA. The ingredient analysis of TFLR indicated that the main ingredient in TFLR was luteoloside . The in vitro metabolism study of TFLR suggested that luteoloside could be converted to luteolin in artificial gastric juice and intestinal juice. Results of MH7A proliferation assay showed that there was no significant difference between TFLR and equal luteoloside on the viability of MH7A cells, indicating that luteoloside was the key active ingredient of TFLR against RA. Additionally, the luteolin (same mol as luteoloside) showed better inhibitory effect on the viability of MH7A cells than luteoloside. Conclusion TFLR showed anti-RA effect, and the mechanism was related to promoting synovial cell apoptosis mediated by PI3K/Akt/Bad pathway. Meanwhile, this work indicated that luteoloside was the key active ingredient of TFLR against RA. This work lays a foundation for providing TFLR product with clear mechanism and stable quality to treat RA.
研究领域:
药理学
·
民族药理学
·
网络药理学
·
炎症
·
风湿病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）