Assessment of the anti-inflammatory effects of three rhubarb anthraquinones in LPS-Stimulated RAW264.7 macrophages using a pharmacodynamic model and evaluation of the structure-activity relationships.

ETHNOPHARMACOLOGICAL RELEVANCE: Rhubarb (Rhei Radix et Rhizoma) is a traditional Chinese medicine, has been used as a strong astringent in China to treat inflammation-related diseases, such as acute pancreatitis, acute cholecystitis, appendicitis and so on. Rhein, emodin and aloe-emodin are the important active anthraquinone in rhubarb, and are considered to be the main ingredients contributing to anti-inflammatory. AIM OF THE STUDY: Rhein, emodin and aloe-emodin, anthraquinones with the same parent structure that are found in rhubarb, have beneficial anti-inflammatory effects in vitro and in vivo. Anthraquinone derivatives also have important clinical roles. However, their pharmacodynamic differences and the structure-activity relationships associated with their anti-inflammatory properties have not been systematically explored. The present study was designed to quantify the effects of three rhubarb anthraquinones on inflammation and to explore the structure-activity relationships of these compounds. MATERIALS AND METHODS: In this study, we detected NF-κB phosphorylation, iNOS protein expression, and IL-6 and NO production in LPS-stimulated RAW264.7 cells and then calculated median effect equations and built a dynamic pharmacodynamic model to quantitatively evaluate the efficacy of these three anthraquinones. Additionally, to determine the structure-activity relationships, we investigated the physicochemical properties and molecular electrostatic potentials of the drug molecules. RESULTS: We found that rhein, emodin, and aloe-emodin exerted at least dual-target (NF-κB, iNOS) inhibition of LPS-induced inflammatory responses. Compared with rhein and emodin, aloe-emodin had a stronger anti-inflammatory effect, and its inhibition of iNOS protein expression was approximately twice that of NF-κB phosphorylation. In addition, aloe-emodin had the strongest hydrophobic effect among the three anthraquinones. CONCLUSIONS: Overall, we concluded that the receptor binding the rhubarb anthraquinones had a hydrophobic pocket. Anthraquinone molecules with stronger hydrophobic effects had higher affinity for the receptor, resulting in greater anti-inflammatory activity. These results suggest that the addition of a hydrophobic group is a potential method for structural modification to design anti-inflammatory anthraquinone derivatives with enhanced potency.

Cancer pain management at home: voice from an underdeveloped region of China.

BACKGROUND: Pain is a major problem for patients with advanced cancer and one of the most frequent and disturbing of all cancer-related symptoms. Researchers continue to report that cancer pain remains undertreated. Inadequate pain control can significantly affect the patient's quality of life and may in turn affect the patient's will to live or comply with treatment recommendations. A better understanding of the experience of cancer pain management is important in identifying factors responsible for undertreated pain. OBJECTIVE: This study aimed to obtain the experience of cancer pain management. INTERVENTIONS: We used a phenomenological approach to explore the status of cancer pain management through participants' experience. Semistructured interviews were conducted with 14 family caregivers, patients, and acquaintances and 14 health professionals (nurses and physicians) from a regional tertiary hospital in northwest China. Data were collected by in-depth interviews. We used a qualitative description after full transcription of every interview. Analysis involved the identification of themes and the development of a taxonomy of participants' experience of cancer pain management. RESULTS: Taxonomy used in this study is to identify, code, group, and name meaning units of the transcribed interviews by reading through repeatedly to obtain an initial sense. Four themes were identified: (1) marginalization, (2) hopelessness and helplessness, (3) deficiency of access and resources, and (4) expectations related to pain. CONCLUSION: Findings from this study suggest that the situation of patients with undertreated cancer pain continues. IMPLICATIONS FOR PRACTICE: Special attention should be paid by policymakers, professionals, and family caregivers to the marginalized group of cancer patients who suffer with pain.