RESUMO
Lappanolides A-N (1-14), 14 undescribed sesquiterpenoids, along with 23 known ones (15-37), were isolated from the roots of Saussurea costus, which were primarily categorized into eudesmane, guaiane, and germacrane types. Lappanolide A (1) possessed an unprecedented pseudo-disesquiterpenoids. Their structures and absolute configurations were established using physical data analyses (HRESIMS, IR, 1D and 2D NMR) and ECD calculations. All isolated compounds were tested for anti-hepatitis B virus (anti-HBV) activity. Ten compounds (1, 9, 11, 12, 19, 22, 28, 29, 31, and 36) exhibited activities against HBsAg secretions as determined by ELISA assay, with IC50 values ranging from 5.2 to 45.7 µM. In particular, compounds 28 and 29 showed inhibition of HBsAg secretion with IC50 values of 5.28 and 5.30 µM, and CC50 values of 9.85 and 6.37 µM, respectively, though they all exhibited low selectivity. Several compounds displayed cytotoxicity in the MTT assay. Among them, compound 28 was the most notable and was chosen for further study using flow cytometry. The result showed that it significantly induced HepG2 cell arrest in the S phase and induced apoptosis.
Assuntos
Antivirais , Vírus da Hepatite B , Saussurea , Sesquiterpenos , Saussurea/química , Humanos , Vírus da Hepatite B/efeitos dos fármacos , Antivirais/farmacologia , Antivirais/química , Antivirais/isolamento & purificação , Sesquiterpenos/farmacologia , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Células Hep G2 , Estrutura Molecular , Antígenos de Superfície da Hepatite B/metabolismo , Antígenos de Superfície da Hepatite B/efeitos dos fármacos , Relação Estrutura-Atividade , Raízes de Plantas/química , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Apoptose/efeitos dos fármacosRESUMO
Saussurea lappa (Asteraceae family), a traditional Chinese medicine, has been found to possess anti-inflammatory, immune-promoting, antibacterial, antitumor, anti-HBV, cholestatic, and hepatoprotective activities. Herein, two undescribed amino acid-sesquiterpene lactone adducts, saussureamines G and H (1 and 2), and two new sesquiterpene glycosides, saussunosids F and G (3 and 4), along with 26 known sesquiterpenoids (5-30) have been isolated from the roots of S. lappa. Their structures and absolute configurations of these compounds were established by physical data analyses such as HRESIMS, IR, 1D and 2D NMR and ECD calculations. All isolated compounds were tested for anti-hepatitis B virus (anti-HBV) activity. Ten compounds (5, 6, 12, 13, 17, 19, 23, 26, 29, and 30) exhibited activities against the secretions of HBsAg and HBeAg. In particular, compound 6 showed inhibition of HBsAg and HBeAg secretion with IC50 values of 11.24 and 15.12 µM, with SI values of 1.25 and 0.93, respectively. Molecular docking studies were also conducted on the anti-HBV compounds. Overall, this study provides insights into the potential therapeutic uses of the compounds found in the roots of S. lappa, particularly in the treatment of hepatitis B virus infections.
Assuntos
Saussurea , Sesquiterpenos , Saussurea/química , Vírus da Hepatite B , Antígenos de Superfície da Hepatite B , Aminoácidos , Glicosídeos , Antígenos E da Hepatite B , Simulação de Acoplamento Molecular , Estrutura Molecular , LactonasRESUMO
INTRODUCTION: Surgical management is commonly used for thyroid cancer. We evaluated the effects of systemic lidocaine versus dexmedetomidine on the recovery quality and analgesia after thyroid cancer surgery. METHODS: A total of 120 patients with thyroid cancer were randomly allocated to group L (received lidocaine 1.5 mg/kg loading, continuously infused 1.5 mg/kg per hour), group D (received dexmedetomidine 0.5 µg/kg loading, continuously infused 0.5 µg/kg per hour) and group C (received normal saline), with 40 cases in each group. Anaesthesia induction and maintenance were performed using target-controlled infusions (TCIs) of propofol and remifentanil. The primary outcome of the quality of recovery-15 (QoR-15) score was recorded on the day before surgery and postoperative day 1 (POD1). Secondary outcomes included the consumption of remifentanil during surgery, time to first required rescue analgesia, number of patients requiring rescue analgesia, postoperative cumulative consumption of tramadol, visual analogue scale (VAS) pain score, incidence of postoperative nausea or vomiting (PONV) and side effects. RESULTS: The total score of the QoR-15 at POD1 (median, IQR) was higher in group L (128.0, 122.0-132.8) and group D (127.5, 122.5-132.5) compared to group C (118.5, 113.0-123.5) (P = 0.000). Compared to group C, systemic lidocaine and dexmedetomidine reduced cumulative consumption of remifentanil and VAS pain score (P = 0.000). The time to first required rescue analgesia (mean, SD) was longer in group L (8.1 h, 1.2 h) and group D (8.5 h, 1.9 h) than group C (5.9 h, 0.9 h) (P = 0.000). The number of patients requiring rescue analgesia was lower in group L (8/40, 20%) and group D (6/40, 15%) than group C (16/40, 40%) (P = 0.029), and cumulative consumption of tramadol (mean, SD) was lower in group L (44.0 mg, 17.1 mg) and group D (51.7 mg, 14.1 mg) than group C (73.9 mg, 18.4 mg) (P = 0.000). The incidence of PONV in group L (7/40, 17.5%) and group D (9/40, 22.5%) was lower than group C (18/40, 45.0%) (P = 0.016). Bradycardia (heart rate less than 50 beats/min or lower) was noted in 25 patients (25/40, 62.5%), which was reversed by intravenous administration of atropine 0.5 mg. CONCLUSION: Systemic lidocaine and dexmedetomidine had similar effects on enhancing the quality of recovery, alleviating the intensity of pain and reducing the incidence of PONV after thyroid cancer surgery. However, dexmedetomidine may result in bradycardia. Therefore, lidocaine was superior to dexmedetomidine. TRIAL REGISTRATION: ChiCTR.org.cn (ChiCTR2000038442). Registered on September 22, 2020.
RESUMO
BACKGROUND: Parathyroidectomy has been proposed as a method for reducing parathyroid hormone levels. We evaluated the effects of ultrasound-guided bilateral superficial cervical plexus block (BSCPB) on the quality of recovery of uremia patients with secondary hyperparathyroidism (SHPT) following parathyroidectomy. METHODS: Eighty-two uremia patients who underwent parathyroidectomy and exhibited SHPT were randomly allocated to the BSCPB group or the control group (CON group). The patients received ultrasound-guided BSCPB with 7.5 ml of ropivacaine 0.5% on each side (BSCPB group) or equal amount of 0.9% normal saline (CON group). The primary outcome of the Quality of Recovery-40(QoR-40) score was recorded on the day before surgery and postoperative day 1(POD1). Secondary outcomes including total consumption of remifentanil, time to first required rescue analgesia, number of patients requiring rescue analgesia, and total consumption of tramadol during the first 24 h after surgery were recorded. The occurrence of postoperative nausea or vomiting (PONV) and the visual analogue scale (VAS) scores were assessed and recorded. RESULTS: The scores on the pain and emotional state dimensions of the QoR-40 and the total QoR-40 score were higher in the BSCPB group than in the CON group on POD1 (P = 0.000). Compared with the CON group, the total consumption of remifentanil was significantly decreased in the BSCPB group (P = 0.000). The BSCPB group exhibited longer time to first required rescue analgesia (P = 0.018), fewer patients requiring rescue analgesia (P = 0.000), and lower postoperative total consumption of tramadol during the first 24 h after surgery (P = 0.000) than the CON group. The incidence of PONV was significantly lower in the BSCPB group than in the CON group (P = 0.013). The VAS scores in the BSCPB group were lower than those in the CON group at all time-points after surgery (P = 0.000). CONCLUSION: Ultrasound-guided BSCPB with ropivacaine 0.5% can enhance the quality of recovery, postoperative analgesia, and reduce the incidence of PONV in uremia patients with SHPT following parathyroidectomy. TRIAL REGISTRATION: ChiCTR1900027185 . (Prospective registered). Initial registration date was 04/11/2019.
Assuntos
Bloqueio do Plexo Cervical/métodos , Hiperparatireoidismo Secundário/epidemiologia , Dor Pós-Operatória/epidemiologia , Paratireoidectomia/métodos , Náusea e Vômito Pós-Operatórios/epidemiologia , Ultrassonografia de Intervenção/métodos , Uremia/epidemiologia , China/epidemiologia , Comorbidade , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos ProspectivosRESUMO
Primary hyperparathyroidism in children and adolescents is rare and often symptomatic at presentation. A 15-year-old bo presented with bilateral genu valgum for two years. Biochemical results were consistent with primary hyperparathyroidism Calcium levels normalized two months after removal of a left inferior parathyroid adenoma.
RESUMO
Co-existence of craniopharyngioma and acromegaly has been very rarely reported. A 65-year-old man presented with visual deterioration, fatigue and frontal headaches. Magnetic resonance imaging revealed a suprasellar heterogeneous, mainly cystic, 1.9 × 2 × 1.9 cm mass compressing the optic chiasm and expanding to the third ventricle; the findings were consistent with a craniopharyngioma. Pituitary hormone profile showed hypogonadotropic hypogonadism, mildly elevated prolactin, increased insulin-like growth factor 1 (IGF-1) and normal thyroid function and cortisol reserve. The patient had transsphenoidal surgery and pathology of the specimen was diagnostic of adamantinomatous craniopharyngioma. Post-operatively, he had diabetes insipidus, hypogonadotropic hypogonadism and adrenocorticotropic hormone and thyroid-stimulating hormone deficiency. Despite the hypopituitarism, his IGF-1 levels remained elevated and subsequent oral glucose tolerance test did not show complete growth hormone (GH) suppression. Further review of the pre-operative imaging revealed a 12 × 4 mm pituitary adenoma close to the right carotid artery and no signs of pituitary hyperplasia. At that time, he was also diagnosed with squamous cell carcinoma of the left upper lung lobe finally managed with radical radiotherapy. Treatment with long-acting somatostatin analogue was initiated leading to biochemical control of the acromegaly. Latest imaging has shown no evidence of craniopharyngioma regrowth and stable adenoma. This is a unique case report of co-existence of craniopharyngioma, acromegaly and squamous lung cell carcinoma that highlights diagnostic and management challenges. Potential effects of the GH hypersecretion on the co-existent tumours of this patient are also briefly discussed. LEARNING POINTS: Although an extremely rare clinical scenario, craniopharyngioma and acromegaly can co-exist; aetiopathogenic link between these two conditions is unlikely.Meticulous review of unexpected biochemical findings is vital for correct diagnosis of dual pituitary pathology.The potential adverse impact of GH excess due to acromegaly in a patient with craniopharyngioma (and other neoplasm) mandates adequate biochemical control of the GH hypersecretion.