Aloperine improves osteoporosis in ovariectomized mice by inhibiting RANKL-induced NF-κB, ERK and JNK approaches.

Presently, postmenopausal osteoporosis mainly caused by excessive activation of in vivo osteoclasts has become a global public health burden. Natural compounds have gradually become the potential drugs for the treatment of postmenopausal osteoporosis. Aloperine is a new alkaloid extracted from the leaves and seeds of sophora bean. The current studies have proved that aloperine has many biological activities, including anti-inflammatory, antiviral and anticancer activities. This study shows that aloperine can inhibit activity and formation of osteoclast mediated by RANKL in a dose-dependent manner without affecting the activity of bone marrow macrophages (BMM). In addition, it is found that aloperine can inhibit the expression of osteoclast specific marker genes, including nuclear factor of activated T cells cytoplasmic 1 (NFATc1), tartrate resistant acid phosphatase (TRAcP), matrix metallopeptidase 9 (MMP9), cathepsin K (Ctsk), V-ATPase d2 and calcitonin receptor. The in vitro experiment of aloperine proved that aloperine can inhibit the degradation of IκBα and the phosphorylation of P65, ERK and JNK. Additionally, aloperine improves bone loss in ovariectomized (OVX) mice by inhibiting osteoclast activity. This project proved that aloperine can affect the formation of osteoclasts by inhibiting RANKL signaling channel, and it is indicated that aloperine has the potential to be developed as a new drug for the prevention and treatment of postmenopausal osteoporosis.

Phytochemical Information and Biological Activities of Quinolizidine Alkaloids in Sophora: A Comprehensive Review.

Quinolizidine alkaloids, a main form of alkaloids found in the genus Sophora, have been shown to have many pharmacological effects. This review aims to summarize the photochemical reports and biological activities of quinolizidine alkaloids in Sophora. The collected information suggested that a total of 99 quinolizidine alkaloids were isolated and detected from different parts of Sophora plants, represented by lupinine-type, cytisine-type, sparteine-type, and matrine-type. However, quality control needs to be monitored because it could provide basic information for the reasonable and efficient use of quinolizidine alkaloids as medicines and raw materials. The nonmedicinal parts may be promising to be used as a source of quinolizidine alkaloid raw materials and to reduce the waste of resources and environmental pollution. In addition, the diversity of chemical compounds based on the alkaloid scaffold to make a biological compound library needs to be extended, which may reduce toxicity and find new bioactivities of quinolizidine alkaloids. The bioactivities most reported are in the fields of antitumor activity along with the effects on the cardiovascular system. However, those studies rely on theoretical research, and novel drugs based on quinolizidine alkaloids are expected.

Enhanced ultrasound-assisted enzymatic hydrolysis extraction of quinolizidine alkaloids from Sophora alopecuroides L. seeds.

Quinolizidine alkaloids are the main bioactive components in Sophora alopecuroides L. This study reports a novel ultrasound-assisted enzymatic hydrolysis method for the extraction of these important alkaloids. Box-Behnken design, a widely used response surface methodology, was used to investigate the effects of process variables on ultrasound bath-assisted enzymatic hydrolysis (UAEH) extraction. Four independent variables, pH, extraction temperature (°C), extraction time (min) and solvent-to-material ratio (mL/g), were studied. For the extraction of sophocarpine, oxysophocarpine, oxymatrine, matrine, sophoramine, sophoridine and cytisine, the optimal UAEH condition was found to be a pH of 5, extraction temperature of 54 °C, extraction time of 60 min and solvent-to-material ratio of 112 mL/g. The experimental values obtained under optimal conditions were fairly consistent with the predicted values. UAEH extraction was then compared with reflux heating, enzymatic extraction and ultrasound-assisted extraction. Of these extraction methods, UAEH extraction under optimal conditions produced the highest yield for seven types of alkaloids. In addition, UAEH extraction resulted in lower ingredient degradation than reflux heating extraction.

Indolo[2,3-a]quinolizidines and Derivatives: Bioactivity and Asymmetric Synthesis.

Corynantheine alkaloids with a tetracyclic indole[2,3-a]-quinolizidine motif are an important issue in academia and in the life science industries due to their broad bioactivity profile. In particular, the main biological effects described for indoloquinolizidines include analgesic, anti-inflammatory, antihypertensive, and antiarrhythmic activities, as well as inhibition of multiple ion channels, affinity for opioid receptors, and activity against Leishmania. For that reason, in the last decades, numerous efforts have been invested in the development of novel synthetic strategies to obtain the indole[2,3-a]-quinolizidine system. This review focuses on the synthetic methodologies developed to target the most important alkaloids of this family, and highlights the potential use of these alkaloids or analogs to treat several diseases, ranging from cancer to neurodegenerative disorders.

Cytotoxic alkaloids from Boehmeria siamensis.

Two new phenanthroquinolizidine alkaloids, boehmeriasins A and B, were isolated from the aqueous ethanolic extract of Boehmeria siamensis Craib (Urticaceae) by bioassay-guided fractionation. Their structures were elucidated on the basis of spectral evidence. Boehmeriasin A possesses cytotoxic activity against 12 cell lines from 6 panels of cancer including lung cancer, colon cancer, breast cancer, prostate cancer, kidney cancer and leukemia with GI (50) between 0.2 and 100 ng/mL, whereas boehmeriasin B showed lower activity.