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Carotenoids: Potent to Prevent Diseases Review
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Takshma Bhatt, Kirtan Patel
Natural Products and Bioprospecting. 2020, 10 (3): 109-117.
DOI: 10.1007/s13659-020-00244-2
Carotenoids are the phytochemicals known for their biological activities. They are found in nature in the form of plants, algae, fungi and in microorganisms. This is the major group having two different structure one with oxygen and without oxygen. The Present article aims to present these molecules as a new therapeutic agent, as it has unrealized efficiency to prevent and reduce the symptoms of many diseases like cancer, neurodegenerative diseases such as Alzheimer, cerebral ischemia, diabetes associated with obesity and hypertension, ophthalmic diseases and many more. It can be utilized in the form of dietary supplement as nutraceutical and pharmaceutical compounds. Yet more research and developing test knowledge is needed to make it available to the humans. In this article its sources, biosynthesis, properties, applicability and commercialization of pigments from naturally produced sources are discussed.
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Genotoxicity and Safety Pharmacology Studies of Indole Alkaloids Extract from Leaves of Alstonia scholaris (L.) R. Br.
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Yun-Li Zhao, Min Su, Jian-Hua Shang, Xia Wang, Guang-Lei Bao, Jia Ma, Qing-Di Sun, Fang Yuan, Jing-Kun Wang, Xiao-Dong Luo
Natural Products and Bioprospecting. 2020, 10 (3): 119-129.
DOI: 10.1007/s13659-020-00242-4
Indole alkaloids extract (IAAS) was prepared from leaves of Alstonia scholaris (L.) R. Br., an evergreen tropical plant widely distributed throughout the world. This plant has been used historically by the Dai ethnic people of China to treat respiratory diseases. This study evaluated the genotoxicity and safety pharmacology of IAAS to support clinical use. The bacterial reverse mutation (Ames) test, in vitro mammalian chromosomal aberration test, and in vivo mammalian erythrocyte micronucleus (MN) test were performed to evaluate genotoxicity. Mice were administered IAAS (240, 480, or 960 mg/kg bw) once orally to observe adverse central nervous system effects. Furthermore, beagle dogs were administered IAAS (10, 30, 60 mg/kg bw) once via the duodenum to evaluate its effects on the cardiovascular and respiratory systems. IAAS with or without S9-induced metabolic activation showed no genotoxicity in the Ames test up to 500 μg/plate, in the mammalian chromosomal aberration test up to 710 μg/mL, or in the MN test up to 800 mg/kg bw. No abnormal neurobehavioral effects were observed in mice following treatment with up to 960 mg/kg bw of IAAS. Moreover, blood pressure, heart rate, electrocardiogram parameters, and depth and rate of breathing in anesthetized beagle dogs did not differ among the IAAS doses or from the vehicle group. These data indicated that IAAS did not induce mutagenicity, clastogenicity, or genotoxicity, and no pharmaco-toxicological effects were observed in the respiratory, cardiovascular, or central nervous systems. Our results increased understanding of safety considerations associated with IAAS, and may indicate that IAAS is a possible drug candidate.
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Eriocalyxin B Inhibits Adipogenesis in 3T3-L1 Adipocytes by Cell Cycle Arrest
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Rong-Fang Mu, Yan-Fen Niu, Qian Wang, Hui-Min Zhou, Jing Hu, Wan-Ying Qin, Wen-Yong Xiong
Natural Products and Bioprospecting. 2020, 10 (3): 131-140.
DOI: 10.1007/s13659-020-00240-6
Eriocalyxin B, an ent-Kaurene diterpenoid extracted from a traditional Chinese herb Isodon eriocalyx, has been shown to possess multifunctional activities such as anti-cancer and anti-inflammatory. However, the function and mechanism of the compound in adipocyte differentiation is still unknown. Here we reported that eriocalyxin B blunted adipogenesis remarkably by inhibiting the accumulation of lipid droplets, triglycerides and the expressions of adipogenesis-related factors, including C/EBPβ, C/EBPα, PPARγ, and FABP4. Moreover, we showed that the inhibition might be the consequence of cell cycle being arrested at the G2/M phase during the mitotic clonal expansion of adipocyte differentiation, most likely by suppressing mRNAs and proteins of CDK1, CDK2, Cyclin A and Cyclin B1. Overall, we conclude that eriocalyxin B is capable of inhibiting adipocyte differentiation at the early stage through downregulating the proteins involved in cell cycle progression.
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Analysis of Four Solvatomorphs of Betulin by TG-DTA-EI/PI-MS System Equipped with the Skimmer-Type Interface
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Peng-Hui Yuan, Yan-Cai Bi, Bin Su, De-Zhi Yang, Ning-Bo Gong, Li Zhang, Yang Lu, Guan-Hua Du
Natural Products and Bioprospecting. 2020, 10 (3): 141-152.
DOI: 10.1007/s13659-020-00243-3
Betulin (BE) has exceedingly become a potential natural product, providing multiple pharmacological and biological activities, including anti-cancer, anti-viral, and anti-inflammatory benefits. Previous research indicated that the solvatomorphism of BE can easily occur through crystallization with different organic solvents. This property of BE can directly affect its extraction, isolation, and preparation process. In this study, a system of thermogravimetry (TG)-differential thermal analysis (DTA) coupled with mass spectrometry (MS) with electron ionization (EI) and photoionization (PI) capability, equipped with the skimmer-type interface (i.e., skimmer-type interfaced TG-DTA-EI/PI-MS system), as a real-time and onsite analysis technique, was employed. Then, four solvatomorphs of BE, namely, with pyridine and water (A), sec-butanol (B), n,n-dimethylformamide (DMF) (C), and isopropanol (V), were analyzed for the first time. Finally, five kinds of the main volatile gaseous species, including H2O, pyridine, sec-butanol, DMF, and isopropanol, were identified clearly. Furthermore, the multi-step desolvation processes of the four solvatomorphs of BE were revealed by this system for the first time. This system showed great potential for the rapid and accurate analysis of various solvatomorphs of natural products.
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Cucurbitane-Type Triterpene Glycosides from Momordica charantia and Their α-Glucosidase Inhibitory Activities
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Ya Gao, Jian-Chao Chen, Xing-Rong Peng, Zhong-Rong Li, Hai-Guo Su, Ming-Hua Qiu
Natural Products and Bioprospecting. 2020, 10 (3): 153-161.
DOI: 10.1007/s13659-020-00241-5
Ten cucurbitane-type triterpene glycosides, including five new compounds named charantosides H (1), J (2), K (3), momorcharacoside A (4), goyaglycoside-L (5), and five known compounds (6-10), were isolated from the EtOAc extract of Momordica charantia fruits. The chemical structures of these compounds were identified by 1D and 2D NMR and HRESIMS spectroscopic analyses. Configurations of new compounds were determined by ROESY correlations and comparison of their 13C NMR data with literature reported values. All compounds were evaluated for their inhibition against α-glucosidase, in which compounds 2, 5, 7, 8, 9 showed moderate inhibitory activities with IC50 values ranging from 28.40 to 63.26 μM comparing with the positive control (acarbose, IC50 87.65±6.51 μM).
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Adipogenesis Inhibitory Activity of Hypersampsone P from Hypericum subsessile
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Hui-Min Zhou, Yan-Song Ye, Na-Na Jiang, Rong-Fang Mu, Qian Wang, Jing Hu, Xia Liu, Wan-Ying Qin, Gang Xu, Wen-Yong Xiong
Natural Products and Bioprospecting. 2020, 10 (3): 163-170.
DOI: 10.1007/s13659-020-00245-1
Adamantane polycyclic polyprenylated acylphloroglucinols (PPAPs) with caged architecture, a special class of hybrid natural products, is specifically rich in the plant family Guttiferae, especially Hypericum or Garcinia genus. Hypersampsone P is one of Adamantane PPAPs compounds extracted from Hypericum subsessile. Here we have chosen, screened ten PPAPs and identified one of them showed an activity in inhibiting of adipocytes differentiation. Particularly, the compound, hypersampsone P, blunted the adipocyte differentiation dose-dependently. Moreover, hypersampsone P down-regulated the expressions of several key regulators for adipogenesis, including PPARγ and FABP4. The treatment of cells at the early stage of adipogenesis by hypersampsone P induced the greatest blunting of adipocyte differentiation and the effect might be involved in the LKB1-AMPK signaling pathway.
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