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1.
J Am Chem Soc ; 145(20): 10998-11004, 2023 May 24.
Article in English | MEDLINE | ID: mdl-37167083

ABSTRACT

The first total synthesis of (±)- and (-)-daphnillonin B, a daphnicyclidin-type alkaloid with a new [7-6-5-7-5-5] A/B/C/D/E/F hexacyclic core, has been achieved. The [6-5-7] B/C/D ring system was efficiently and diastereoselectively constructed via a mild type I intramolecular [5+2] cycloaddition, followed by a Grubbs II catalyst-catalyzed radical cyclization. The [5-5] fused E/F ring system was synthesized via a diastereoselective intramolecular Pauson-Khand reaction. Notably, the synthetically challenging [7-6-5-7-5-5] hexacyclic core was reassembled by a unique Wagner-Meerwein-type rearrangement from the [6-6-5-7-5-5] hexacyclic framework found in calyciphylline A-type Daphniphyllum alkaloids.

2.
Chem Rev ; 123(8): 4934-4971, 2023 04 26.
Article in English | MEDLINE | ID: mdl-36917457

ABSTRACT

Taxol (paclitaxel), the most well-known taxane diterpenoid, is the best-selling natural-source anticancer drug ever produced and one of the most common prescriptions in the treatment of breast, lung, and ovarian cancers, saving countless lives around the world. Structurally, Taxol possesses a highly oxygenated [6-8-6-4] core bearing 11 stereocenters, seven of which are contiguous chiral centers. Moreover, the extremely strained bicyclo[5.3.1] undecane ring system with a bridgehead double bond is a unique structural feature. All these features make Taxol a highly challenging synthetic target. Tremendous synthetic efforts from more than 60 research groups around the world have already culminated in ten total syntheses and three formal syntheses, as well as more than 60 synthetic model studies of Taxol. This review is intended to provide a long-overdue appraisal of the great achievements in the total syntheses of Taxol reported in the last few decades. In doing so, we summarize the development of synthesis toward Taxol from 1994 to 2022, including the evolution of synthetic strategy for accessing this complex molecular scaffold and key lessons learned from such endeavors. Finally, we briefly discuss the future of the research in this area.


Subject(s)
Antineoplastic Agents , Paclitaxel , Paclitaxel/chemistry , Paclitaxel/therapeutic use
3.
Zhongguo Xiu Fu Chong Jian Wai Ke Za Zhi ; 31(3): 257-261, 2017 03 15.
Article in Chinese | MEDLINE | ID: mdl-29806250

ABSTRACT

Objective: To investigate the clinical efficacy of computer-assisted cannulated screw internal fixation system based on error correction method for femoral neck fractures. Methods: A retrospective analysis was made on the clinical data of 20 femoral neck fracture patients treated by computer-assisted cannulated screw internal fixation system based on error correction method between January 2014 and October 2015 (trial group), and 36 femoral neck fracture patients undergoing traditional manual surgery with closed reduction by cannulated screw fixation in the same period (the control group). There was no significant difference in gender, age, injury cause, side of fracture, types of fracture, and time from injury to operation between 2 groups ( P>0.05). The operation time, intraoperative blood loss, intraoperative frequency of fluoroscopy and guide pin insertion, fracture healing time, fracture healing rate, and Harris hip score were compared between 2 groups. Results: All incisions healed by first intention after operation, and no complication of blood vessel and nerve injury occurred. The operation time of trial group was significantly longer than that of control group ( t=2.290, P=0.026), however, the intraoperative blood loss, intraoperative frequency of fluoroscopy and guide pin insertion of trial group were significantly less than those of control group ( t=-10.650, P=0.000; t=18.320, P=0.000; t=-16.625, P=0.000). All patients were followed up 12-18 months (mean, 14.7 months). X-ray films showed that fracture healing was obtained in 2 groups, showing no significant difference in fracture healing time between 2 groups ( t=0.208, P=0.836). No complication of ischemic necrosis of femoral head occurred during follow-up period. At last follow-up, the Harris hip score was 87.05±3.12 in trial group and was 86.78±2.83 in control group, showing no significant difference ( t=0.333, P=0.741). Conclusion: Computer-assisted cannulated screw internal fixation surgery based on error correction method for femoral neck fractures is better than traditional manual surgery in decreasing intraoperative radiation and surgical trauma during operation.


Subject(s)
Bone Screws , Femoral Neck Fractures/surgery , Fracture Fixation, Internal , Fracture Healing , Humans , Retrospective Studies , Treatment Outcome
4.
J Pharm Biomed Anal ; 80: 24-33, 2013 Jun.
Article in English | MEDLINE | ID: mdl-23511229

ABSTRACT

SiJunZiTang (SJZT), a classic Traditional Chinese Formula (TCMF) consisting of four herbs, Radix Ginseng, Atractylodes macrocephala, Poria cocos and Glycyrrhiza uralensis, has been demonstrated to show protective effects on intestine and stomach injure. The chromatographic quality control is needed. UPLC-Q-TOF-MS is a rapid and efficient technique for analysis of complex sample in combination with UPLC and tandem mass spectrometry (MS/MS). In this paper, UPLC-MS fingerprinting of SJZT was developed. As a result, 66 compounds including ginsenosides, flavonoids, triterpenoid and coumarins were detected, 58 of them were tentatively identified. The major constituents of SJZT were ginsenosides and flavonoids that coming from Radix Ginseng and Glycyrrhiza uralensis.


Subject(s)
Chromatography, Liquid/methods , Drugs, Chinese Herbal/analysis , Tandem Mass Spectrometry/methods , Drugs, Chinese Herbal/chemistry , Medicine, Chinese Traditional/methods , Quality Control , Time Factors
5.
Sheng Wu Yi Xue Gong Cheng Xue Za Zhi ; 29(2): 212-6, 2012 Apr.
Article in Chinese | MEDLINE | ID: mdl-22616160

ABSTRACT

At present, ray-casting algorithm is the most widely used algorithm in the field of medical image visualization, and it can achieve the best image quality. Due to large amounts of computation like sampling, gradient, lighting and blending calculation, the cost of ray-casting algorithm is very large. The characteristic of Streaming single instruction multiple datum extensions (SSE) instruction--supporting vector computation--can satisfy the property of ray-casting algorithm well. Therefore, in this paper, we improved the implementation efficient significantly by vectorization of gradient, lighting and blending calculation, and still achieved a high quality image at the same time.


Subject(s)
Algorithms , Image Interpretation, Computer-Assisted/methods , Image Processing, Computer-Assisted/methods , Pattern Recognition, Automated/methods , Humans
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