The Experts below are selected from a list of 7101 Experts worldwide ranked by ideXlab platform
Simone Fulda - One of the best experts on this subject based on the ideXlab platform.
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Betulinic Acid for cancer treatment and prevention
International Journal of Molecular Sciences, 2008Co-Authors: Simone FuldaAbstract:Betulinic Acid is a natural product with a range of biological effects, for example potent antitumor activity. This anticancer property is linked to its ability to induce apoptotic cell death in cancer cells by triggering the mitochondrial pathway of apoptosis. In contrast to the cytotoxicity of Betulinic Acid against a variety of cancer types, normal cells and tissue are relatively resistant to Betulinic Acid, pointing to a therapeutic window. Compounds that exert a direct action on mitochondria present promising experimental cancer therapeutics, since they may trigger cell death under circumstances in which standard chemotherapeutics fail. Thus, mitochondrion-targeted agents such as Betulinic Acid hold great promise as a novel therapeutic strategy in the treatment of human cancers.
Yin Zhiqi - One of the best experts on this subject based on the ideXlab platform.
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Determination of Betulinic Acid in Semen Ziziphi Spinosae by HPLC
Pharmaceutical biotechnology, 2020Co-Authors: Yin ZhiqiAbstract:To establish a HPLC method for the determination of the content of Betulinic Acid in Semen Ziziphi Spinosae,the Alltech C18(4.6mm × 250mm,5μm)column was used with the acetonitrile:water containing 0.4% phosphoric Acid(85∶15) as mobile phase,with the flow rate at 1.0mL/min and UV detector at 205nm.The linear range of Betulinic Acid was 0.4462～6.693μg(r=0.9998).The average recovery of Betulinic Acid was 100.3%(RSD=1.7%).The method is simple and accurate,it can be used for the quality control of Betulinic Acid in Semen Ziziphi Spinosae.
Yang Guang - One of the best experts on this subject based on the ideXlab platform.
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HPLC determination of Betulinic Acid in Semen Ziziphi Spinosae
Chinese Journal of Pharmaceutical Analysis, 2020Co-Authors: Yang GuangAbstract:Objective:To establish an HPLC method for the determination of Betulinic Acid in Semen Ziziphi Spi- nosae.Method:The separation was achieved on a ALCHROM~(TM)Hyper Sil C_(18)column(250mm×4.6mm,5μm) at 25℃.The mobile phase composition was methanol-water-triethylamine-glacial acetic Acid(85:15:0.05: 0.03)with a flow rate of 0.8mL·min~(-1).The detection wavelength was 210nm.Result:The cahbration curves was linear in the rang of 0.8-4.0μg,r=0.9995 and the resolution of Betulinic Acid was more than 1.5.The recovery rate was 102.5%,RSD=2.0%.Conclusion:This method is sensitive,rapid and accurate with good reproducibility for quantitative analysis of Betulinic Acid in Semen Ziziphi Spinosae.
Anand C Burman - One of the best experts on this subject based on the ideXlab platform.
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synthesis and cytotoxic activity of heterocyclic ring substituted Betulinic Acid derivatives
Bioorganic & Medicinal Chemistry Letters, 2008Co-Authors: Vivek Kumar, Manu Jaggi, Nidhi Rani, Pawan Aggarwal, Vinod K Sanna, Anu T Singh, Narendra Shriram Joshi, Pramod Kumar Sharma, Raghuveer Irchhaiya, Anand C BurmanAbstract:Abstract A new series of Betulinic Acid derivatives have been synthesized by introducing heterocyclic ring between C-2 and C-3 positions of Betulinic Acid. Further modifications were also carried out by reduction of C-20(29) unsaturated bond and substitution of C-28 carboxyl group by ester and amide linkage to enhance the selectivity. Compound 11 resulted in IC 50 of 2.44, 2.5, and 2.7 μg / ml on MIAPaCa, PA-1, and SW620 cancer cell lines, respectively. Compound 38 resulted in IC 50 of 0.67 μg / ml on MIAPaCa cell line.
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Betulinic Acid derivatives as anticancer agents structure activity relationship
Anti-cancer Agents in Medicinal Chemistry, 2006Co-Authors: Rama Mukherjee, Vivek Kumar, Sanjay K Srivastava, Shiv K Agarwal, Anand C BurmanAbstract:Betulinic Acid, a pentacyclic triterpene, is widely distributed throughout the tropics. It possesses several biological properties such as anticancer, anti-inflammatory, antiviral, antiseptic, antimalarial, spermicidal, antimicrobial, antileshmanial, antihelmentic and antifeedent activities. However, Betulinic Acid was highly regarded for its anticancer and anti-HIV activities. Anticancer role of Betulinic Acid appeared by inducing apoptosis in cells irrespective of their p53 status. Due to high order safety in Betulinic Acid, a number of structural modifications carried out to improve its potency and efficacy. The C-1, C-2, C-3, C-4, C-20 and C-28 positions are the diversity centers in Betulinic Acid, and the derivatives resulted on various structural modifications at these positions screened for their anticancer activity. This review presents the structure activity relationship carried out on C-1, C-2, C-3, C-4, C-20, C-28, A-ring, D-ring and E-ring modified Betulinic Acid derivatives. We have compiled the most active Betulinic Acid derivatives along with their activity profile in each series. Structure activity relationship studies revealed that C-28 carboxylic Acid was essential for the cytotoxicity. The halo substituent at C-2 position in Betulinic Acid enhanced the cytotoxicity. Though the relation of the cytotoxicity with the nature of substituents at C-3 position could not be generalized but the ester functionality appeared to be a better substituent for enhancing the cytotoxicity. An interesting observation is that the three rings skeleton (A, B and C rings) had played an important role in eliciting anticancer activity, which could be a new molecular skeleton to design new anticancer drugs.
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Betulinic Acid and its derivatives as anti angiogenic agents
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Rama Mukherjee, Sanjay K Srivastava, Manu Jaggi, Praveen Rajendran, Mohammad Jamshed Ahmad Siddiqui, Anand Vardhan, Anand C BurmanAbstract:Abstract Betulinic Acid ( 1 ) significantly caused cytotoxicity to endothelial cell line ECV304 (IC 50 1.26 ± 0.44 μg/mL) in a 5-day MTT assay. Novel and more potent derivatives of Betulinic Acid ( 2 , 4 , 6 – 8 ) have been synthesized with IC 50 less than 0.4 μg/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further Betulinic Acid ( 1 ) inhibited TLS formation of ECV304 cells on Matrigel TM by 5.5% while its derivatives caused an inhibition of 13.1–49.2%.
Subash C Jonnalagadda - One of the best experts on this subject based on the ideXlab platform.
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synthesis and cytotoxicity of baylis hillman template derived Betulinic Acid triazole conjugates
Tetrahedron, 2017Co-Authors: Pathi Suman, Amardeep Patel, Lucas N Solano, Gayathri Jampana, Zachary S Gardner, Crystal M Holt, Subash C JonnalagaddaAbstract:Abstract Several alkynes and azides were prepared starting from Betulinic Acid and Baylis-Hillman reaction-derived allylic alcohols. These alkynes and azides were then coupled under click cycloaddition conditions to obtain functionalized Betulinic Acid-triazole conjugates. Similarly, pyrazinyl- and indolylBetulinic Acid-triazoles were also prepared employing cycloaddition chemistry. All the synthetic compounds were tested for their cytotoxicity against murine breast cancer (4T1) and human pancreatic cancer (MIA PaCa-2) cell lines. Based on these in vitro assays, two series of compounds have been identified as lead compounds for further development.
