Structure-activity relationship of serotonin derived tocopherol lipids

Muripiti, Venkanna; Mujahid, Thasneem Yoosuf; Boddeda, Venkata Harsha Vardhan; Tiwari, Shrish; Marepally, Srujan; Patri, Srilakshmi V.; Gopal, Vijaya

doi:10.1016/j.ijpharm.2018.10.072

Cited by 11 publications

(16 citation statements)

References 56 publications

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“…In this context, we designed three new cationic lipid analogues as depicted in Figure 1 with variations in the head group region and a common α‐tocopherol based hydrophobic domain. α‐Tocopherol as anchoring group has extensively contributed in liposomal gene delivery in the recent past, through its membrane solubility, biocompatibility and antioxidant nature [22–26] . A control lipid (TA) was initially synthesized with α‐tocopherol as hydrophobic region and a cationic head group prone to substitution.…”

Section: Introductionmentioning

confidence: 99%

α‐Tocopherol‐Conjugated, Open Chain Sugar‐Mimicking Cationic Lipids: Design, Synthesis and In–Vitro Gene Transfection Properties

et al. 2021

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Sugar based cationic lipids are promising carriers of nucleic acids into various cells. Particularly, abundant hydroxyl functional groups in the sugar‐like moieties are believed to enhance target oriented uptake as well as biocompatibility. Towards this direction, we have synthesized three new cationic lipid analogues with or without sugar‐like multi‐hydroxyl functional head groups. Liposomal formulations of these lipids were developed and thoroughly characterized by means of DNA binding ability, size and zeta potential. Optimal lipid‐DNA complexes were determined by their transfection efficiency in HEK‐293 (Human embryonic kidney) cells. 1,4 gluconic γ‐lactone derived lipid (TS1) and ascorbic acid derived lipid (TS2), have exhibited 25‐fold and 12‐fold increase in transfected HEPG2 (human liver cancer) cells, respectively, when compared with a control lipid without sugar‐like moiety (TA). However, this property was reversed in the case of U87 (human primary glioblastoma) cell line. The results point out that the transfection efficiencies of sugar alcohol‐based cationic lipids are cell‐dependant. Cytotoxicity of the lipid complexes revealed that the sugar‐mimicking cationic lipids are non‐toxic as ≈80 % viable cells were observed in the treated cell lines. In conclusion, the current paper adds knowledge on the sugar based cationic lipids and reiterates that these lipids could yield potential applications towards liver targeted gene delivery.

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Section: Introductionmentioning

confidence: 99%

α‐Tocopherol‐Conjugated, Open Chain Sugar‐Mimicking Cationic Lipids: Design, Synthesis and In–Vitro Gene Transfection Properties

et al. 2021

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“…Hence it is necessary to deliver the genetic material into the targeted cell to cure such diseases. As of now, different types of nano-vectors [2][3][4][5] are being in use to deliver the desired gene into the cytosol [3][4][5][6] effectively. From the recent past, cationic lipids are also emerged as a new choice and extensively have been using as vectors (vehicles) in order to replace the novel gene in place of such a defective gene.…”

Section: Introductionmentioning

confidence: 99%

“…Generally, there exists a strong electrostatic interaction between the anionic phosphate backbone of deoxyribonucleic acid (DNA) and cationic part of lipid that affects the higher cellular uptake of the gene. [4][5][6][7] However, there is a problem with cationic lipids that, the highly positive surface charges can induce non-specific binding to the components of blood and may lead to less-transport efficacy and high toxicity. In this regard, to overcome the above anomalies, Zn(II)-coordinated cationic lipids are widely investigated and are expected to become ideal carriers for the gene delivery system (GDS) owing to their favourable bio-compatibilities and their sole structures.…”

Section: Introductionmentioning

confidence: 99%

“…From the recent past, cationic lipids are also emerged as a new choice and extensively have been using as vectors (vehicles) in order to replace the novel gene in place of such a defective gene. Generally, there exists a strong electrostatic interaction between the anionic phosphate backbone of deoxyribonucleic acid (DNA) and cationic part of lipid that affects the higher cellular uptake of the gene . However, there is a problem with cationic lipids that, the highly positive surface charges can induce non‐specific binding to the components of blood and may lead to less‐transport efficacy and high toxicity.…”

Section: Introductionmentioning

confidence: 99%

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Review of Zinc(II) Scaffolds: Efficient Role in Gene Delivery

Muripiti

Gondru²,

Patri

2020

ChemistrySelect

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Over the past two decades, enormous research has been focused on cationic non-viral vectors because of their advantages like flexible properties, easy synthesis, robustness, etc. It was also proved that, because of their efficient gene delivery properties, Zinc cationic lipids have received great attention as promising non-viral gene-delivery systems. Herewith, the review mainly aimed at the most recent scientific advances of Zinc-metal coordinative non-viral gene-delivery systems. The major progress in the fields of gene-delivery as well as tissue engineering applications are summarized in the current review.

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“…Vitamin E is a classical antioxidant due to properties free-radical scavenger (4) and has been used in treating reactive oxygen species (ROS) releated diseases (5). Vitamin E derivatives have been shown to be potent inducers of apoptosis in cancer cells because of their antioxidant activity.…”

Section: Introductionmentioning

confidence: 99%

Farmasötik Yumuşak Kapsülde α-Tokoferolün Spektrofotometri ile Kantitatif Tayini

Artuç¹

2020

Experimed

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Objective: Vitamin E is an essential micronutrient for maintaining a healthy status and preventing disease. The purpose of this study was to develop and validate a simple, sensitive and easily applicable spectrophotometric method for determination of α-tocopherol in pharmaceutical preparations. Material and Method: The quantitative determination of the α-tocopherol in pharmaceutical prepation was carried out using the maximum absorbance value measured at 290 nm. Calibration graphs were constructed by plotting the absorbance against the corresponding concentration of standart α-tocopherol samples at five different concentrations (10-100 µg/mL). Results: The amount of α-tocopherol in the pharmaceutical soft capsule was calculated as 101.572% (203.145 IU/capsule) (Evicap soft capsule labelled content: 200 IU/capsule). Conclusion: It suggested that the developed spectrophotometric method in this study is accurate, sensitive, precise, reproducible and easily applied to soft capsules and the other pharmaceutical preparations.

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Structure-activity relationship of serotonin derived tocopherol lipids

Cited by 11 publications

References 56 publications

α‐Tocopherol‐Conjugated, Open Chain Sugar‐Mimicking Cationic Lipids: Design, Synthesis and In–Vitro Gene Transfection Properties

α‐Tocopherol‐Conjugated, Open Chain Sugar‐Mimicking Cationic Lipids: Design, Synthesis and In–Vitro Gene Transfection Properties

Review of Zinc(II) Scaffolds: Efficient Role in Gene Delivery

Farmasötik Yumuşak Kapsülde α-Tokoferolün Spektrofotometri ile Kantitatif Tayini

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