Perspectives and challenges of tropical medicinal herbs and modern drug discovery in the current scenario

Kesharwani, Rajesh K.; Misra, Krishna; Singh, Dev Bukhsh

doi:10.4103/1995-7645.250337

Cited by 18 publications

(14 citation statements)

References 9 publications

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“…Aside of the toxicity of the currently applied drugs, the emergence of drug‐resistant parasite forms poses a growing problem to the clinician and, thus, the search for new potent anti‐parasitic drugs is ongoing. The treatment of trypanosomiasis and leishmaniasis with natural products or with drugs derived from them appears promising [3,13] . Naphthoquinones represent a significant group of secondary metabolites of plants and lichens with a variety of biological activities such as antioxidant and trypanocidal activities [3,13–15] .…”

Section: Introductionmentioning

confidence: 99%

“…The treatment of trypanosomiasis and leishmaniasis with natural products or with drugs derived from them appears promising [3,13] . Naphthoquinones represent a significant group of secondary metabolites of plants and lichens with a variety of biological activities such as antioxidant and trypanocidal activities [3,13–15] . The natural 2‐hydroxy‐1,4‐naphthoquinone (lawsone, 1a ) isolated from the Henna plant Lawsonia inermis showed biological activities including antibacterial effects and was applied as starting material for quinone drug candidates such as lapachol and atovaquone (ATO) [3,13–16] .…”

Section: Introductionmentioning

confidence: 99%

“…[3,13] Naphthoquinones represent a significant group of secondary metabolites of plants and lichens with a variety of biological activities such as antioxidant and trypanocidal activities. [3,[13][14][15] The natural 2-hydroxy-1,4-naphthoquinone (lawsone, 1a) isolated from the Henna plant Lawsonia inermis showed biological activities including antibacterial effects and was applied as starting material for quinone drug candidates such as lapachol and atovaquone (ATO). [3,[13][14][15][16] Modified lawsone derivatives with antitumor and antifungal activities are also known.…”

Section: Introductionmentioning

confidence: 99%

“…[3,[13][14][15] The natural 2-hydroxy-1,4-naphthoquinone (lawsone, 1a) isolated from the Henna plant Lawsonia inermis showed biological activities including antibacterial effects and was applied as starting material for quinone drug candidates such as lapachol and atovaquone (ATO). [3,[13][14][15][16] Modified lawsone derivatives with antitumor and antifungal activities are also known. [3,17,18] Quite a few lawsone derivatives were found efficacious against various parasites including Plasmodium falciparum, Leishmania donovani, Trypanosoma cruzi and Toxoplasma gondii.…”

Section: Introductionmentioning

confidence: 99%

“…H, m) 13. C-NMR (75.5 MHz, (D 6 )DMSO)) 36.2, 56.2, 57.1, 60.1, 111.5, 119.2, 120.4, 120.7, 125.8, 126.0, 126.8, 130.8, 131.0, 134.1, 134.4, 140.6, 143.6, 149.3, 153.4, 158.3, 176.8, 182.6; EI-MS: 424 (34) [M + ], 422 (100) [M + ], 387 (63), 251 (77).…”

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confidence: 99%

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New Pyrano‐4H‐benzo[g]chromene‐5,10‐diones with Antiparasitic and Antioxidant Activities

Nasr

Jentzsch

Shaikh

et al. 2020

Chemistry & Biodiversity

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New pyranonaphthoquinone derivatives were synthesized and investigated for their activity against Trypanosoma brucei, Leishmania major, and Toxoplasma gondii parasites. The pentafluorophenyl derivative was efficacious against T. brucei with single digit micromolar EC 50 values and against T. gondii with even submicromolar values. The 3-chloro-4,5-dimethoxyphenyl derivative showed an activity against amastigotes of Leishmania major parasites comparable to that of amphotericin B. In addition, antioxidant activities were observed for the bromophenyl derivatives, and their redox behavior was studied by cyclovoltammetry. Antiparasitic and antioxidative activities of the new naphthoquinone derivatives appear uncorrelated.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

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New Pyrano‐4H‐benzo[g]chromene‐5,10‐diones with Antiparasitic and Antioxidant Activities

Nasr

Jentzsch

Shaikh

et al. 2020

Chemistry & Biodiversity

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Garcinol from Garcinia indica inhibits HIV‐1 reverse transcriptase‐associated ribonuclease H

Corona

Seibt

Schaller

et al. 2021

Archiv der Pharmazie

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The bioactive components of Garcinia indica, garcinol (camboginol), and isogarcinol (cambogin), are suitable drug candidates for the treatment of various human diseases. HIV‐1‐RNase H assay was used to study the RNase H inhibition by garcinol and isogarcinol. Docking of garcinol into the active site of the enzyme was carried out to rationalize the difference in activities between the two compounds. Garcinol showed higher HIV‐1‐RNase H inhibition than the known inhibitor RDS1759 and retained full potency against the RNase H of a drug‐resistant HIV‐1 reverse transcriptase form. Isogarcinol was distinctly less active than garcinol, indicating the importance of the enolizable β‐diketone moiety of garcinol for anti‐RNase H activity. Docking calculations confirmed these findings and suggested this moiety to be involved in the chelation of metal ions of the active site. On the basis of its HIV‐1 reverse transcriptase‐associated RNase H inhibitory activity, garcinol is worth being further explored concerning its potential as a cost‐effective treatment for HIV patients.

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Activity of Fluorinated Curcuminoids against Leishmania major and Toxoplasma gondii Parasites

Khan

Koko

Nasr

et al. 2021

Chemistry & Biodiversity

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A new 3,4‐difluorobenzylidene analog of curcumin, CDF, was recently reported, which demonstrated significantly enhanced bioavailability and in vivo anticancer activity compared with curcumin. For highlighting the antiparasitic behavior of CDF, we tested this compound together with its new O‐methylated analog MeCDF against Leishmania major and Toxoplasma gondii parasites. Both CDF and MeCDF were tested in vitro against L. major and T. gondii. In addition, the in vitro cytotoxicity against Vero cells and macrophages was determined and selectivity indices were calculated. The DPPH radical scavenging activity assay was carried out in order to determine the antioxidant activity of the test compounds. Both compounds showed high activities against both parasite forms with EC50 values in the (sub‐)micromolar range (0.35 to 0.8 μM for CDF, 0.31 to 1.2 μM for MeCDF). The higher activity of CDF against L. major amastigotes when compared with MeCDF can in parts be attributed to the antioxidant activity of CDF while MeCDF lacking any antioxidant activity was more active than CDF against T. gondii parasites. In conclusion, CDF and MeCDF are promising antiparasitic drug candidates due to their high activities against L. major and T. gondii parasites.

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Perspectives and challenges of tropical medicinal herbs and modern drug discovery in the current scenario

Cited by 18 publications

References 9 publications

New Pyrano‐4H‐benzo[g]chromene‐5,10‐diones with Antiparasitic and Antioxidant Activities

New Pyrano‐4H‐benzo[g]chromene‐5,10‐diones with Antiparasitic and Antioxidant Activities

Garcinol from Garcinia indica inhibits HIV‐1 reverse transcriptase‐associated ribonuclease H

Activity of Fluorinated Curcuminoids against Leishmania major and Toxoplasma gondii Parasites

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