Cancer is one of the main causes of death worldwide. There are several different types of cancer recognized thus far, which can be treated by different approaches including surgery, radiotherapy, chemotherapy or a combination thereof. However, these approaches have certain drawbacks and limitations. Photodynamic therapy (PDT) is regarded as an alternative noninvasive approach for cancer treatment based on the generation of toxic oxygen (known as reactive oxygen species (ROS)) at the treatment site. PDT requires photoactivation by a photosensitizer (PS) at a specific wavelength (λ) of light in the vicinity of molecular oxygen (singlet oxygen). The cell death mechanisms adopted in PDT upon PS photoactivation are necrosis, apoptosis and stimulation of the immune system. Over the past few decades, the use of natural compounds as a photoactive agent for the selective eradication of neoplastic lesions has attracted researchers’ attention. Many reviews have focused on the PS cell death mode of action and photonanomedicine approaches for PDT, while limited attention has been paid to the photoactivation of phytocompounds. Photoactivation is ever-present in nature and also found in natural plant compounds. The availability of various laser light setups can play a vital role in the discovery of photoactive phytocompounds that can be used as a natural PS. Exploring phytocompounds for their photoactive properties could reveal novel natural compounds that can be used as a PS in future pharmaceutical research. In this review, we highlight the current research regarding several photoactive phytocompound classes (furanocoumarins, alkaloids, poly-acetylenes and thiophenes, curcumins, flavonoids, anthraquinones, and natural extracts) and their photoactive potential to encourage researchers to focus on studies of natural agents and their use as a potent PS to enhance the efficiency of PDT.

Up-regulation of stress-activated proteins in cancer cells plays a protective role against photodynamic induced apoptosis. Post photodynamic therapy extracted normal rat liver tissue usually shows a fraction of surviving cells, the photodynamic resistant cells, residing in the necrotic region. To treat these photo-dynamic resistant cells a technique has been proposed based on fractionated drug administration of diluted photosensitizer, keeping the net concentration (5 mg/kg) constant, and subsequently varying drug light interval (DLI). Flourescence measurements were made for the presence of photosensitizer in a tissue. For qualitative analysis both histological and morphological studies were made. Although preliminary aim of this approach was not achieved but there were some interesting observation made i.e. for higher dilution of photosensitizer there was a sharp boundary between necrotic and normal portion of tissue. An increase in the absorption coefficient (α) from 2.7 → 2.9 was observed as photosensitizer was diluted while the corresponding threshold dose (D _th) persistently decreases from (0.10 → 0.02) J/cm² when irradiated with a 635 nm laser fluence of 150 J/cm².

Photosensitizers have been used for years to treat or diagnose several oncological diseases. In this research, we evaluate Rhodamine (Rh-640 perchlorate), a second-generation photosensitizer’s mediated preliminary photodynamic effects. To investigate these preliminary dose–response effects on the Rhabdomyosarcoma cancer cell line, the UV absorption spectra, standard curve, and cytotoxic analysis of Rh-640 perchlorate are demonstrated. The absorption spectra suggest that longer wavelengths of light like yellow-red light are best used for light irradiation. Different concentrations are used to evaluate absorbance and cytotoxic response. The results suggest that Rh-640 perchlorate may be used for the selective destruction of cancer cells without imposing any toxicity on normal cells in the dark. This research finding also suggests that its efficiency may also be evaluated on other cancer cell lines.